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PI3K / Akt / mTOR

PI3K / Akt / mTOR

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CC-223

Catalog No. A13078
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mTOR 抑制剂

CC-223是一种有效的mTOR激酶抑制剂（IC50 = 16 nM），其敏感性是相关脂质激酶PI3K-alpha（IC50 = 4 uM）的> 150倍。了解更多

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CZ415

Catalog No. A16476
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mTOR inhibitor

CZ415 is a potent and highly selective mTOR inhibitor with a pIC50 of 8.07. CZ415 inhibits mTORC1 and mTORC2 protein complex. 了解更多

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mTOR inhibitor-2

Catalog No. A13035
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mTOR inhibitor

mTOR inhibitor-2 is a highlt potent, selective and oral mTOR inhibitor with an IC50 of 7 nM. mTOR inhibitor-2 inhibits cellular phosphorylation of mTORC1 (pS6 and p4E-BP1) and mTORC2 (pAKT (S473)) substrates. 了解更多

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HDACs/mTOR Inhibitor 1

Catalog No. A13462
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HDACs/mTOR Inhibitor 1

HDACs/mTOR Inhibitor 1 is a dual Histone Deacetylases (HDACs) and mammalian target of Rapamycin (mTOR) target inhibitor for treating hematologic malignancies. 了解更多

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42-(2-Tetrazolyl)rapamycin

Catalog No. A21394
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mTOR inhibitor

42-(2-Tetrazolyl)rapamycin is a prodrug compound of a rapamycin analog extracted from patent US 20080171763 A1, Example 1. Rapamycin is a specific mTOR inhibitor. 了解更多

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mTOR inhibitor (mTOR-IN-1)

Catalog No. A15175
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mTOR 抑制剂

mTOR inhibitor (mTOR-IN-1)是mTOR的有效且选择性的ATP竞争性抑制剂，Ki为1.5 nM。了解更多

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MHY1485

Catalog No. A15508
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mTOR 抑制剂

MHY1485是mTOR激活剂；通过抑制自噬体和溶酶体之间的融合导致LC3II蛋白的积累和自噬体扩大，从而抑制自噬过程。了解更多

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QL-IX-55

Catalog No. A11537
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mTORC1/2 抑制剂

QL-IX-55是mTORC1/2的选择性ATP竞争性抑制剂，其IC50分别为50/50/10-50nM，用于人mTORC1/酵母mTORC1/酵母mTORC2。了解更多

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PP242 (Torkinib)

Catalog No. A10746
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mTOR 抑制剂

PP242 (Torkinib)在mTORC1和mTORC2中都是有效的选择性mTOR抑制剂。了解更多

Product Citations (2)

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- 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
- 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
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WYE-354

Catalog No. A10989
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mTOR 抑制剂

WYE-354是一种有效的mTOR细胞渗透抑制剂（IC50 = 4.3 nM），可阻断通过mTOR复合体1（mTORC1）和mTORC2的信号传导。它是PI3Kα（IC50 = 1026 nM）和其他激酶的弱得多的抑制剂。了解更多

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- H Weber ,etc. Rapamycin and WYE-354 suppress human gallbladder cancer xenografts in mice. Oncotarget, 2015, 6(31), 31877.
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FK-506 (Tacrolimus)

Catalog No. A10389
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mTOR 抑制剂

FK-506 (Tacrolimus)是一种免疫抑制药物，通过结合到抑免蛋白FKBP12 (FK506 结合蛋白)产生新的复合物，从而降低T细胞中肽酰脯氨酰异构酶活性。了解更多

Product Citations (2)

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- Ogawa Y, .et al. Inhibition of astrocytic adenosine receptor A2A attenuates microglial activation in a mouse model of Sandhoff disease, Neurobiol Dis, 2018, Oct;118:142-154 PMID: 30026035
- Yuko Okamoto, .et al. In vivo drug delivery efficiency of albumin-encapsulated liposomes as hydrophobic drug carriers, J Drug Deliv Sci Technol, 2018, 47: 62-66
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AZD2014 (Vistusertib)

Catalog No. A11303
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mTORC1/2 抑制剂

Vistusertib (AZD2014)是一种新型mTOR抑制剂，无细胞试验中IC50为2.8 nM；对多种PI3K亚型(α/β/γ/δ)具有较高选择性。浓度为1 μM时，对大多数激酶无或有微弱结合力。了解更多

