Osi-296

OSI-296是cMET和RON激酶的强效和双重抑制剂(cMET和sfRon的IC50值分别为42nM和200nM)。OSI-206显示出体内功效,并且在口服给药后在肿瘤异种移植物模型中具有良好的耐受性。OSI-296还可以减少骨中肿瘤的生长。

1. Steinig AG, Li AH, Wang J, Chen X, Dong H, Ferraro C, Jin M, Kadalbajoo M, Kleinberg A, Stolz KM, Tavares-Greco PA, Wang T, Albertella MR, Peng Y, Crew L, Kahler J, Kan J, Schulz R, Cooke A, Bittner M, Turton RW, Franklin M, Gokhale P, Landfair D, Mantis C, Workman J, Wild R, Pachter J, Epstein D, Mulvihill MJ. Novel 6-aminofuro[3,2-c]pyridines as potent, orally efficacious inhibitors of cMET and RON kinases. Bioorg Med Chem Lett. 2013 Aug 1;23(15):4381-7. doi: 10.1016/j.bmcl.2013.05.074. PubMed PMID: 23773865.