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搜索结果：“AG+490”

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AG-490

Catalog No. A10047
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EGFR 抑制剂

AG 490是EGF受体酪氨酸激酶的选择性抑制剂 (EGFR和ErbB2的IC50值分别为2和13.5μM)。也抑制对Lck，Lyn，Btk，Syk和Src无活性的JAK2。了解更多

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- Matozaki M, .et al. Involvement of Stat3 phosphorylation in mild heat shock-induced thermotolerance, Exp Cell Res, 2019, Feb 15. pii: S0014-4827(18)31030-9 PMID: 30776355
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GW2580

Catalog No. A11959
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CSF-1R 抑制剂

GW2580是cFMS激酶的小分子，ATP竞争性抑制剂。了解更多

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- Ravikanth Maddipati, .et al. MYC controls metastatic heterogeneity in pancreatic cancer, bioRxiv, 2021, February 01
- Liu M, .et al. Metabolic rewiring of macrophages by CpG potentiates clearance of cancer cells and overcomes tumor-expressed CD47-mediated 'don't-eat-me' signal, Nat Immunol, 2019, Jan 21 PMID: 30664738
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AG1295

Catalog No. A17227
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PDGFR 抑制剂

AG1295 is a PDGF receptor specific inhibitor. 了解更多

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AG 555

Catalog No. A18337
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EGFR 抑制剂

AG555 is a potent epidermal growth factor receptor (EGFR) kinase inhibitor. 了解更多

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PD166866

Catalog No. A17161
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FGFR 抑制剂

PD166866是FGFR1抑制剂，IC50值为55 nM，对c-Src，PDGFR-b，EGFR或胰岛素受体酪氨酸激酶或MEK，PKC和CDK4无影响。了解更多

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Avitinib (AC0010)

Catalog No. A16826
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irreversible EGFR 抑制剂

Avitinib (AC0010)是一种基于吡咯并嘧啶的不可逆EGFR抑制剂，对EGFR L858R/T790M双重突变具有突变选择性，IC50值为0.18 nM，效力比野生型EGFR（IC50值为7.68 nM）高近43倍。它具有可比的抗肿瘤活性和耐受的毒性。了解更多

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AG-1517

Catalog No. A13001
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EGFR 抑制剂

AG 1517是表皮生长因子受体酪氨酸激酶EGFR的有效和选择性ATP竞争性抑制剂。了解更多

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ARRY-380 (Irbinitinib)

Catalog No. A16413
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HER2 抑制剂

ARRY-380是人表皮生长因子受体酪氨酸激酶ErbB-2（也称为HER2）的口服生物利用抑制剂，具有潜在的抗肿瘤活性。了解更多

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Sitravatinib (MGCD516)

Catalog No. A16259
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RTK 抑制剂

Sitravatinib是一种新型小分子抑制剂，靶向多种参与驱动肉瘤细胞生长的RTK。了解更多

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Alofanib (RPT835)

Catalog No. A15946
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FGFR2 抑制剂

Alofanib (RPT835)是FGFR2的强效选择性变构抑制剂，具有潜在的抗癌活性。了解更多

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KX2-391 2HCl

Catalog No. A11471
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Src 抑制剂

Tirbanibulin dihydrochloride是首个靶向Src肽底物位点的临床Src抑制剂(拟肽类),在癌细胞系中GI50为9-60 nM。了解更多

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PF-04217903 methanesulfonate

Catalog No. A15208
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c-Met 抑制剂

PF-04217903 methanesulfonate是一种选择性ATP竞争性c-Met抑制剂，IC50为4.8 nM，易致癌突变（对Y1230C突变体无活性）。了解更多

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LDK378 (Ceritinib) dihydrochloride

Catalog No. A15142
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ALK 抑制剂

LDK378 (Ceritinib) dihydrochloride是有效的抗ALK抑制剂，IC50为0.2 nM，对IGF-1R和InsR的选择性分别为40倍和35倍。了解更多

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LDC1267

Catalog No. A13003
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TAM Receptor 抑制剂

LDC1267是一种高选择性TAM（Tyro3，Axl和Mer）激酶抑制剂，对于Tyro3，Axl和Mer的IC50分别小于5 nM/8 nM/29 nM。了解更多

