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R406 (Tamatinib)

Catalog No. A10770
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Syk 抑制剂

R406 (Tamatinib)是一种口服酪氨酸激酶抑制剂，IC50为41 nM。对Syk抑制作用强，但是不抑制Lyn，对Flt3的作用比对Syk低5倍。了解更多

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BI 2536

Catalog No. A10134
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PLK 抑制剂

BI 2536是Plk1的选择性抑制剂，可在低纳摩尔浓度下抑制Plk1酶的活性。了解更多

Product Citations (9)

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- Kei K Ito, .et al. Cep57 and Cep57L1 maintain centriole engagement in interphase to ensure centriole duplication cycle, J Cell Biol, 2021, Mar 1;220(3):e202005153 PMID: 33492359
- Ryuzaburo Yuki, .et al. The tyrosine kinase v-Src modifies cytotoxicities of anticancer drugs targeting cell division, J Cell Mol Med, 2021, Feb;25(3):1677-1687 PMID: 33465289
- Yamagishi A, .et al. Targeting Insulin-Like Growth Factor 1 Receptor Delays M-Phase Progression and Synergizes with Aurora B Inhibition to Suppress Cell Proliferation, Int J Mol Sci, 2020, Feb 5;21(3) PMID: 32033461
- Bucko PJ, .et al. Subcellular drug targeting illuminates local kinase action, Elife, 2019, Dec 24;8. pii: e52220 PMID: 31872801
- Watanabe K, .et al. The Cep57-pericentrin module organizes PCM expansion and centriole engagement, Nat Commun, 2019, Feb 25;10(1):931 PMID: 30804344
- Valérian Pasche, .et al. Screening a repurposing library, the Medicines for Malaria Venture Stasis Box, against Schistosoma mansoni, Parasit Vectors, 2018, 11: 298 PMID: 29764454
- Takeshi Wakida, .et al. The CDK-PLK1 axis targets the DNA damage checkpoint sensor protein RAD9 to promote cell proliferation and tolerance to genotoxic stress, eLife, 2017, 6: e29953 PMID: 29254517
- Majid Momeny, .et al. Dacomitinib, a pan-inhibitor of ErbB receptors, suppresses growth and invasive capacity of chemoresistant ovarian carcinoma cells, Sci Rep, 2017, 7: 4204 PMID: 28646172
- Ifuji A, .et al. A novel immunofluorescence method to visualize microtubules in the antiparallel overlaps of microtubule-plus ends in the anaphase and telophase midzone, Exp Cell Res, 2017, Nov 15;360(2):347-357 PMID: 28942021
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Pomalidomide (CC-4047)

Catalog No. A10743
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TNF-alpha 抑制剂

Pomalidomide (CC-4047)是沙利度胺的衍生物，在PBMCs中IC50为13 nM，并起免疫调节剂的作用。了解更多

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Trichostatin-A (TSA)

Catalog No. A10947
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HDAC 抑制剂

Trichostatin-A (TSA)是抑制HDAC 1、3、4、6和10，IC50值约为20 nM。了解更多

Product Citations (3)

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- Goudreault M, .et al. Afadin couples RAS GTPases to the polarity rheostat Scribble, Research Square, 2021, 22 Nov
- Hiroyuki Imuta, .et al. Histone methylation and demethylation are implicated in the transient and sustained activation of the interleukin-1β gene in murine macrophages, Heart Vessels, 2020, Jul 16 PMID: 32676696
- M??ndez-Blanco C, .et al. Stabilization of Hypoxia-Inducible Factors and BNIP3 Promoter Methylation Contribute to Acquired Sorafenib Resistance in Human Hepatocarcinoma Cells, Cancers (Basel), 2019, Dec 9;11(12). pii: E1984 PMID: 31835431
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Temsirolimus (Torisel)

Catalog No. A10906
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mTOR 抑制剂

Temsirolimus (Torisel)是mTOR的特异性抑制剂，会干扰调节肿瘤细胞增殖，生长和存活的蛋白质的合成。了解更多

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AT9283

Catalog No. A10095
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Aurora/JAK 抑制剂

AT9283抑制极光激酶A和B，并靶向与骨髓细胞增殖相关的其他酪氨酸和丝氨酸/苏氨酸激酶。了解更多

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- Tomoya Takeda, .et al. AT9283 exhibits antiproliferative effect on tyrosine kinase inhibitor-sensitive and -resistant chronic myeloid leukemia cells by inhibition of Aurora A and Aurora B, Oncol Rep, 2020, August 18
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Belinostat (PXD101)

Catalog No. A10122
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HDAC 抑制剂

Belinostat（PXD101）是一种HDAC抑制剂，可抑制HeLa细胞提取物中的HDAC活性，IC50为27 nM。了解更多

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- Shariful Islam, .et al. Resistance to histone deacetylase inhibitors confers hypersensitivity to oncolytic reovirus therapy, Blood Adv, 2020, 4(20): 5297-5310 PMID: 33108458
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Apixaban (BMS-562247-01)

Catalog No. A10082
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Factor Xa 抑制剂

Apixaban (BMS-562247-01)是一种抗凝剂，用于预防静脉血栓栓塞和静脉血栓栓塞事件。了解更多

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- Daniël Verhoef, .et al. Engineered factor Xa variants retain procoagulant activity independent of direct factor Xa inhibitors, Nat Commun, 2017, 8: 528 PMID: 28904343
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Streptozotocin (Zanosar)

Catalog No. A10868
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O-GlcNAcase 抑制剂

Streptozotocin (Streptozocin,Zanosar,STZ)用于医学研究中，用于产生1型糖尿病的动物模型，该模型直接抑制NCOAT酶在体外的O-GlcNAcase活性。了解更多

Product Citations (8)

