Dovitinib
CAS No. | 405169-16-6 | Cat. No. | BCP01981 |
Name | Dovitinib | ||
Synonyms | CHIR-258;TKI258;TKI-258;TKI 258;CHIR258;CHIR 258; | ||
Formula | C21H21FN6O | M. Wt | 392.44 |
Description | Dovitinib potently inhibits the FGF-stimulated growth of WT and F384L-FGFR3-expressing B9 cells with IC50 of 25 nM. In addition, Dovitinib inhibits proliferation of B9 cells expressing each of the various activated mutants of FGFR3. Interestingly, there are minimal observed differences in the sensitivity of the different FGFR3 mutations to Dovitinib, with the IC50 ranging from 70 to 90 nM for each of the various mutations. IL-6-dependent B9 cells containing vector only (B9-MINV cells are resistant to the inhibitory activity of Dovitinib at concentrations up to 1 μM. Dovitinib inhibits cell proliferation of KMS11 (FGFR3-Y373C), OPM2 (FGFR3-K650E), and KMS18 (FGFR3-G384D) cells with IC50 of 90 nM (KMS11 and OPM2) and 550 nM, respectively. Dovitinib inhibits FGF-mediated ERK1/2 phosphorylation and induces cytotoxicity in FGFR3-expressing primary MM cells. BMSCs does confer a modest degree of resistance with 44.6% growth inhibition for cells treated with 500 nM Dovitinib and cultured on st | ||
Pathways | Angiogenesis/Protein Tyrosine Kinase | ||
Targets | PDGFR VEGFR c Kit FLT3 FGFR |
Structure
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