Dovitinib

Dovitinib Basic information
Product Name:Dovitinib
Synonyms:4-Amino-5-fluoro-3-[5-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2(1H)-one;dovitinib;Unii-I35H55G906;CHIR258 7.7G;TKI-258;4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2(1H)-one;CHIR-258(Dovitinib,TKI258);CHIR-258(Dovitinib)
CAS:405169-16-6
MF:C21H21FN6O
MW:392.43
EINECS:1308068-626-2
Product Categories:Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals;API intermediates
Mol File:405169-16-6.mol
Dovitinib Structure
Dovitinib Chemical Properties
density 1.386
storage temp. -20°
solubility Soluble in DMSO (up to 30 mg/ml).
form solid
pka9.44±0.70(Predicted)
color Yellow-green
Stability:Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
CAS DataBase Reference405169-16-6
Safety Information
MSDS Information
Dovitinib Usage And Synthesis
DescriptionDovitinib (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.
UsesCompound used in treating melanoma
UsesDovitinib is a receptor tyrosine kinase inhibitor that targets vascular endothelial growth factor-2, basic fibroblast growth factor-1, and platelet-derived growth factor β receptors (IC50s = 65, 11, and 5 nM, respectively). At 0.04 μM, dovitinib can inhibit endothelial cell proliferation and motility. These antiangiogenic effects have been proposed to be the mechanism by which dovitinib inhibits hepatocellular carcinoma growth and metastasis. Dovitinib has been evaluated in clinical trials for the treatment of advanced solid tumors.
UsesDovitinib (TKI258, CHIR258) is a novel multi-target inhibitor for Flt3, c-Kit, FGFR1/3, VEGFR1/2/3, PDGFRα/β with IC50 of 1 nM, 2 nM, 8 nM/9 nM and 10 nM/13 nM/8 nM, 210 nM/27 nM respectively.
UsesDovitinib (TKI258, CHIR-258) is a multitargeted tyrosine kinase inhibitor of FLT3 and c-KIT with IC50 of 1 nM and 2 nM, respectively.
DefinitionChEBI: 4-amino-5-fluoro-3-[5-(4-methyl-1-piperazinyl)-1,3-dihydrobenzimidazol-2-ylidene]-2-quinolinone is a N-arylpiperazine.
in vivothe combination of tigatuzumab and tki258 inhibited huh-7 xenograft tumor growth [3]. tki258 reduced wm tumor progression [4].
targetFLT3
References1) 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
Dovitinib Preparation Products And Raw materials
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