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- Andressa Braga, .et al. Free interstitial levels of metformin in the liver of healthy and diabetic Wistar rats, Braz J Pharm Sci, 2022, 58: e19674
- Yuanyuan Du, .et al. Human pluripotent stem-cell-derived islets ameliorate diabetes in non-human primates, Nat Med, 2022, Feb;28(2):272-282 PMID: 35115708
- Karemah A. Alatawi, .et al. Coconut products alleviate hyperglycaemic, hyperlipidimic and nephropathy indices in streptozotocin-induced diabetic wistar rats, Saudi Journal of Biological Sciences, 2021, 25 June
- D.H. Mhya, .et al. Evaluation of Anti-hyperglycemic Effect of Sub-fractions Derived from Ethanol-aqueous Fraction of Balanites aegyptiaca Leaves in Streptozotocin-induced Diabetic Rats, Asian J Exp Biol Sci, 2019, 12 (2): 164-172
- Stanley I. R. Okoduwa, .et al. Validation of the antidiabetic effects of Vernonia amygdalina delile leaf fractions in fortified diet-fed streptozotocin-treated rat model of type-2 diabetes, J Diabetol, 2017, 8(3): 74-85
- Stanley I. R. Okoduwa, .et al. Anti-Diabetic Potential of Ocimum gratissimum Leaf Fractions in Fortified Diet-Fed Streptozotocin Treated Rat Model of Type-2 Diabetes, Medicines (Basel), 2017, Dec; 4(4): 73 PMID: 29019956
- Stanley I. R. Okoduwa, .et al. Appropriate Insulin Level in Selecting Fortified Diet-Fed, Streptozotocin-Treated Rat Model of Type 2 Diabetes for Anti-Diabetic Studies, PLoS One, 2017, 12(1): e0170971 PMID: 28129400
- Stanley I. R. Okoduwa, .et al. Evaluation of extraction protocols for anti-diabetic phytochemical substances from medicinal plants, World J Diabetes, 2016, Dec 15; 7(20): 605-614 PMID: 28031778
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Dovitinib (TKI-258)

Catalog No. A11411
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RTK 抑制剂

Dovitinib是一种小分子多靶点酪氨酸激酶抑制剂，可抑制通过ZNF198-FGFR1或BCR-FGFR1转化为IL3独立性的Ba / F3细胞，IC50值分别为150 nM和90 nM。了解更多

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- Yunping Hu, .et al. FGFR1/MAPK-directed brachyury activation drives PD-L1-mediated immune evasion to promote lung cancer progression, Cancer Lett, 2022, Oct 28;547:215867 PMID: 35985510
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VX-770 (Ivacaftor)

Catalog No. A10985
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CFTR activator

VX-770 (Ivacaftor)被称为CFTR增强剂，靶向作用于G551D-CFTR和F508del-CFTR，在fisher大鼠甲状腺细胞中EC50分别为100 nM和25 nM。了解更多

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- Okiyoneda T, .et al. Chaperone-Independent Peripheral Quality Control of CFTR by RFFL E3 Ligase, Dev Cell, 2018, Mar 26;44(6):694-708.e7 PMID: 29503157
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Foretinib (GSK1363089, XL880)

Catalog No. A10998
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c-MET 抑制剂

Foretinib (GSK1363089,XL880)是c-Met和VEGFR-2的多激酶抑制剂，可抑制增殖，诱导Anoikis并损害卵巢癌转移。了解更多

Product Citations (4)

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- Hamzehlou S, .et al. Anti-tumor activity of neratinib, a pan-HER inhibitor, in gastric adenocarcinoma cells, Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
- Hayato Ogura, .et al. TKI-addicted ROS1-rearranged cells are destined to survival or death by the intensity of ROS1 kinase activity, Sci Rep, 2017, 7: 5519 PMID: 28717217
- Fuse MJ, .et al. Mechanisms of Resistance to NTRK Inhibitors and Therapeutic Strategies in NTRK1-Rearranged Cancers, Mol Cancer Ther, 2017, Oct;16(10):2130-2143 PMID: 28751539
- Ryohei Katayama, .et al. Cabozantinib overcomes crizotinib resistance in ROS1 fusion positive cancer, Clin Cancer Res. , 2015, Jan 1; 21(1): 166–174. PMID: 25351743
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LY2157299

Catalog No. A11017
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TGF-βR 抑制剂

LY2157299是一种口服活性转化生长因子β受体（TGF-βR）激酶抑制剂。了解更多

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- Satoshi Endo, .et al. Flavonol glycosides of Rosa multiflora regulates intestinal barrier function through inhibiting claudin expression in differentiated Caco-2 cells, Nutr Res, 2019, 4 November
- Oguri G, .et al. Effects of methylglyoxal on human cardiac fibroblast: roles of transient receptor potential ankyrin 1 (TRPA1) channels., Am J Physiol Heart Circ Physiol., 2014, 307(9):H1339-52 PMID: 25172898
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BIBW2992 (Afatinib)

Catalog No. A10141
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EGFR 抑制剂

BIBW2992 (Afatinib)是酪氨酸激酶抑制剂（TKI），它不可逆地抑制人表皮生长因子受体2（Her2）和表皮生长因子受体（EGFR）激酶。了解更多

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- Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Van Sebille YZ, .et al. Use of zebrafish to model chemotherapy and targeted therapy gastrointestinal toxicity, Exp Biol Med (Maywood), 2019, Jun 11:1535370219855334 PMID: 31184924
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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AZD8931 (Sapitinib)

Catalog No. A10116
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pan-EGFR/pan-erbB 抑制剂

AZD8931 (Sapitinib)是ErbB1，ErbB2和ErbB3受体信号传导的等效抑制剂。了解更多

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- Takeshi Ito, .et al. Mathematical analysis of gefitinib resistance of lung adenocarcinoma caused by MET amplification, Biochem Biophys Res Commun, 2019, in Press
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Rapamycin (Sirolimus)

Catalog No. A10782
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mTOR 抑制剂

Rapamycin (Sirolimus)是通过抑制T细胞和B细胞对白介素2（IL-2）的反应来防止其活化。了解更多

Product Citations (9)

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- R Mahalakshmi, .et al. Hormetic effect of low doses of rapamycin triggers anti-aging cascades in WRL-68 cells by modulating an mTOR-mitochondria cross-talk, Mol Biol Rep, 2022, Jan;49(1):463-476 PMID: 34739690
- Yusuke Murase, .et al. Antitumor activity of the dual PI3K/mTOR inhibitor gedatolisib and the involvement of ABCB1 in gedatolisib resistance in canine tumor cells, Oncol Rep, 2022, Apr;47(4):61 PMID: 35088890
- Zhichao Wu, .et al. Prompt Graft Cooling Enhances Cardioprotection during Heart Transplantation Procedures through the Regulation of Mitophagy, Cells, 2021, Oct 27;10(11):2912 PMID: 34831135
- Matthew A Schaller, .et al. Ex vivo SARS-CoV-2 infection of human lung reveals heterogeneous host defense and therapeutic responses, JCI Insight, 2021, Sep 22;6(18):e148003 PMID: 34357881
- Matthew A. Schaller, .et al. In vitro infection of human lung tissue with SARS-CoV-2: Heterogeneity in host defense and therapeutic response, bioRxiv, 2021, January 21
- Ashley VanCleave, .et al. Development and characterization of the novel human osteosarcoma cell line COS-33 with sustained activation of the mTOR pathway, Oncotarget, 2020, Jul 7; 11(27): 2597-2610 PMID: 32676162
- Y Huang, .et al. STIM1 controls calcineurin/Akt/mTOR/NFATC2?mediated osteoclastogenesis induced by RANKL/M-CSF, Experimental and Therapeutic Medicine, 2020, 20(2), 736-747 PMID: 32742319
- Takuya Hirao, .et al. Altered intracellular signaling by imatinib increases the anti-cancer effects of tyrosine kinase inhibitors in chronic myelogenous leukemia cells, Cancer Sci, 2018, Jan; 109(1): 121-131 PMID: 29121435
- Ya-Hui Chen, .et al. The Different Effects of Atorvastatin and Pravastatin on Cell Death and PARP Activity in Pancreatic NIT-1 Cells, J Diabetes Res, 2016, 2016: 1828071 PMID: 28004006
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PCI-32765 (Ibrutinib)