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Poziotinib

Catalog No. A13044
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EGFR 抑制剂

Poziotinib是一种口服生物利用的，基于喹唑啉的泛表皮生长因子受体（EGFR或HER）抑制剂，具有潜在的抗肿瘤活性。了解更多

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- Ikei S Kobayashi, .et al. EGFR-D770>GY and Other Rare EGFR Exon 20 Insertion Mutations with a G770 Equivalence Are Sensitive to Dacomitinib or Afatinib and Responsive to EGFR Exon 20 Insertion Mutant-Active Inhibitors in Preclinical Models and Clinical Scenarios, Cells, 2021, 10(12): 3561 PMID: 34944068
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AZD 2932

Catalog No. A14156
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mutil-targeted protein tyrosine kinase 抑制剂

AZD2932是一种有效且靶向多用途的蛋白酪氨酸激酶抑制剂，对VEGFR-2，PDGFRβ，Flt-3和c-Kit的IC50分别为8 nM，4 nM，7 nM和9 nM。了解更多

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AZD-9291 (Osimertinib)

Catalog No. A13681
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EGFR 抑制剂

AZD-9291 (Osimertinib)是第三代EGFR抑制剂，在临床前研究中显示出希望，并为已对现有EGFR抑制剂产生耐药性的晚期肺癌患者提供了希望。了解更多

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- Liu YN, .et al. Acquired resistance to EGFR tyrosine kinase inhibitors is mediated by the reactivation of STC2/JUN/AXL signaling in lung cancer, Int J Cancer, 2019, Jun 4 PMID: 31162839
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LDK-378

Catalog No. A13238
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ALK 抑制剂

LDK-378是ALK(间变性淋巴瘤激酶)的高度选择性、生物利用度和AT竞争性小分子抑制剂，ALK是一种受体酪氨酸激酶，被认为是肺癌的重要药物靶点。了解更多

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Pacritinib (SB1518)

Catalog No. A12694
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JAK2/FLT3 抑制剂

Pacritinib (SB1518)是Janus激酶2（JAK2）和JAK2突变体JAK2V617F的口服生物利用抑制剂，无细胞试验中IC50分别为23和22 nM，具有潜在的抗肿瘤活性。Pacritinib与JAK2竞争ATP结合，这可能导致抑制JAK2活化，抑制JAK-STAT信号传导途径以及半胱天冬酶依赖性凋亡。了解更多

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- Daniel Doheny, .et al. Combined inhibition of JAK2-STAT3 and SMO-GLI1/tGLI1 pathways suppresses breast cancer stem cells, tumor growth, and metastasis, Oncogene, 2020, Oct;39(42):6589-6605 PMID: 32929154
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SU 5416 (Semaxinib)

Catalog No. A12437
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VEGFR 抑制剂

SU 5416 (Semaxinib)是血管内皮生长因子受体（VEGFR）的抑制剂，它还抑制其他酪氨酸激酶KIT，MET，FLT3和RET。了解更多

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- Guangyan Zhang, .et al. Sulforaphane Does Not Protect Right Ventricular Systolic and Diastolic Functions in Nrf2 Knockout Pulmonary Artery Hypertension Mice, Cardiovasc Drugs Ther, 2022, Feb 14 PMID: 35157168
- Michel R. Corboz, .et al. Treprostinil palmitil inhibits the hemodynamic and histopathological changes in the pulmonary vasculature and heart in an animal model of pulmonary arterial hypertension, Eur J Pharmacol, 2022, 916: 174484 PMID: 34508752
- Avner Adini, .et al. PR1P Stabilizes VEGF and Upregulates its Signaling to Reduce Elastase Induced Murine Emphysema, Am J Respir Cell Mol Biol, 2020, Jul 14 PMID: 32663413
- Yin Kang, .et al. Sulforaphane Prevents Right Ventricular Injury and Reduces Pulmonary Vascular Remodeling in Pulmonary Arterial Hypertension, Am J Physiol Heart Circ Physiol, 2020, Apr 1;318(4):H853-H866 PMID: 32108526
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Lapatinib (free base)

Catalog No. A11752
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Lapatinib (free base)是一种双重酪氨酸激酶抑制剂，是一种有效的EGFR和ErbB2抑制剂，在无细胞试验中IC50分别为10.2和9.8 nM。可阻断HER2生长受体途径。了解更多

Product Citations (7)

