Torin2

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Torin2 是一种有效、选择性、口服的 mTOR 抑制剂，抑制 S6K 上 mTORC1 依赖性 T389 磷酸化，IC50 为 0.25 nM。

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; 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); 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; demonstrates significant growth inhibition against KRAS-driven lung tumors combined with MEK inhibitor AZD6244, does not yield significant efficacy as a single agent; overcomes the resistance of ALK(F1174L)/MYCN tumors to crizotinib in vivo.

——

——

Torin 2 | Torin-2

PI3K/Akt/mTOR signaling

mTOR

ATM|ATR|DNA-PK|mTOR

Cancer

——

1223001-51-1

432.3973

C24H15F3N4O

>98% (HPLC)

10 mM in DMSO

O=C1N(C2=CC=CC(C(F)(F)F)=C2)C3=C(C=NC4=CC=C(C5=CC=C(N)N=C5)C=C43)C=C1

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

(-20℃)

With Ice Pack

≥ 2 years