Dovitinib-d is intended for use as an internal standard for the quantification of dovitinib by GC- or LC-MS. Dovitinib is a multi-kinase inhibitor. It inhibits the receptor tyrosine kinases FLT3, CSF1R, and c-Kit (ICs = 1, 36, and 2 nM, respectively), as well as FGFR1, FGFR3, VEGFR1-3, PDFGRα, and PDGFRβ (ICs = 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 (ICs = 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. It reduces tumor growth in KM12L4A colon, DU145 prostate, and MV4-11 acute myelogenous leukemia mouse xenograft models with ED values of 17, 23, and 3 mg/kg per day, respectively.
Dovitinib-d8 is the deuterium labeled Dovitinib. Dovitinib (CHIR-258) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/FGFR3, VEGFR1/VEGFR2/VEGFR3 and PDGFRα/PDGFRβ, respectively.
分子式
C21H13D8FN6O
分子量
400.4781632
CAS号
1246819-84-0
中文名称
多韦替尼 d8
运输条件
Room temperature in continental US; may vary elsewhere.