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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-mTOR-Torin2
Torin2

Chemical Structure : Torin2

CAS No.: 1223001-51-1

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Torin2 (Torin 2;Torin-2)

货号: PC-43313Not For Human Use, Lab Use Only.

Torin2 is a potent, selective, orally available inhibitor of mTOR, inhibits mTORC1-dependent T389 phosphorylation on S6K with IC50 of 0.25 nM, exhibits 800-fold selectivity over PI3K, and >100-fold over 440 other protein kinases.

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25 mg ￥1780 In stock
50 mg ￥2880 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Torin 2 is a potent, selective, orally available inhibitor of mTOR, inhibits mTORC1-dependent T389 phosphorylation on S6K with IC50 of 0.25 nM, exhibits 800-fold selectivity over PI3K, and >100-fold over 440 other protein kinases.
Torin 2 also exhibits potent biochemical and cellular activity against PIKK family kinases including ATM (EC50=28 nM), ATR (EC50=35 nM), and DNA-PK (EC50=118 nM).
Torin 2 inhibits mTOR kinase and mTORC1 signaling activities, results in a prolonged block in negative feedback and consequent T308 phosphorylation on Akt in treated cancer cells.
Torin 2 demonstrates significant growth inhibition against KRAS-driven lung tumors combined with MEK inhibitor AZD6244, does not yield significant efficacy as a single agent.
Torin 2 overcomes the resistance of ALK(F1174L)/MYCN tumors to crizotinib in vivo.

物理化学性质&存储条件

分子量 432.3973
分子式 C24H15F3N4O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

Benzo[h]-1,6-naphthyridin-2(1H)-one, 9-(6-amino-3-pyridinyl)-1-[3-(trifluoromethyl)phenyl]-

参考文献

1. Liu Q, et al. J Med Chem. 2011 Mar 10;54(5):1473-80.

2. Liu Q, et al. Cancer Res. 2013 Apr 15;73(8):2574-86.

3. Berry T, et al. Cancer Cell. 2012 Jul 10;22(1):117-30.

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