Dovitinib (405169-16-6) is a potent kinase inhibitor. Inhibits FLT3 (IC50 = 1 nM), c-KIT (IC50 = 2 nM), FGFR (IC50 = 8 nM), VEGFR1/2/3 (IC50 = 10 nM), PDGFRβ (IC50 = 27 nM), and CSF-1R (IC50 = 36 nM).1 Active in cell culture and in whole animals. Dovitinib selectively blocks the growth B9 cells transformed by wild type, or activated mutant FGFR3. Induces apoptosis, or sensitizes cells to induction of apoptosis by other means in a variety of cancer cell lines.
1) Lee et al. (2005), In vivo target modulation and biological activity of CHIR-258, a multitargeted growth factor receptor kinase inhibitor, in colon cancer models; Clin. Cancer Res., 11 3633
2) Xin et al. (2006), CHIR-258 is efficacious in a newly developed fibroblast growth factor receptor 3-expressing orthotopic multiple myeloma model in mice; Clin. Cancer Res., 12 4908