A multi-kinase inhibitor; inhibits FLT3

Dovitinib – 5 mg

Brand:
Cayman
CAS:
405169-16-6
Storage:
-20
UN-No:
Non-Hazardous - /

Dovitinib is a multi-kinase inhibitor.{47801} It inhibits the receptor tyrosine kinases FLT3, CSF1R, and c-Kit (IC50s = 1, 36, and 2 nM, respectively), as well as FGFR1, FGFR3, VEGFR1-3, PDFGRα, and PDGFRβ (IC50s = 8, 9, 10, 13, 8, 27, and 210 nM, respectively). Dovitinib inhibits proliferation of human multiple myeloma cell lines expressing mutant, but not wild-type, FGFR3 (IC50s = 90-550 and >2,500 nM, respectively). It decreases FGF-induced ERK1/2 phosphorylation and induces apoptosis in patient-derived multiple myeloma cells when used at a concentration of 500 nM. Dovitinib (3-300 mg/kg for eight days) inhibits bFGF-induced angiogenesis in a Matrigel™ plug assay in mice.{24514} It reduces tumor growth in KM12L4A colon, DU145 prostate, and MV4-11 acute myelogenous leukemia mouse xenograft models with ED50 values of 17, 23, and 3 mg/kg per day, respectively.  

 

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Description

A multi-kinase inhibitor; inhibits FLT3, CSF1R, c-Kit, FGFR1, FGFR3, VEGFR1, -2, and -3, PDFGRα, and PDGFRβ (IC50s = 1, 36, 2, 8, 9, 10, 13, 8, 27, and 210 nM, respectively); inhibits proliferation of human multiple myeloma cell lines expressing mutant, but not wild-type, FGFR3 (IC50s = 90-550 and >2,500 nM, respectively); decreases FGF-induced ERK1/2 phosphorylation and induces apoptosis in patient-derived multiple myeloma cells at 500 nM; inhibits bFGF-induced angiogenesis in a Matrigel™ plug assay in mice at 3-300 mg/kg for 8 days; reduces tumor growth in KM12L4A, DU145, and MV4-11 mouse xenograft models (ED50s = 17, 23, and 3 mg/kg per day, respectively)

Formal name: 4-amino-5-fluoro-3-[6-(4-methyl-1-piperazinyl)-1H-benzimidazol-2-yl]-2(1H)-quinolinone

Synonyms:  CHIR-258|TKI-258

Molecular weight: 392.4

CAS: 405169-16-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|FGFR Family||Product Type|Biochemicals|Kinase Inhibitors|PDGFR Family||Product Type|Biochemicals|Kinase Inhibitors|VEGFR Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Angiogenesis||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling

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