Catalog No. A11020
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Bruton tyrosine kinase 抑制剂

PCI-32765 (Ibrutinib)是Bruton酪氨酸激酶（BTK）的口服生物利用小分子抑制剂，具有潜在的抗肿瘤活性。对Bmx，CSK，FGR，BRK及HCK适度有效，对EGFR，Yes，ErbB2，JAK3等作用效果较弱。了解更多

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- Simonowski A, .et al. Differential use of BTK and PLC in FcεRI- and KIT-mediated mast cell activation: A marginal role of BTK upon KIT activation, Biochim Biophys Acta Mol Cell Res, 2019, Dec 11;1867(4):118622 PMID: 31837347
- Carolin N. Zorn, .et al. Stimulus strength determines the BTK-dependence of the SHIP1-deficient phenotype in IgE/antigen-triggered mast cells, Sci Rep, 2018, 8: 15467 PMID: 30341350
- Li T, .et al. Bruton's tyrosine kinase potentiates ALK signaling and serves as a potential therapeutic target of neuroblastoma, Oncogene, 2018, Nov;37(47):6180-6194 PMID: 30013190
- Brittany M. Duggan, .et al. Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia, Sci Rep, 2017, 7: 1578 PMID: 28484277
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PD184352 (CI-1040)

Catalog No. A10212
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MEK1/2 抑制剂

PD184352 (CI-1040)是一种ATP非竞争性MEK1/2抑制剂，在基于细胞的测定中，IC50为17 nM，对MEK1/2的选择性是对MEK5的100倍。了解更多

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- Sachio Suzuki, .et al. A chemogenetic platform for controlling plasma membrane signaling and synthetic signal oscillation, Cell Chem Biol, 2022, Sep 15;29(9):1446-1464 PMID: 35835118
- Masaru Yoshikawa, .et al. Synthetic Protein Condensates That Inducibly Recruit and Release Protein Activity in Living Cells, J Am Chem Soc, 2021, May 5;143(17):6434-6446 PMID: 33890764
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Bortezomib (Velcade)

Catalog No. A10160
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Proteasome 抑制剂

Bortezomib (Velcade)是26S蛋白酶体的高度选择性，可逆抑制剂。了解更多

Product Citations (13)

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- Yoshitaka Sato, .et al. Epstein-Barr virus tegument protein BGLF2 in exosomes released from virus-producing cells facilitates de novo infection, Cell Commun Signal, 2022, Jun 21;20(1):95 PMID: 35729616
- Shin-Ichi Makino, .et al. Impairment of Proteasome Function in Podocytes Leads to CKD, J Am Soc Nephrol, 2021, Mar;32(3):597-613 PMID: 33510039
- Yusuke Yamashita, .et al. Targeting Adaptive IRE1α Signaling and PLK2 in Multiple Myeloma: Possible Anti-Tumor Mechanisms of KIRA8 and Nilotinib, Int J Mol Sci, 2020, Sep; 21(17): 6314 PMID: 32878237
- Nandini Verma, .et al. Synthetic lethal combination targeting BET uncovered intrinsic susceptibility of TNBC to ferroptosis, Sci Adv, 2020, 6 : eaba8968
- A Hayano, .et al. Cell-type-specific sensitivity of bortezomib in the methotrexate-resistant primary central nervous system lymphoma cells, Int J Clin Oncol, 2019, 1-10 PMID: 30993483
- Hiroshi Fukamachi, .et al. A subset of diffuse-type gastric cancer is susceptible to mTOR inhibitors and checkpoint inhibitors, J Exp Clin Cancer Res, 2019, 38:127 PMID: 30866995
- Y Sato, .et al. S-like phase CDKs stabilize the Epstein-Barr virus BDLF4 protein to temporally control late gene transcription, J Virol, 2019, Jan 30. pii: JVI.01707-18 PMID: 30700607
- Takashi Azuma, .et al. Removal of pharmaceuticals in water by introduction of ozonated microbubbles, SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Wenhan Deng, .et al. Variable Responses of MYC Translocation Positive Lymphoma Cell Lines To Different Combinations of Novel Agents: Impact of BCL2 Family Protein Expression, Transl Oncol, 2018, Oct; 11(5): 1147-1154 PMID: 30055346
- Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
- Hokyung K. Chung, .et al. Tunable and reversible drug control of protein production via a self-excising degron, Nat Chem Biol, 2015, Sep; 11(9): 713-720 PMID: 26214256
- S Raz, .et al. Severe hypoxia induces complete antifolate resistance in carcinoma cells due to cell cycle arrest, Cell Death Dis., 2014, 5(2): e1067 PMID: 24556682
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NVP-AEW541

Catalog No. A11021
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IGF-1R 抑制剂

NVP-AEW541是一种选择性的IGF-1R激酶抑制剂，可抑制IGF-1R的自磷酸化活性（IC50 = 0.086 uM）并阻止IGF-1介导的MCF-7细胞存活和增殖（IC50分别为0.16和1.64 uM）。了解更多

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- Tsushima H, .et al. Kinase inhibitors of the IGF-1R as a potential therapeutic agent for rheumatoid arthritis, Autoimmunity, 2017, Aug;50(5):329-335 PMID: 28682648
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Tipifarnib (Zarnestra)

Catalog No. A10935
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FTase 抑制剂

