Catalog No.: PC-42452Not For Human Use, Lab Use Only.
Dovitinib lactate (CHIR-258, TKI-258) is a multitargeted RTK inhibitor of class III, IV, and V RTKs with IC50 of 1/2/36/8/9 nM for FLT3/c-KIT/c-Fms/FGFR1/FGFR3, respectively.
Dovitinib lactate (CHIR-258, TKI-258) is a multitargeted RTK inhibitor of class III, IV, and V RTKs with IC50 of 1/2/36/8/9 nM for FLT3/c-KIT/c-Fms/FGFR1/FGFR3, respectively.
Dovitinib also inhibits VEGFR1/2/3 (IC50=10/13/8 nM) and PDGFRβ/α (IC50=27/210 nM).
Dovitinib selectively inhibits the growth of B9 cells and human myeloma cell lines expressing wild-type (WT) or activated mutant FGFR3.
Dovitinib inhibits downstream ERK 1/2 phosphorylation and induces cytostatic and cytotoxic effects.
Dovitinib demonstrates activity in a xenograft mouse model of FGFR3 MM; orally active.
Physicochemical Properties
M.Wt
482.5073832
Formula
C24H27FN6O4
Appearance
Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility
DMSO: ≥ 30 mg/mL
Chemical Name/SMILES
Propanoic acid, 2-hydroxy-, compd. with 4-amino-5-fluoro-3-[6-(4-methyl-1-piperazinyl)-1H-benzimidazol-2-yl]-2(1H)-quinolinone (1:1)
References
1. Trudel S, et al. Blood. 2005 Apr 1;105(7):2941-8.
2. Lopes de Menezes DE, et al. Clin Cancer Res. 2005 Jul 15;11(14):5281-91.
3. Xin X, et al. Clin Cancer Res. 2006 Aug 15;12(16):4908-15.
