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A multi-kinase inhibitor, inhibits FLT3, CSF1R, c-Kit, FGFR1, FGFR3, VEGFR1, -2, and -3, PDFGRalpha, and PDGFRbeta (IC50s = 1, 36, 2, 8, 9, 10, 13, 8, 27, and 210 nM, respectively), inhibits the proliferation of human multiple myeloma cell lines expressing mutant, but not wild-type, FGFR3 (IC50s = 90-550 and >2,500 nM, respectively), decreases FGF-induced ERK1/2 phosphorylation and induces apoptosis in patient-derived multiple myeloma cells at 500 nM, inhibits bFGF-induced angiogenesis in a Matrigel(TM) plug assay in mice at 3-300 mg/kg for 8 days, reduces tumor growth in KM12L4A, DU145, and MV4-11 mouse xenograft models (ED50s = 17, 23, and 3 mg/kg per day, respectively). Formulation: A solid. InChI: InChI=1S/C21H21FN6O.2C3H6O3/c1-27-7-9-28(10-8-27)12-5-6-14-16(11-12)25-20(24-14)18-19(23)17-13(22)3-2-4-15(17)26-21(18)29,2*1-2(4)3(5)6/h2-6,11H,7-10H2,1H3,(H,24,25)(H3,23,26,29),2*2,4H,1H3,(H,5,6). InChIKey: XXLPVQZYQCGXOV-UHFFFAOYSA-N. SMILES: O=C(C(C)O)O.CN1CCN(C2=CC=C3C(NC(C4=C(C5=C(NC4=O)C=CC=C5F)N)=N3)=C2)CC1.O=C(C(C)O)O
Keywords:
CHIR258, TKI-258, 2-hydroxy-propanoic acid, compd. with 4-amino-5-fluoro-3-[6-(4-methyl-1-piperazinyl)-1H-benzimidazol-2-yl]-2(1H)-quinolinone (2:1)
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