Tipifarnib (Zarnestra)是一种法尼基转移酶抑制剂，可在激酶途径变得过度活跃之前的翻译后修饰步骤中抑制Ras激酶。了解更多

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- Xiaoming Liu, .et al. Small extracellular vesicles induce resistance to anti-GD2 immunotherapy unveiling tipifarnib as an adjunct to neuroblastoma immunotherapy, J Immunother Cancer, 2022, Apr;10(4):e004399 PMID: 35483745
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AP24534 (Ponatinib)

Catalog No. A10080
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BCR-ABL 抑制剂

AP24534 (Ponatinib)是有效的多激酶和pan-BCR-ABL抑制剂。了解更多

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- Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Yamamoto Y, .et al. Development of a sandwich enzyme-linked immunosorbent assay for the quantification of ponatinib in serum, Anal Biochem, 2019, Feb 13. pii: S0003-2697(18)31083-2 PMID: 30771339
- N Naganna, .et al. Amino alkynylisoquinoline and alkynylnaphthyridine compounds potently inhibit acute myeloid leukemia proliferation in mice, EBioMedicine, 2019, Jan 24. pii: S2352-3964(19)30012-X PMID: 30686755
- Takuya Hirao, .et al. Altered intracellular signaling by imatinib increases the anti-cancer effects of tyrosine kinase inhibitors in chronic myelogenous leukemia cells, Cancer Sci, 2018, Jan; 109(1): 121-131 PMID: 29121435
- Brittany M. Duggan, .et al. Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia, Sci Rep, 2017, 7: 1578 PMID: 28484277
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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Mosapride citrate

Catalog No. A10607
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5-HT4-receptor 激动剂

Mosapride citrate起5-HT4受体激动剂和5-HT3受体拮抗剂的作用。了解更多

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Thiazovivin

Catalog No. A10928
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ROCK 抑制剂

Thiazovivin是一种Rho相关激酶（ROCK）的选择性抑制剂。了解更多

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U0126-EtOH

Catalog No. A10957
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MEK 抑制剂

U0126-EtOH是MEK1和MEK2的抑制剂，IC50分别为72 nM和58 nM。了解更多

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- Hanna Galganska, .et al. Carbon dioxide inhibits COVID-19-type proinflammatory responses through extracellular signal-regulated kinases 1 and 2, novel carbon dioxide sensors, Cell Mol Life Sci, 2021, Dec;78(24):8229-8242 PMID: 34741187
- Paul Mark Medina, .et al. Revealing the anticancer potential of candidate drugs in vivo using Caenorhabditis elegans mutant strains, Transl Oncol, 2021, Jan;14(1):100940 PMID: 33221682
- Byungki Jang, .et al. The Peptidylarginine Deiminase Inhibitor Cl-Amidine Suppresses Inducible Nitric Oxide Synthase Expression in Dendritic Cells, Int J Mol Sci, 2017, Nov; 18(11): 2258 PMID: 29077055
- Choe YJ, .et al. Nutlin-3 induces HO-1 expression by activating JNK in a transcription-independent manner of p53., Int J Oncol., 2014, 44(3):761-8. PMID: 24366007
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17-AAG (KOS953)

Catalog No. A10010
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HSP90 抑制剂

17-AAG (KOS953)是一种有效的HSP90抑制剂，无细胞试验中IC50为5 nM，作用于来自肿瘤细胞的HSP90比作用于来自正常细胞HSP90结合亲和力高100倍。了解更多

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- Yool Lee, .et al. Time-of-day specificity of anticancer drugs may be mediated by circadian regulation of the cell cycle, Sci Adv, 2021, 7
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AUY922 (Luminespib, NVP-AUY922)

Catalog No. A10659
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HSP90 抑制剂

AUY922 (Luminespib,NVP-AUY922)是一种高效的HSP90抑制剂，在Hsp90 FP结合测定中的IC50 = 21 nM，并在体外抑制多种人类癌细胞系的增殖，GI50平均为9 nM。Luminespib (AUY-922, NVP-AUY922)是一种高效的HSP90抑制剂，无细胞试验中作用于HSP90α/β的IC50为13 nM /21 nM，对HSP90家族成员GRP94和TRAP-1具有稍弱的作用，与任何小分子HSP90配体均可紧密结合。了解更多

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- Haruka Wakasa, .et al. Adverse Effects of High Temperature On Mammary Alveolar Development In Vitro, J Mammary Gland Biol Neoplasia, 2022, Jun;27(2):155-170 PMID: 35581442
- Hiroki Murano, .et al. A purine-type heat shock protein 90 inhibitor promotes the heat shock response in Arabidopsis, Plant Biotechnol Rep, 2017, 11:107-113
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BIIB021

Catalog No. A10143
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HSP90 抑制剂

BIIB021是一种口服全合成Hsp90抑制剂，可选择性和有效地抑制分子伴侣Hsp90。了解更多

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- Ting-Yu Chang, .et al. A novel histone deacetylase inhibitor MPT0L184 dysregulates cell-cycle checkpoints and initiates unscheduled mitotic signaling, Biomed Pharmacother, 2021, Jun;138:111485 PMID: 33740521
- Hiroki Murano, .et al. A purine-type heat shock protein 90 inhibitor promotes the heat shock response in Arabidopsis, Plant Biotechnol Rep, 2017, 11:107-113
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BMS-790052 (Daclatasvir)

Catalog No. A10159
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HCV NS5A 抑制剂

BMS-790052 (Daclatasvir)是一种高度选择性的HCV NS5A抑制剂，EC50为9-50 pM，用于治疗丙型肝炎病毒（HCV）感染。了解更多

Product Citations (3)

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- TS Wahyuni, .et al. Enhancement of Anti-Hepatitis C Virus Activity by the Combination of Chalepin From Ruta Angustifolia and Current Antiviral Drugs, Southeast Asian J Trop Med public health, 2020, 51(1)
- Miyayama Y, .et al. Comparative study on the replication of HCV1b genome between wild type and cell culture adaptive mutant in regard to sensitivities against anti-HCV drugs, Microbiol Immunol, 2019, Dec 19 PMID: 31854467
- Sato K, .et al. Elevated serum uric acid level was a notable adverse event during combination therapy with sofosbuvir and ribavirin, Hepatol Res, 2018, Feb;48(3):E347-E353 PMID: 28834004
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Cediranib (AZD2171)

Catalog No. A10185
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VEGFR 抑制剂

Cediranib (AZD2171)是一种高效的VEGFR(KDR)抑制剂，此外对c-Kit和PDGFRβ也具有相似的抑制活性，对VEGFR的选择性比PDGFR-α，CSF-1R和Flt3分别高36倍，110倍和1000倍以上。了解更多

Product Citations (2)