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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
- 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
- Momeny M, .et al. The ERBB receptor inhibitor dacomitinib suppresses proliferation and invasion of pancreatic ductal adenocarcinoma cells, Cell Oncol (Dordr), 2019, Apr 25 PMID: 31025257
- Tzeng SF, .et al. O-Glycosylation-mediated signaling circuit drives metastatic castration-resistant prostate cancer, FASEB J, 2018, Jun 15:fj201800687 PMID: 29906246
- 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
- Yuki Kawasaki, .et al. Feedback control of ErbB2 via ERK-mediated phosphorylation of a conserved threonine in the juxtamembrane domain, Sci Rep, 2016, 6: 31502 PMID: 27531070
- Tetsuya Saita, .et al. Preparation of Antibodies and Development of an Enzyme-Linked Immunosorbent Assay for the Tyrosine Kinase Inhibitors Lapatinib and Nilotinib., Biol Pharm Bull. , 2015, 38(10):1652-7 PMID: 26424026
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Genistin (Genistoside)

Catalog No. A10426
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Genistin (Genistoside)是一种异黄酮，存在于许多饮食植物中，如大豆和葛根。显示出刺激体内雌激素依赖性乳腺癌细胞生长。了解更多

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- Azuma T, .et al. Distribution of six anticancer drugs and a variety of other pharmaceuticals, and their sorption onto sediments, in an urban Japanese river, Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. Detection of pharmaceuticals and phytochemicals together with their metabolites in hospital effluents in Japan, and their contribution to sewage treatment plant influents, Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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E7080 (Lenvatinib)

Catalog No. A10340
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VEGFR 抑制剂

E7080 (Lenvatinib)是一种多激酶抑制剂，可同时抑制VEGFR2和VEGFR3激酶。了解更多

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- Mai Nakahara, .et al. Effect of Lenvatinib treatment on the cell cycle and microRNA profile in hepatocellular carcinoma cells, Biomed Rep, 2022, Aug 3;17(4):78 PMID: 36158319
- Paula Sagmeister, .et al. Comparative Response of HCC Cells to TKIs: Modified in vitro Testing and Descriptive Expression Analysis, J Hepatocell Carcinoma, 2022, Jul 9;9:595-607 PMID: 35845819
- 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
- Keisuke Enomoto, .et al. Synergistic Effects of Lenvatinib (E7080) and MEK Inhibitors against Anaplastic Thyroid Cancer in Preclinical Models, Cancers (Basel), 2021, Feb 18;13(4):862 PMID: 33670725
- Jindal A, .et al. Milciclib and sorafenib synergistically downregulate c-Myc to suppress tumor growth in an orthotopic murine model of human hepatocellular carcinoma, J Transl Sci, 2020, 7: 1-10
- Koide H, .et al. Substrate-dependent effects of molecular-targeted anticancer agents on activity of organic anion transporting polypeptide 1B1, Xenobiotica, 2018, Oct;48(10):1059-1071 PMID: 29034773
- 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
- Tomoko Ogawa-Morita, .et al. Validation of a Liquid Chromatography-Tandem Mass Spectrometric Assay for Quantitative Analysis of Lenvatinib in Human Plasma, Int J Anal Chem, 2017, 2017: 2341876 PMID: 28680445
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CYC116 (CYC-116)

Catalog No. A10248
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Aurora Kinase 抑制剂

CYC116 (CYC-116)是一种有效的Aurora A/B抑制剂，Ki为8.0 nM/9.2 nM，对VEGFR2(Ki为44 nM)作用稍弱。了解更多

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TG101209

Catalog No. A11180
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JAK2 抑制剂

TG101209是一种新型的JAK2抑制剂，无细胞试验中IC50为6 nM，对Flt3和RET作用效果稍弱，IC50分别为25 nM和17 nM，作用于JAK2比作用于JAK3选择性高30倍左右，对JAK2V617F和MPLW515L/K突变型敏感。在多发性骨髓瘤中具有显着的体外活性，并且对CD45+骨髓瘤细胞显示出优先的细胞毒性。了解更多

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KX2-391

Catalog No. A11177
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Src 抑制剂

KX2-391是新型的非ATP竞争底物口袋定向SRC抑制剂。了解更多

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BGJ398 (NVP-BGJ398)

