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Description: Dovitinib Lactate (formerly TKI-258 lactate; CHIR-258 lactate), a benzimidazole-quinolinone analog, is a potent, orally bioavailable and multitargeted RTK inhibitor with potential antineoplastic activity. It mostly inhibits class III (FLT3/c-Kit) with an IC50 of 1 nM/2 nM, also potently inhibits class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, and is less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGFR1 and HER2. Dovitinib strongly binds to FGFR3 and inhibits its phosphorylation, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell death.
References: Blood. 2005; 105(7):2941-8; J Hepatol. 2012; 56(3):595-601; Clin Cancer Res. 2005; 11(10):3633-41.
Related CAS #: 692737-80-7 or 915769-50-5 (lactate) 405169-16-6 (free base) 852433-84-2 (dilactate)
Chemical Name: 4-Amino-5-fluoro-3-[6-(4-methyl-1-piperazinyl)-1H-benzimidazol-2-yl]-2(1H)-quinolinone 2-hydroxypropanoate
InChi Key: ZRHDKBOBHHFLBW-UHFFFAOYSA-N
InChi Code: InChI=1S/C21H21FN6O.C3H6O3/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; 1-2(4)3(5)6/h2-6, 11H, 7-10H2, 1H3, (H, 24, 25)(H3, 23, 26, 29); 2, 4H, 1H3, (H, 5, 6)
SMILES Code: O=C1NC2=C(C(F)=CC=C2)C(N)=C1C3=NC4=CC=C(N5CCN(C)CC5)C=C4N3.CC(O)C(O)=O
CHIR 258; TKI258; TKI-258; CHIR-258; CHIR258; TKI 258; Dovitinib lactate
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