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- Majid Momeny, .et al. Cediranib, a pan-inhibitor of vascular endothelial growth factor receptors, inhibits proliferation and enhances therapeutic sensitivity in glioblastoma cells, Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Majid Momeny, .et al. Cediranib, an inhibitor of vascular endothelial growth factor receptor kinases, inhibits proliferation and invasion of prostate adenocarcinoma cells, Eur J Pharmacol, 2020, 882:173298
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Olaparib (AZD2281)

Catalog No. A10111
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PARP 抑制剂

Olaparib (AZD2281)是聚ADP核糖聚合酶（PARP）的抑制剂，该酶是一种与DNA修复有关的酶。了解更多

Product Citations (28)

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- Saptarshi Sinha, .et al. Olaparib enhances the Resveratrol-mediated apoptosis in breast cancer cells by inhibiting the homologous recombination repair pathway, Exp Cell Res, 2022, Nov 1;420(1):113338 PMID: 36075449
- Subhajit Chatterjee, .et al. Combination of talazoparib and olaparib enhanced the curcumin-mediated apoptosis in oral cancer cells by PARP-1 trapping, J Cancer Res Clin Oncol, 2022, Dec;148(12):3521-3535 PMID: 35962813
- Yuki Uchihara, .et al. DNA damage promotes HLA class I presentation by stimulating a pioneer round of translation-associated antigen production, Mol Cell, 2022, Jul 21;82(14):2557-2570 PMID: 35594857
- Ji-Ye Kim, .et al. ARL6IP5 reduces cisplatin-resistance by suppressing DNA repair and promoting apoptosis pathways in ovarian carcinoma, Cell Death Dis, 2022, Mar 15;13(3):239 PMID: 35293383
- Emad Matanes, .et al. Inhibition of Poly ADP-Ribose Glycohydrolase Sensitizes Ovarian Cancer Cells to Poly ADP-Ribose Polymerase Inhibitors and Platinum Agents, Front Oncol, 2021, Oct 27;11:745981 PMID: 34778062
- Shino Endo, .et al. BRCA1/ATF1-Mediated Transactivation is Involved in Resistance to PARP Inhibitors and Cisplatin, Cancer Res Commun, 2021, 1(2): 90-105
- Yan Baglo, .et al. Evolutionary dynamics of cancer multidrug resistance in response to olaparib and photodynamic therapy, Transl Oncol, 2021, Nov;14(11):101198 PMID: 34418731
- Joseph M Gozgit, .et al. PARP7 negatively regulates the type I interferon response in cancer cells and its inhibition triggers antitumor immunity, Cancer cell, 2021, Jul 22;S1535-6108(21)00340-8 PMID: 34375612
- Sefinew Molla, .et al. Olaparib enhances curcumin-mediated apoptosis in oral cancer cells by inducing PARP trapping through modulation of BER and chromatin assembly, DNA Repair (Amst), 2021, Jun 10;105:103157 PMID: 34144488
- Jianming Wang, .et al. Persistence of RNA transcription during DNA replication delays duplication of transcription start sites until G2/M, Cell Rep, 2021, Feb 16;34(7):108759 PMID: 33596418
- Ai Ito, .et al. Metolazone upregulates mitochondrial chaperones and extends lifespan in Caenorhabditis elegans, Biogerontology, 2021, Feb;22(1):119-131 PMID: 33216250
- Tim J Wigle, .et al. In Vitro and Cellular Probes to Study PARP Enzyme Target Engagement, Cell Chem Biol, 2020, Jul 16;27(7):877-887 PMID: 32679093
- Ali Divan, .et al. Structurally unique PARP-1 inhibitors for the treatment of prostate cancer, Pharmacol Res Perspect, 2020, Apr; 8(2): e00586 PMID: 32342655
- Jianwei Dou, .et al. Development and evaluation of poly adenosine 5'-diphosphate-ribose polymerase 1 immobilization-based receptor chromatography, J Sep Sci, 2020, Dec 4 PMID: 33275824
- Sai Dimple Manavitha Gullipalli, .et al. Development and Validation of Bioanalytical Method for Estimation of Niraparib in Rat Plasma Using High Performance LC-MS/MS And Its Application to Pharmacokinetic Study, Int. J. Adv. Pharm. Biotech, 2020, 6(2) 01-08
- Chao Zhang, .et al. Phenotypic Switching of Atherosclerotic Smooth Muscle Cells is Regulated by Activated PARP1-Dependent TET1 Expression, J Atheroscler Thromb, 2020, Sep 25 PMID: 32981917
- Wigle TJ, .et al. Forced Self-Modification Assays as a Strategy to Screen MonoPARP Enzymes, SLAS Discov, 2019, Dec 19:2472555219883623 PMID: 31855104
- Wang Q, .et al. Biguanides in combination with olaparib limits tumorigenesis of drug-resistant ovarian cancer cells through inhibition of Snail, Cancer Med, 2019, Dec 21 PMID: 31863638
- Molla S, .et al. PARP inhibitor Olaparib Enhances the Apoptotic Potentiality of Curcumin by Increasing the DNA Damage in Oral Cancer Cells through Inhibition of BER Cascade, Pathol Oncol Res, 2019, Nov 25 PMID: 31768967
- Alvin Z.Lu, .et al. Enabling drug discovery for the PARP protein family through the detection of mono-ADP-ribosylation, Biochem Pharmacol, 2019, May 7. pii: S0006-2952(19)30171-6 PMID: 31075269
- Bian C, .et al. NADP+ is an endogenous PARP inhibitor in DNA damage response and tumor suppression, Nat Commun, 2019, Feb 11;10(1):693 PMID: 30741937
- HC de Silva, .et al. IGFBP-3 interacts with NONO and SFPQ in PARP-dependent DNA damage repair in triple-negative breast cancer, Cell Mol Life Sci, 2019, 1-16 PMID: 30725116
- Kamada Y, .et al. Castalagin and vescalagin purified from leaves of Syzygium samarangense (Blume) Merrill & L.M. Perry: Dual inhibitory activity against PARP1 and DNA topoisomerase II, Fitoterapia, 2018, Sep;129:94-101 PMID: 29928967
- 2018, .et al. Augmentation of the therapeutic efficacy of WEE1 kinase inhibitor AZD1775 by inhibiting the YAP-E2F1-DNA damage response pathway axis, FEBS Open Bio, 2018, Jun; 8(6): 1001-1012 PMID: 29928579
- Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
- Hiro Sato, .et al. DNA double-strand break repair pathway regulates PD-L1 expression in cancer cells, Nat Commun, 2017, 8: 1751 PMID: 29170499
- Charles-André Philip, .et al. Inhibition of PI3K-AKT-mTOR pathway sensitizes endometrial cancer cell lines to PARP inhibitors, BMC Cancer, 2017, 17: 638 PMID: 28886696
- Rulina AV, .et al. Distinct outcomes of CRL-Nedd8 pathway inhibition reveal cancer cell plasticity, Cell Death Dis, 2016, Dec 1;7(12):e2505 PMID: 27906189
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RAF265 (CHIR-265)

