OSI-930 | HY-10204

OSI-930 is an orally selective inhibitor of Kit, KDR and CSF-1R (c-Fms) with IC50s of 80 nM, 9 nM and 15 nM, respectively. OSI-930 also moderately inhibits Flt-1, c-Raf, Lck and low activity against PDGFRα/β, Flt-3 and Abl. OSI-930 has antitumor activity.

IC50 & Target:

In Vitro:

OSI-930 inhibits cell proliferation in the HMC-1 cell line with IC50 of 14 nM but has no significant effect on the growth of COLO-205 cell line that does not express constitutively active mutant receptor tyrosine kinase[1]. OSI-930 induces apoptosis in HMC-1 cell line with an EC50 value of 34 nM. OSI-930 inactivates purified, recombinant cytochrome P450 3A4 with a Ki of 24 μM in a time- and concentration-dependent manner.

In Vivo:

OSI-930 (oral gavage; once a day; 38 days; 200 mg/kg) exhibits potent antitumor activity in a broad range of preclinical xenograft models.

Molecular weight:

443.44

Formula:

C₂₂H₁₆F₃N₃O₂S

SMILES:

O=C(C1=C(NCC2=CC=NC3=CC=CC=C23)C=CS1)NC4=CC=C(OC(F)(F)F)C=C4

Storage: