tcsc0237 Torin 1

Torin 1 is a potent inhibitor of mTOR with an IC₅₀ of 3 nM. Torin 1 inhibits both mTORC1/2 complexes with IC₅₀ values between 2 and 10 nM.

IC50 & Target: IC50: 2-10 nM (mTORC1), 2-10 nM (mTORC2), 3 nM (mTOR), 0.6 μM (ATM), 1 μM (DNA-PK), 1.8 μM (PI3K-α), 3 μM (hVPS34)^[2]

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^[1]. 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^[2].

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^[2].