Catalog No. A10773
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RAF/VEGFR 抑制剂

RAF265 (CHIR-265)是一种口服，高度选择性的RAF和VEGFR激酶抑制剂，可控制或正常化VEGFR-2，同时抑制B-raf和c-Raf突变以预防癌症。了解更多

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VX-809 (Lumacaftor)

Catalog No. A10986
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CFTR modulator

VX-809 (Lumacaftor)是用于治疗囊性纤维化（CF）的第二种口服研究候选化合物，通过促进突变型CFTR(F508del-CFTR)的成熟，从而纠正囊性纤维症中常见的CFTR突变，在fisher大鼠甲状腺细胞中EC50为0.1 μM。了解更多

Product Citations (4)

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- Kusumika Saha, .et al. Pharmacological chaperone-rescued cystic fibrosis CFTR-F508del mutant overcomes PRAF2-gated access to endoplasmic reticulum exit sites, Cell Mol Life Sci, 2022, Sep 27;79(10):530 PMID: 36167862
- Heledd H Jarosz-Griffiths, .et al. Different CFTR Modulator Combinations Downregulate Inflammation Differently in Cystic Fibrosis, Elife, 2020, Mar 2;9:e54556 PMID: 32118580
- Okiyoneda T, .et al. Chaperone-Independent Peripheral Quality Control of CFTR by RFFL E3 Ligase, Dev Cell, 2018, Mar 26;44(6):694-708.e7 PMID: 29503157
- Junko Kido, .et al. Cystic Fibrosis Transmembrane Conductance Regulator Reduces Microtubule-Dependent Campylobacter jejuni Invasion, Infect Immun, 2017, Oct; 85(10): e00311-17 PMID: 28784926
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Y-27632 2HCl

Catalog No. A11001
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ROCK 抑制剂

Y-27632是一种Rho相关的线圈激酶（ROCK）抑制剂，可提高人类胚胎干细胞（hESCs）的克隆效率。比对其他激酶包括PKC，cAMP依赖性蛋白激酶，MLCK和PAK的作用强200多倍。了解更多

Product Citations (27)

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- Sergio Pedraza-Arevalo, .et al. Differentiation of beta-like cells from human induced pluripotent stem cell-derived pancreatic progenitor organoids, STAR Protoc, 2022, Aug 30;3(3):101656 PMID: 36092820
- Ji-Hyun Lee, .et al. p57Kip2 imposes the reserve stem cell state of gastric chief cells, Cell Stem Cell, 2022, May 5; 29(5): 826-839 PMID: 35523142
- Adam Pietrobon, .et al. Renal organoid modeling of tuberous sclerosis complex reveals lesion features arise from diverse developmental processes, Cell Rep, 2022, Jul 5;40(1):111048 PMID: 35793620
- Sarkawt Hamad, .et al. High-efficient serum-free differentiation of endothelial cells from human iPS cells, Stem Cell Res Ther, 2022, Jun 11;13(1):251 PMID: 35690874
- Stasia Krishtul, .et al. Development of a bioactive microencapsulation platform incorporating decellularized extracellular matrix to entrap human induced pluripotent stem cells for versatile biomedical applications, Polym Adv Technol, 2022, 33( 11): 3842-3852
- Peter T Ruane, .et al. Trophectoderm differentiation to invasive syncytiotrophoblast is promoted by endometrial epithelial cells during human embryo implantation, Hum Reprod, 2022, Apr 1;37(4):777-792 PMID: 35079788
- Takayuki Miyoshi, .et al. Successful induction of human chemically induced liver progenitors with small molecules from damaged liver, J Gastroenterol, 2022, Jun;57(6):441-452 PMID: 35294680
- Ana-Maria Cujba, .et al. An HNF1α truncation associated with maturity-onset diabetes of the young impairs pancreatic progenitor differentiation by antagonizing HNF1β function, Cell Rep, 2022, Mar 1;38(9):110425 PMID: 35235779
- Dan Zhao, .et al. From crypts to enteroids: establishment and characterization of avian intestinal organoids, Poult Sci, 2022, Mar; 101(3): 101642 PMID: 35016046
- Antigoni Gogolou, .et al. Generating Enteric Nervous System Progenitors from Human Pluripotent Stem Cells, Curr Protoc, 2021, Jun;1(6):e137 PMID: 34102038
- Tiago De Oliveira, .et al. Effects of the Novel PFKFB3 Inhibitor KAN0438757 on Colorectal Cancer Cells and Its Systemic Toxicity Evaluation In Vivo, Cancers (Basel), 2021, Mar 2;S2451-9456(21)00095-7 PMID: 33671096
- Denise Muller, .et al. Functional apoptosis profiling identifies MCL-1 and BCL-xL as prognostic markers and therapeutic targets in advanced thymomas and thymic carcinomas, BMC Med, 2021, Nov 16;19(1):300 PMID: 34781947
- Ayumi Horikawa, .et al. A simple method of hiPSCs differentiation into insulin-producing cells is improved with vitamin C and RepSox, PloS one, 2021, Jul 12;16(7):e0254373 PMID: 34252142
- Hayato Mizuta, .et al. Gilteritinib overcomes lorlatinib resistance in ALK-rearranged cancer, Nat Commun, 2021, Feb 24;12(1):1261 PMID: 33627640
- Scott Bell, .et al. Lesch-Nyhan disease causes impaired energy metabolism and reduced developmental potential in midbrain dopaminergic cells, Stem Cell Reports, 2021, Jul 13;16(7):1749-1762 PMID: 34214487
- Shenyang Li, .et al. Effect of porcine corneal stromal extract on keratocytes from SMILE-derived lenticules, J Cell Mol Med, 2020, Dec 20;25(2):1207-1220 PMID: 33342057
- Takao FUCHIGAMI, .et al. Ameloblastoma cell lines derived from different subtypes demonstrate distinct developmental patterns in a novel animal experimental model, J Appl Oral Sci, 2020, 28: e20190558 PMID: 32348439
- Jing-Yu Lin, .et al. In vitro expansion of pancreatic islet clusters facilitated by hormones and chemicals, Cell Discov, 2020, 6: 20 PMID: 32284878
- Yu Huang, .et al. Development of Bifunctional Three-Dimensional Cysts from Chemically Induced Liver Progenitors, Stem Cells Int, 2019, 2019: 3975689 PMID: 31565060
- XinYan, .et al. Establishment of CSUASOi001-A, a non-integrated induced pluripotent stem cell line from urine-derived cells of a Chinese patient carrying RS1 gene mutation, Stem Cell Res, 2019, May 17 PMID: 31141763
- Daniela F. Duarte Campos, .et al. Corneal bioprinting utilizing collagen?\based bioinks and primary human keratocytes, J Biomed Mater Res A, 2019, April 22 PMID: 31012205
- Scott Bell, .et al. Mutations in ACTL6B Cause Neurodevelopmental Deficits and Epilepsy and Lead to Loss of Dendrites in Human Neurons, Am J Hum Genet, 2019, May 2;104(5):815-834 PMID: 31031012
- Ooi J, .et al. Unbiased Profiling of Isogenic Huntington Disease hPSC-Derived CNS and Peripheral Cells Reveals Strong Cell-Type Specificity of CAG Length Effects, Cell Rep, 2019, Feb 26;26(9):2494-2508 PMID: 30811996
- Scott Bell, .et al. Disruption of GRIN2B Impairs Differentiation in Human Neurons, Stem Cell Reports, 2018, Jul 10; 11(1):183-196 PMID: 29937144
- Christina Zarouchlioti, .et al. Antisense Therapy for a Common Corneal Dystrophy Ameliorates TCF4 Repeat Expansion-Mediated Toxicity, Am J Hum Genet, 2018, Apr 5; 102(4): 528-539 PMID: 29526280
- Ai Takemoto, .et al. A critical role of platelet TGF-β release in podoplanin-mediated tumour invasion and metastasis, Sci Rep, 2017, 7: 42186 PMID: 28176852
- Scott Bell, .et al. A Rapid Pipeline to Model Rare Neurodevelopmental Disorders with Simultaneous CRISPR/Cas9 Gene Editing, Stem Cells Transl Med, 2017, Mar; 6(3): 886-896 PMID: 28170165
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ZSTK474

