产品
编 号:F439687
分子式:C22H16F3N3O2S
分子量:443.44
产品类型
结构图
CAS No: 728033-96-3
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产品详情
生物活性:
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.
体内研究:
OSI-930 (oral gavage; once a day; 38 days; 200 mg/kg) exhibits potent antitumor activity in a broad range of preclinical xenograft models.Animal Model:Female nu/nu CD-1 mice bearing HMC-1, NCI-SNU-5, COLO-205 and U251 xenograft models
Dosage:200 mg/kg
Administration:Oral gavage; once a day; 38 days
Result:Showed a significant level of inhibition of Kit, KDR and CSF-1R.
体外研究:
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.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