Catalog No. A11159
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FGFR 抑制剂

BGJ398 (NVP-BGJ398)是一种有效的选择性抑制剂，具有成纤维细胞生长因子受体（FGFR）酪氨酸激酶1、2、3和4的潜在抗血管生成和抗肿瘤活性（对于FGFR1，FGFR2，FGFR3，IC50值为0.9、1.4、1.0和60 nM，和FGFR4）。了解更多

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- Takehito Yamamoto, .et al. Chemosensitivity of Patient-Derived Cancer Stem Cells Identifies Colorectal Cancer Patients with Potential Benefit from FGFR Inhibitor Therapy, Cancers (Basel), 2020, Jul 22;12(8):E2010 PMID: 32708005
- Daniel Limonta, .et al. Fibroblast growth factor 2 enhances Zika virus infection in human fetal brain, J Infect Dis, 2019, 2019 PMID: 30799482
- Li Li, .et al. Evidence for activated Lck protein tyrosine kinase as the driver of proliferation in acute myeloid leukemia cell, CTV-1, Leukemia Res, 2019, 78:12-20 PMID: 30660961
- Anil Kumar, .et al. Human Sertoli cells support high levels of Zika virus replication and persistence, Sci Rep, 2018, 8: 5477 PMID: 29615760
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AG-1024 (Tyrphostin)

Catalog No. A11400
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IGF-1R 抑制剂

AG-1024 (Tyrphostin)是胰岛素样生长因子-1 (IGF-1) 和胰岛素受体酪氨酸激酶活性的特异性抑制剂。与胰岛素受体相比，IGF-1的IC50值更低。还抑制胰岛素刺激的细胞增殖。了解更多

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- Maeda A, .et al. Safranal, a novel protein tyrosine phosphatase 1B inhibitor, activates insulin signaling in C2C12 myotubes and improves glucose tolerance in diabetic KK-Ay mice., Mol Nutr Food Res. , 2014, 58(6):1177-89 PMID: 24668740
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Imatinib Mesylate

Catalog No. A10468
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Bcr-Abl 抑制剂

Imatinib mesylate是一种选择性酪氨酸激酶抑制剂，通过抑制KIT信号转导途径，在治疗胃肠间质瘤中诱导了持续的客观反应。了解更多

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- Inge Govaerts, .et al. PSEN1-selective gamma-secretase inhibition in combination with kinase or XPO-1 inhibitors effectively targets T cell acute lymphoblastic leukemia, J Hematol Oncol, 2021, 14: 97 PMID: 34167562
- Genevra Kuziel, .et al. Stromal CCL2 Signaling Promotes Mammary Tumor Fibrosis through Recruitment of Myeloid-Lineage Cells, Cancers (Basel), 2020, Jul 28;12(8):E2083 PMID: 32731354
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AZD4547

Catalog No. A11075
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FGFR 抑制剂

AZD4547是一种有效，选择性和口服活性的pan-FGFR抑制剂，对于FGFR1、2、3和4的IC50分别为0.2、2.5、1.8和165 nM。了解更多

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- Ryuma Tokunaga, .et al. Fibroblast growth factor receptor 2 expression, but not its genetic amplification, is associated with tumor growth and worse survival in esophagogastric junction adenocarcinoma, Oncotarget, 2016, Apr 12; 7(15): 19748-19761 PMID: 26933914
- Mitsuko Kawano, .et al. FGF18 signaling in the hair cycle resting phase determines radioresistance of hair follicles by arresting hair cycling, Adv Radiat Oncol, 2016, Jul-Sep; 1(3): 170-181 PMID: 28740887
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Dasatinib (BMS-354825)

Catalog No. A10290
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Abl-Src 抑制剂

Dasatinib (BMS-354825)是一种口服多BCR/ABL和Src家族酪氨酸激酶抑制剂。Dasatinib (BMS-354825)的主要靶标是BCR/ABL，Src，c-Kit，ephrin受体和其他几种酪氨酸激酶，但不是erbB激酶，例如EGFR或Her2。了解更多