Catalog No. A11014
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PI3K 抑制剂

ZSTK474是I类磷脂酰肌醇3激酶同工型的ATP竞争性抑制剂。了解更多

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- Pridham KJ, .et al. PIK3CB/p110β is a selective survival factor for glioblastoma, Neuro Oncol, 2018, Mar 27;20(4):494-505 PMID: 29016844
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LBH589 (Panobinostat)

Catalog No. A10518
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HDAC 抑制剂

LBH589是异羟肟酸，用作非选择性HDAC抑制剂，HDAC1的IC5o为0.23 nM。了解更多

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- Jalila Chagraoui, .et al. UM171 Preserves Epigenetic Marks that Are Reduced in Ex Vivo Culture of Human HSCs via Potentiation of the CLR3-KBTBD4 Complex, Cell Stem Cell, 2021, Jan 7;28(1):48-62.e6 PMID: 33417871
- Gils Jose, .et al. Co-Delivery of CPT-11 and Panobinostat with Anti-GD2 Antibody Conjugated Immunoliposomes for Targeted Combination Chemotherapy, Cancers (Basel), 2020, Oct 31;12(11):E3211 PMID: 33142721
- Shariful Islam, .et al. Resistance to histone deacetylase inhibitors confers hypersensitivity to oncolytic reovirus therapy, Blood Adv, 2020, 4(20): 5297-5310 PMID: 33108458
- Giovanni Bocci, .et al. Virtual and In Vitro Antiviral Screening Revive Therapeutic Drugs for COVID-19, ACS Pharmacol Transl Sci, 2020, Oct 14
- Justin Kale, .et al. Phosphorylation switches Bax from promoting to inhibiting apoptosis thereby increasing drug resistance, EMBO Rep, 2018, Sep; 19(9): e45235 PMID: 29987135
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IC-87114

Catalog No. A10463
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PI3K 抑制剂

IC-87114是首个同种型选择性PI3K抑制剂:p110M-NM-4(IC50 = 0.13 M-BM-5M)与p110M-NM-1(IC50 = 200 M-BM-5M)、p110M-NM-2(IC50 = 16 M-BM-5M)和p110M-NM-3(IC50 = 61 M-BM-5M)。了解更多

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AZD1152-HQPA (Barasertib)

Catalog No. A10109
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Aurora Kinase B 抑制剂

AZD1152-HQPA (Barasertib)是Aurora B的高效抑制剂，Ki值分别为0.36（Aurora B）和1369 nM（Aurora A），与一组其他50种激酶相比具有很高的特异性。了解更多

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- Sakamoto K, .et al. Recurrent 8q24 rearrangement in blastic plasmacytoid dendritic cell neoplasm: association with immunoblastoid cytomorphology, MYC expression, and drug response, Leukemia, 2018, May 23 PMID: 29795241
- Jennifer M. Sahni, .et al. Bromodomain and Extraterminal Protein Inhibition Blocks Growth of Triple-negative Breast Cancers through the Suppression of Aurora Kinases, J Biol Chem, 2016, Nov 4; 291(45): 23756-23768 PMID: 27650498
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AZD7762

Catalog No. A10113
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Chk1 & Chk2 抑制剂

AZD7762是一种有效的ATP竞争性检查点激酶抑制剂，可促进检查点废止并增强DNA靶向疗法。了解更多

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PI-103

Catalog No. A10726
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PI3K 抑制剂

PI-103是一种有效的，细胞可渗透的，ATP竞争性磷脂酰肌醇3激酶（PI3K）家族抑制剂，对DNA-PK，PI3K（p110α）和mTOR具有选择性。了解更多

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- Diane Yang, .et al. Pancreatic Differentiation of Stem Cells Reveals Pathogenesis of a Syndrome of Ketosis-Prone Diabetes, Diabetes, 2021, Oct;70(10):2419-2429 PMID: 34344789
- Byungki Jang, .et al. The Peptidylarginine Deiminase Inhibitor Cl-Amidine Suppresses Inducible Nitric Oxide Synthase Expression in Dendritic Cells, Int J Mol Sci, 2017, Nov; 18(11): 2258 PMID: 29077055
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XL147 analogue

