OSI-930

Research use only, not for human use.

A potent, orally active, dual inhibitor of c-Kit and VEGFR-2 (KDR) with IC50 of 15 nM and 9 nM, respectively.

A potent, orally active, dual inhibitor of c-Kit and VEGFR-2 (KDR) with IC50 of 15 nM and 9 nM, respectively; also inhibits Lck, c-Raf, Flt1, and CSF-1R (IC50<100 nM); exhibits antitumor activity in mutant Kit-expressing HMC-1 xenograft model.Solid Tumors Phase 1 Discontinued(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. 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.

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

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.

OSI 930 | OSI930

Angiogenesis

c-Kit

C-Raf|CSF-1R|FLT1|Lck|VEGFR2?(KDR)

Cancer

Solid Tumors

728033-96-3

443.4416

C22H16F3N3O2S

>98% (HPLC)

10 mM in DMSO

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

2-Thiophenecarboxamide, 3-[(4-quinolinylmethyl)amino]-N-[4-(trifluoromethoxy)phenyl]-

(-20℃)

With Ice Pack

≥ 2 years