Torin1

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

Torin1 是一种高效、选择性的 mTORC1 和 mTORC2 抑制剂，IC50 分别为 2 和 10 nM。

Torin1 is a highly potent, selective inhibitor of mTORC1 and mTORC2 with IC50 of 2 and 10 nM in cell-free assays, exhibits 1,000-fold selectivity PI3K (EC50=1,800 nM); exhibits 100-fold binding selectivity relative to 450 other protein kinases; causes cell cycle arrest through a rapamycin-resistant mechanism that is also independent of mTORC2, disrupts mTORC1-dependent phenotypes more completely than rapamycin; prevents the anti-inflammatory potency of GC both in human monocytes and myeloid dendritic cells.(In Vitro):Torin1 (250 nM) completely inhibits proliferation and causes a G1/S cell cycle arrest, and decreases cell size to a greater degree than 50 nM rapamycin in wild-type MEFs. Torin1 has more than 800-fold selectivity between mTOR and PI3Kis, and is very selective relative to other PIKK family kinases with the exception of DNA-PK.(In Vivo):Torin1 (20 mg/kg, i.p.) is efficacious in a U87MG xenograft model, and demonstrates good pharmacodynamic inhibition of downstream effectors of mTOR in tumor and peripheral tissues.

Torin1 (250 nM) completely inhibits proliferation and causes a G1/S cell cycle arrest, and decreases cell size to a greater degree than 50 nM rapamycin in wild-type MEFs. Torin1 has more than 800-fold selectivity between mTOR and PI3Kis, and is very selective relative to other PIKK family kinases with the exception of DNA-PK.

Torin1 (20 mg/kg, i.p.) is efficacious in a U87MG xenograft model, and demonstrates good pharmacodynamic inhibition of downstream effectors of mTOR in tumor and peripheral tissues.

Torin 1 | Torin-1

PI3K/Akt/mTOR signaling

mTOR

DNA-PK|mTOR|mTORC1|mTORC2|p110γ

Cancer

——

1222998-36-8

607.6243

C35H28F3N5O2

>98% (HPLC)

DMSO: 6.6 mg/mL (Need ultrasonic or warming)

O=C1N(C2=CC=C(N3CCN(C(CC)=O)CC3)C(C(F)(F)F)=C2)C4=C(C=NC5=CC=C(C6=CC7=CC=CC=C7N=C6)C=C54)C=C1

Benzo[h]-1,6-naphthyridin-2(1H)-one, 1-[4-[4-(1-oxopropyl)-1-piperazinyl]-3-(trifluoromethyl)phenyl]-9-(3-quinolinyl)-

(-20℃)

With Ice Pack

≥ 2 years