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- Chihiro Motozono, .et al. The SARS-CoV-2 Omicron BA.1 spike G446S mutation potentiates antiviral T-cell recognition, Nat Commun, 2022, Sep 21;13(1):5440 PMID: 36130929
- 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
- David E J Klawon, .et al. Altered selection on a single self-ligand promotes susceptibility to organ-specific T cell infiltration, J Exp Med, 2021, Jun 7;218(6) PMID: 33914024
- Reiko Watanabe, .et al. Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration, J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Li Li, .et al. Evidence for activated Lck protein tyrosine kinase as the driver of proliferation in acute myeloid leukemia cell, CTV-1, Leukemia Res, 2019, 78:12-20 PMID: 30660961
- Sano T, .et al. Gliding Basal Cell Migration of the Urothelium during Wound Healing, Am J Pathol, 2018, Nov;188(11):2564-2573 PMID: 30121259
- Ines Peschel, .et al. FLT3 and FLT3-ITD phosphorylate and inactivate the cyclin-dependent kinase inhibitor p27Kip1 in acute myeloid leukemia, Haematologica, 2017, Aug; 102(8): 1378-1389 PMID: 28522571
- 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
- John D. Leonard, .et al. Identification of natural regulatory T cell epitopes reveals convergence on a dominant autoantigen, Immunity, 2017, Jul 18; 47(1): 107-117.e8 PMID: 28709804
- 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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Linifanib (ABT-869)

Catalog No. A10025
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VEGFR/PDGFR 抑制剂

Linifanib (ABT-869)是一种结构新颖的有效RTK，VEGF和PDGF抑制剂，对人内皮细胞，PDGFR-β，KDR和CSF-1R的IC50分别为0.2、2、4和7 nM。了解更多

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- Li Li, .et al. Evidence for activated Lck protein tyrosine kinase as the driver of proliferation in acute myeloid leukemia cell, CTV-1, Leukemia Res, 2019, 78:12-20 PMID: 30660961
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BMS-777607

Catalog No. A10153
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c-Met 抑制剂

BMS-777607是一种MET酪氨酸激酶抑制剂，与c-Met蛋白或HGFR结合，可防止HGF结合并破坏MET信号通路。了解更多

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WZ3146

Catalog No. A10990
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EGFR 抑制剂

WZ3146是EGFR受体激酶突变体的抑制剂，该突变体在活性位点网守残基（T790M）中带有突变，并且对野生型EGFR激酶的效力要低得多。了解更多

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WZ8040

Catalog No. A10992
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EGFR 抑制剂

WZ8040是一种新型的EGFR抑制剂，可抑制含有EGFR-T790M的细胞系的生长并抑制EGFR磷酸化。了解更多

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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

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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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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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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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WZ4002

Catalog No. A10991
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EGFR 抑制剂

WZ4002是一种新型的，突变选择性EGFR抑制剂，作用于EGFR(L858R)/(T790M)，在BaF3细胞系中IC50为2 nM/8 nM；对ERBB2磷酸化(T798I)没有抑制作用。了解更多

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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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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

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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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Axitinib

Catalog No. A10103
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VEGFR 抑制剂

Axitinib是一种小分子酪氨酸激酶抑制剂，可抑制多种靶标，包括VEGFR-1，VEGFR-2，VEGFR-3，血小板衍生生长因子受体（PDGFR）和cKIT（CD117）。了解更多

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- Youcef M. Rustum, .et al. Non-Coding Micro RNAs and Hypoxia-Inducible Factors Are Selenium Targets for Development of a Mechanism-Based Combination Strategy in Clear-Cell Renal Cell Carcinoma-Bench-to-Bedside Therapy, Int J Mol Sci, 2018, Nov; 19(11): 3378 PMID: 30380599
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AC220 (Quizartinib)

Catalog No. A10027
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FLT3 抑制剂

AC220 (Quizartinib)是一种有效的选择性FLT3抑制剂，对于MC4-11和A375，IC50分别为0.56±0.3 nM和> 10 mM。了解更多

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- 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
- Cong Li, .et al. AMG 925 is a dual FLT3/CDK4 inhibitor with the potential to overcome FLT3 inhibitor resistance in acute myeloid leukemia., Mol Cancer Ther., 2015, Feb;14(2):375-83. PMID: 25487917
- Yaping Zhang, .et al. FLT3 and CDK4/6 inhibitors: Signaling mechanisms and tumor burden in subcutaneous and orthotopic mouse models of acute myeloid leukemia, J Pharmacokinet Pharmacodyn., 2014, 41(6): 675-691. PMID: 25326874

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