Catalog No. A10995
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PI3K 抑制剂

XL147 analogue是一种有效的，选择性的，口服可生物利用的I类磷脂酰肌醇3激酶（PI3K）小分子抑制剂，作用于PI3Kα/δ/γ，对PI3Kβ作用效果稍弱。具有潜在的抗肿瘤活性。了解更多

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- Yushi Hayashida, .et al. Invention of a novel photodynamic therapy for tumors using a photosensitizing PI3K inhibitor, Int J Cancer, 2016, Aug 1;139(3):700-11 PMID: 26989815
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CAL-101 (GS-1101, Idelalisib)

Catalog No. A10172
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PI3K 抑制剂

CAL-101 (GS-1101,Idelalisib)是PI3K的同种型选择性抑制剂，可诱导慢性淋巴细胞性白血病（CLL）细胞凋亡。了解更多

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- Ming-Chun Hung, .et al. AKT phosphorylation as a predictive biomarker for PI3K/mTOR dual inhibition-induced proteolytic cleavage of mTOR companion proteins in small cell lung cancer, Cell Biosci, 2022, 12: 122 PMID: 35918763
- Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
- Pridham KJ, .et al. PIK3CB/p110β is a selective survival factor for glioblastoma, Neuro Oncol, 2018, Mar 27;20(4):494-505 PMID: 29016844
- Yoshihiro Umezawa, .et al. Molecular mechanisms for enhancement of stromal cell-derived factor 1?Cinduced chemotaxis by platelet endothelial cell adhesion molecule 1 (PECAM-1), J Biol Chem, 2017, Dec 1; 292(48): 19639-19655 PMID: 28974577
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GSK1059615

Catalog No. A10438
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mTOR/PI3K 抑制剂

GSK1059615是PI3Kα (IC50 = 2 nM)的强效、可逆、ATP竞争性噻唑烷二酮抑制剂。了解更多

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- Jing Xie, .et al. GSK1059615 kills head and neck squamous cell carcinoma cells possibly via activating mitochondrial programmed necrosis pathway, Oncotarget, 2017, Aug 1; 8(31): 50814-50823 PMID: 28881606
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TG100-115

Catalog No. A10922
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PI3K 抑制剂

TG100-115是一种PI3Kγ/δ抑制剂（IC50值分别为83和235 nM）。了解更多

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Gefitinib (Iressa)

Catalog No. A10422
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EGFR 抑制剂

Gefitinib (Iressa)是一种EGFR抑制剂，可阻断靶细胞中表皮生长因子受体(EGFR)的信号传导。了解更多

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- Hamzehlou S, .et al. Anti-tumor activity of neratinib, a pan-HER inhibitor, in gastric adenocarcinoma cells, Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
- Mansi Srivastava, .et al. Inhibition of the TIRAP-c-Jun interaction as a therapeutic strategy for AP1-mediated inflammatory responses, Int Immunopharmacol, 2019, 71: 188-197 PMID: 30909134
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Erlotinib HCl

Catalog No. A10362
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EGFR 抑制剂

Erlotinib hydrochloride是一种可逆的酪氨酸激酶抑制剂，作用于表皮生长因子受体（EGFR）。了解更多

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- Yuta Yamamoto, .et al. Quantitative determination of erlotinib in human serum using competitive enzyme-linked immunosorbent assay, J Pharm Anal, 2018, Apr; 8(2): 119-123 PMID: 29736298
- Aikawa S, .et al. Proliferation of mouse endometrial stromal cells in culture is highly sensitive to lysophosphatidic acid signaling, Biochem Biophys Res Commun, 2017, Feb 26;484(1):202-208 PMID: 28073697
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Lapatinib Ditosylate

Catalog No. A10514
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HER2 抑制剂

Lapatinib是一种双重酪氨酸激酶抑制剂，可阻断HER2生长受体途径。了解更多

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AG-1478 (Tyrphostin AG-1478)

Catalog No. A11022
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EGFR 抑制剂

AG-1478 (Tyrphostin AG-1478)是EGFR激酶的抑制剂，IC50值为3 nM。了解更多

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- Khattab M, .et al. Conformational Plasticity in Tyrosine Kinase Inhibitor-Kinase Interactions Revealed with Fluorescence Spectroscopy and Theoretical Calculations, J Phys Chem B, 2018, May 3;122(17):4667-4679 PMID: 29629773
- Muhammad Khattab, .et al. A pH-induced conformational switch in a tyrosine kinase inhibitor identified by electronic spectroscopy and quantum chemical calculations, Sci Rep, 2017, 7: 16271 PMID: 29176733
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Everolimus (RAD001)

Catalog No. A10374
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mTOR 抑制剂

Everolimus (RAD001)是西罗莫司的40-O-(2-羟乙基)衍生物，与西罗莫司作为mTOR抑制剂的作用相似。了解更多

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- Ming-Chun Hung, .et al. AKT phosphorylation as a predictive biomarker for PI3K/mTOR dual inhibition-induced proteolytic cleavage of mTOR companion proteins in small cell lung cancer, Cell Biosci, 2022, 12: 122 PMID: 35918763
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Tivozanib (AV-951)

Catalog No. A10101
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VEGFR 抑制剂

Tivozanib (AV-951)是一种口服VEGF受体酪氨酸激酶抑制剂，旨在抑制所有三种VEGF受体。了解更多

Product Citations (6)

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- Majid Momeny, .et al. Cediranib, a pan-inhibitor of vascular endothelial growth factor receptors, inhibits proliferation and enhances therapeutic sensitivity in glioblastoma cells, Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Majid Momeny, .et al. Cediranib, an inhibitor of vascular endothelial growth factor receptor kinases, inhibits proliferation and invasion of prostate adenocarcinoma cells, Eur J Pharmacol, 2020, 882:173298
- Majid Momeny, .et al. Anti-tumour activity of tivozanib, a pan-inhibitor of VEGF receptors, in therapy-resistant ovarian carcinoma cells, Sci Rep, 2017, 7: 45954 PMID: 28383032
- Majid Momeny, .et al. Blockade of vascular endothelial growth factor receptors by tivozanib has potential anti-tumour effects on human glioblastoma cells, Sci Rep, 2017, 7: 44075 PMID: 28287096
- Nicholas A. Manieri, .et al. Mucosally transplanted mesenchymal stem cells stimulate intestinal healing by promoting angiogenesis, J Clin Invest, 2015, Sep 1; 125(9): 3606-3618 PMID: 26280574
- Usui T, .et al. Brain-derived neurotrophic factor promotes angiogenic tube formation through generation of oxidative stress in human vascular endothelial cells., Acta Physiol (Oxf), 2014, 211, 385-394 PMID: 24612679

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