Product Citations (1)

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- Shuhang Dai, .et al. Calcium/calmodulin-dependent protein kinase kinase 2 mediates pleiotropic effects of epidermal growth factor in cancer cells, Biochim Biophys Acta Mol Cell Res, 2022, Jul;1869(7):119252 PMID: 35271909
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Torin 1

Catalog No. A11587
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mTOR 抑制剂

Torin1是mTOR的有效抑制剂，IC50为2-10 nM。了解更多

Product Citations (4)

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- Andromachi Lambrianidou, .et al. mTORC2 deploys the mRNA binding protein IGF2BP1 to regulate c-MYC expression and promote cell survival, Cell Signal, 2021, Apr;80:109912 PMID: 33388443
- Kowalsky AH, .et al. The GATOR2?CmTORC2 axis mediates Sestrin2-induced AKT Ser/Thr kinase activation, J Biol Chem, 2020, Feb 14;295(7):1769-1780 PMID: 31915252
- Ashyad Rayhan, .et al. Using genetic buffering relationships identified in fission yeast to reveal susceptibilities in cells lacking hamartin or tuberin function, Biol Open, 2018, Jan 15; 7(1): bio031302 PMID: 29343513
- Jin H. Song, .et al. Mechanisms Behind Resistance to PI3K Inhibitor Treatment Induced by the PIM Kinase, Mol Cancer Ther, 2018, Dec;17(12):2710-2721 PMID: 30190422
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AZD8055

Catalog No. A10114
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mTOR 抑制剂

AZD8055是一种有效的，选择性的ATP竞争性mTOR激酶抑制剂，IC50为0.8 nM。了解更多

Product Citations (3)

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- L. M. C. Koene, .et al. Effects of antiepileptic drugs in a new TSC/mTOR-dependent epilepsy mouse model, ACTN, 2019, June PMID: 31353861
- Helga Weber, .et al. Rapamycin and WYE-354 suppress human gallbladder cancer xenografts in mice, Oncotarget, 2015, Oct 13; 6(31): 31877–31888 PMID: 26397134
- Kentaro Hirose, .et al. Mechanistic target of rapamycin complex 1 signaling regulates cell proliferation, cell survival, and differentiation in regenerating zebrafish fins, BMC Dev Biol, 2014, 14: 42. PMID: 25480380
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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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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

Product Citations (9)

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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
- 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
- Gabriela Torres-Flores, .et al. Preparation and Characterization of Liposomal Everolimus by Thin-Film Hydration Technique, Adv Polym Technol, 2020, ID 5462949
- Takaaki Fujimura, .et al. Enhanced antitumor effect of alectinib in combination with cyclin-dependent kinase 4/6 inhibitor against RET-fusion-positive non-small cell lung cancer cells, Cancer Biol Ther, 2020, Sep 1;21(9):863-870 PMID: 32835580
- BD Henriksbo, .et al. Statins Activate the NLRP3 Inflammasome and Impair Insulin Signaling via p38 and mTOR, Am J Physiol Endocrinol Metab, 2020, Jul 1;319(1):E110-E116 PMID: 32421368
- 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
- Nachi Namatame, .et al. Antitumor profile of the PI3K inhibitor ZSTK474 in human sarcoma cell lines, Oncotarget, 2018, Oct 12; 9(80): 35141-35161 PMID: 30416685
- 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
- Rieko Ohki, .et al. PHLDA3 is a novel tumor suppressor of pancreatic neuroendocrine tumors, Proc Natl Acad Sci U S A, 2014, 111(23): E2404-E2413 PMID: 24912192
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AZD6482

Catalog No. A10112
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PI3K 抑制剂

AZD6482是一种PI3Kβ抑制剂，(IC50 = 0.021M)。了解更多

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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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AS-605240

Catalog No. A10088
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PI3K 抑制剂

AS-605240是PI3激酶γ抑制剂，以ATP竞争的方式抑制人重组PI3Kγ，α，β和δ，IC50值为8、60、270和300 nM。了解更多

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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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GDC-0980 (Apitolisib, RG7422)

Catalog No. A11023
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mTOR/PI3K 抑制剂

GDC-0980 (Apitolisib,RG7422)是一种有效的，I型PI3激酶和mTOR激酶抑制剂（TORC1/2），对于p110α，β，δ和γ的体外IC50为5、27、7和14 nM。了解更多

