Bioactivity | 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[1]. | ||||||||||||
Invitro | 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[1].OSI-930 inactivates purified, recombinant cytochrome P450 3A4 with a Ki of 24 μM in a time- and concentration-dependent manner[2] | ||||||||||||
Name | OSI-930 | ||||||||||||
CAS | 728033-96-3 | ||||||||||||
Formula | C22H16F3N3O2S | ||||||||||||
Molar Mass | 443.44 | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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