Torin 1 | CAS:1222998-36-8

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Name:Torin 1; 
Cat. No. :CS-0237
CAS No. :1222998-36-8
Formula:C35H28F3N5O2
M. Wt. : 607.62
Solubility:DMSO: 6.6 mg/mL (Need ultrasonic or warming)

Torin 1 is a potent inhibitor of mTOR, with IC50 values of 2 nM and 10 nM against mTORC1 and mTORC2, respectively.IC50 & Target: IC50: 2 nM (mTORC1), 10 nM (mTORC2)[1]IC50: 4.32 nM (mTOR), 6.34 nM (DNA-PK), 171 nM (P110γ), 176 nM (PI3K-C2 α), 533 nM (hVPS34), 549 nM (PI3K-C2β), 6.68 μM (PI4K β)[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].

Thoreen CC, et al, An ATP-competitive mammalian target of rapamycin inhibitor reveals rapamycin-resistant functions of mTORC1. J Biol Chem, 2009, 284(12), 8023-8032. Brandt M, et al. mTORC1 Inactivation Promotes Colitis-Induced Colorectal Cancer but Protects from APC Loss-Dependent Tumorigenesis. Cell Metab. 2018 Jan 9;27(1):118-135.e8. Bi C, et al. Inhibition of 4EBP phosphorylation mediates the cytotoxic effect of mechanistic target of rapamycin kinase inhibitors in aggressive B-cell lymphomas. Haematologica. 2017 Apr;102(4):755-764. Liu Q, et al. Discovery of 1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one as a highly potent, selective mammalian target of rapamycin (mTOR) inhibitor for the treatment of cancer. J Med Che