PF-05139962 is a potent mTOR inhibitor with excellent mTOR bioactive compound inhibition, cellular potency, kinase selectivity and in vitro ADME properties. PF-05139962 has pS473 and pS6 cellular IC50 = 48 and 6 nM respectively. PF-05139962 has great selectivity against other receptors and kinases. No genotoxicity was observed on this compound and no more than 25% inhibiton was observed for major CYP enzymes (3A4, 1A2, 2C9, 2D6) at 3 uM. This compound has LE = 0.35 and LipE up to 6.8 which is in a very desirable range for a kinase inhibitor. References: Liu KK, Bailey S, Dinh DM, Lam H, Li C, Wells PA, Yin MJ, Zou A. Conformationally-restricted cyclic sulfones as potent and selective mTOR kinase inhibitors. Bioorg Med Chem Lett. 2012 Aug 1;22(15):5114-7. doi: 10.1016/j.bmcl.2012.05.104. Epub 2012 Jun 6. PubMed PMID: 22765900.

纯度：≥98%

CAS：1393712-18-9