OSI-930 (C09-0997-847)

InformationOSI-930 is a potent inhibitor ofKit (c-Kit),KDRandCSF-1RwithIC50of 80 nM, 9 nM and 15 nM, respectively; also potent to Flt-1, c-Raf and Lck and low activity against PDGFRα/β, Flt-3 and Abl. Phase 1.In vitroOSI-930 inhibits the cell proliferation in the HMC-1 cell line with IC50 of 14 nM without significant effect on growth of the COLO-205 cell line that does not express a constitutively active mutant receptor tyrosine kinase. Moreover, OSI-930 also induces apoptosis in HMC-1 cell line with EC50 of 34 nM. A recent study shows that OSI-930 inactivates purified, recombinant cytochrome P450 (P450) 3A4 with a Ki of 24 μM in a time- and concentration-dependent mode.In vivoOSI-930, administrated at the maximally efficacious dose of 200 mg/kg by oral gavage, exhibits potent antitumor activity in a broad range of preclinical xenograft models including HMC-1, NCI-SNU-5, COLO-205 and U251 xenograft models.Cell Datacell lines：Concentrations：0--1 μMIncubation Time：48 hoursPowder Purity:≥99%. Specification: 10mM in DMSO Molecular Formula: C22H16F3N3O2S Molecular Weight: 443.44