Dovitinib

Bezeichnung:Dovitinib

CAS-Nr405169-16-6

Englisch Name:Dovitinib

CBNumberCB11512534

SummenformelC21H21FN6O

Molgewicht392.43

MOL-Datei405169-16-6.mol

Dovitinib physikalisch-chemischer Eigenschaften

Dichte	1.386
storage temp.	-20°
Löslichkeit	Soluble in DMSO (up to 30 mg/ml).
Aggregatzustand	solid
pka	9.44±0.70(Predicted)
Farbe	Yellow-green
Stabilität	Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
CAS Datenbank	405169-16-6

Gefahreninformationscode (GHS)

Dovitinib Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
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.
Verwenden
Compound used in treating melanoma
Verwenden
Dovitinib (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.
Verwenden
Dovitinib (TKI258, CHIR-258) is a multitargeted tyrosine kinase inhibitor of FLT3 and c-KIT with IC50 of 1 nM and 2 nM, respectively.
Verwenden
Dovitinib 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.
Definition
ChEBI: 4-amino-5-fluoro-3-[5-(4-methyl-1-piperazinyl)-1,3-dihydrobenzimidazol-2-ylidene]-2-quinolinone is a N-arylpiperazine.
in vivo
the combination of tigatuzumab and tki258 inhibited huh-7 xenograft tumor growth [3]. tki258 reduced wm tumor progression [4].
target
FLT3
Einzelnachweise
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

Dovitinib Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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