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- Kasun Wanigasooriya, .et al. Patient Derived Organoids Confirm That PI3K/AKT Signalling Is an Escape Pathway for Radioresistance and a Target for Therapy in Rectal Cancer, Front Oncol, 2022, Jul 4;12:920444 PMID: 35860583
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GSK2126458 (Omipalisib)

Catalog No. A11035
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mTOR/PI3K 抑制剂,

GSK2126458 (Omipalisib)是一种高选择性的，有效的p110α/β/γ/δ和 mTORC1/2抑制剂，无细胞试验中Ki分别为0.019 nM/0.13 nM/0.024 nM/0.06 nM和0.18 nM/0.3 nM。了解更多

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XL765

Catalog No. A10997
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PI3K 抑制剂

XL765是PI3K/mTOR双激酶抑制剂，与单独抑制PI3K激酶或mTOR激酶的药物相比，它的效力更高。了解更多

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PKI-587 ( Gedatolisib )

Catalog No. A11079
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PI3K/mTOR 抑制剂

PKI-587 (Gedatolisib)是一种高效的PI3K/mTOR激酶抑制剂，可抑制PI3K-α，β，γ，δ亚型和mTOR，IC50分别为0.4、6.0、5.4、6.0和1.6 nM。了解更多

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PKI-402

Catalog No. A11089
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PI3K 抑制剂

PKI-402是一种有效的，pan-PI3K/mTOR双重抑制剂，靶向作用于PI3Kα/β/γ/δ和mTOR，IC50分别为2 nM/7 nM/16 nM/14 nM和3 nM，也有效作用于PI3Kα突变型E545K和H1047R。了解更多

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AS-252424

Catalog No. A11099
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PI3K 抑制剂

AS-252424是有效的PI3K抑制剂，对γ亚型具有选择性。它抑制人重组PI3Kγ，α，β和δ，IC50值分别为30、940、20,000和20,000 nM。了解更多

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3-Methyladenine

Catalog No. A11151
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Autophagy/PI3K 抑制剂

3-Methyladenine是III类磷脂酰肌醇3-激酶（PI 3-激酶）的抑制剂。了解更多

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PIK-293

Catalog No. A10727
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PI3K 抑制剂

PIK-293是PI3-K抑制剂。PIK-293抑制p110α，p110β，p110δ。PIK-293是PIK-294的母体化合物。了解更多

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PIK-294

Catalog No. A10728
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PI3K 抑制剂

PIK-294是PI3激酶抑制剂，其效力比母体化合物PIK-293高20至60倍。它是已报道的最有效的p110δ选择性抑制剂之一。了解更多

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Quercetin (Sophoretin)

Catalog No. A10766
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MAO-B 抑制剂

Quercetin (Sophoretin)抑制许多酶系统，包括酪氨酸蛋白激酶，磷脂酶A2，磷酸二酯酶，线粒体ATPase，PI 3-激酶和蛋白激酶C。了解更多

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Quercetin dihydrate (Sophoretin)

Catalog No. A10765
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MAO-B 抑制剂

Quercetin dihydrate (Sophoretin)抑制许多酶系统，包括酪氨酸蛋白激酶，磷脂酶A2，磷酸二酯酶，线粒体ATPase，PI 3-激酶和蛋白激酶C。了解更多

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NVP-BGT226

Catalog No. A11162
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PI3K 抑制剂

NVP-BGT226，新型磷酸肌醇3-激酶/mTOR双重抑制剂，作用于PI3Kα/β/γ，IC50为4 nM/63 nM/38 nM，在体外和体内对人的头颈癌细胞均显示出强大的生长抑制活性。了解更多

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CH5132799

Catalog No. A11169
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PI3K 抑制剂

CH5132799是一种新型的I类PI3K抑制剂，尤其对PI3Kα (IC (50) = 0.014μM) 表现出很强的抑制活性。了解更多

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CAY10505

Catalog No. A11196
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PI3K 抑制剂

CAY10505是PI3K的有效抑制剂，与α，β和δ亚型（分别为IC50 = 0.94、20和20μM）相比，对γ亚型（IC50 = 30 nM）的选择性抑制作用更好。了解更多

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AS-604850

Catalog No. A11197
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PI3K 抑制剂

AS-604850抑制MCP-1介导的单核细胞趋化性，IC50值为21 ?M，并在ED50值为42.4 mg/kg的白细胞趋化性小鼠模型中降低了RANTES诱导的腹膜中性粒细胞募集。了解更多

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D-106669

Catalog No. A11198
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PI3K 抑制剂

D-106669是一种高效且选择性的PI3K抑制剂（PI3KαIC50 <10 nM，对酪氨酸或丝氨酸/苏氨酸激酶的对数选择性> 3，ERK1和2除外）。了解更多

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A66

Catalog No. A11202
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PI3K 抑制剂

A66的S对映异构体是PI 3-激酶（PIK3CA）的p110alpha亚型的有效抑制剂。无细胞试验中IC50为32 nM，作用于p110α比作用于其他I类PI3K亚型选择性高100多倍。了解更多

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PIK-90

Catalog No. A10730
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PI3K 抑制剂

PIK-90是一种合成的磷酸肌醇3激酶（PI3K）抑制剂，对于p110α，β，γ和δ亚型的IC50值（nM）为11、350、18和58，mTOR活性低。了解更多

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PX-866 (Sonolisib)

Catalog No. A11261
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PI3K 抑制剂

PX-866 (Sonolisib)是磷酸肌醇3激酶(PI3K)的α，γ和δ亚型的小分子渥曼青霉素类似物抑制剂，具有潜在的抗肿瘤活性。了解更多

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NVP-BAG956

Catalog No. A11511
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PI3K/PDK-1 抑制剂

NVP-BAG956是一种强效、可逆和ATP竞争性PI3-K/PDK1双激酶抑制剂，对VEGFR 1(IC50 = 2.56 μM)的效力大大降低，对其他15种激酶(IC50 > 10 uM)的活性很小或没有活性。了解更多

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TG 100713

Catalog No. A11956
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PI3K 抑制剂

TG 100713是PI3K的抑制剂，可抑制内皮细胞的增殖。了解更多

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IPI-145 (Duvelisib, INK1197)

Catalog No. A12422
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PI3K-δ/PI3K-γ 抑制剂

IPI-145 (Duvelisib,INK1197)是磷酸肌醇-3激酶(PI3K)δ和γ亚型的生物可利用、高选择性和有效的小分子抑制剂，具有潜在的免疫调节和抗肿瘤活性。了解更多

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SF1126

Catalog No. A12704
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Pan PI3K 抑制剂

SF1126是一种水溶性小分子前药，包含泛PI3K/mTOR抑制剂LY294002/SF1101与含RGD的四肽SF1174共轭，具有潜在的抗肿瘤和抗血管生成活性。了解更多

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GDC-0032 (Taselisib)

Catalog No. A12831
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PI3K 抑制剂

GDC-0032 (Taselisib)是有效的下一代PI3抑制剂，靶向PI3α。了解更多

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ETP-46464

Catalog No. A13328
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ATR 抑制剂

ETP-46464是一种有效的选择性ATR抑制剂，IC50为25 nM。了解更多

Product Citations (1)

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- Fu-Xing Gong, .et al. De-dimerization of PTB is catalyzed by PDI and is involved in the regulation of p53 translation, Nucleic Acids Res, 2021, Sep 20;49(16):9342-9352 PMID: 34403458
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PF-04979064

Catalog No. A12935
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PI3K/mTOR Dual 抑制剂

PF-04979064是一种高效的生物利用PI3K/mTOR双重抑制剂。Ki 分别为 0.13 nM 和 1.42 nM。了解更多

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CNX-1351

Catalog No. A13879
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PI3Kα 抑制剂

CNX-1351是一种有效的选择性PI3Kα抑制剂，IC50为6.8 nM。了解更多

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GNE 477

Catalog No. A14114
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PI3K/mTOR 抑制剂

GNE-477是一种有效的PI3K/mTOR双重抑制剂，PI3Kα的IC50为4 nM，Kiapp为mTOR的IC50为21 nM。了解更多

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PI3k-delta inhibitor 1

Catalog No. A14109
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PI3Kδ 抑制剂

PI3k-delta inhibitor 1是有效的选择性PI3Kδ抑制剂，IC50为3.8 nM。了解更多

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GNE-493

Catalog No. A14432
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Dual Pan PI3k/mTOR 抑制剂

GNE-493是有效，选择性的pan-PI3-激酶和双重pan-PI3-激酶/mTOR抑制剂，具有潜在的抗癌活性。了解更多

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