Price and Availability of CHIR-258(Dovitinib,TKI258):
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10mg
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50mg
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100mg
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Biological Activity:
A multitargeted growth factor receptor kinase inhibitor to VEGFR, FGFR3, PDGFR and c-KIT. CHIR-258 was highly potent against FLT3 (1 nmol/L) with nanomolar activity against c-KIT (2 nmol/L), VEGFR1/2/3 (10 nmol/L); FGFR1/3 (8 nmol/L); PDGFRß (27 nmol/L) and CSF-1R (36 nmol/L). To confirm selectivity against class III, IV, and V RTKs, CHIR-258 was tested against other kinases in the phosphatidylinositol 3-kinase/Akt and mitogen-activated protein kinase pathways and was found to have negligible activity (IC50 > 10 Amol/L). CHIR-258 potently inhibited proliferation of MV4;11 cells in a dose-dependent manner with EC50 = 13 nmol/L. Although similar concentrationdependent effects on proliferation were observed with RS4; 11 cells, they were f24-fold less sensitive to CHIR-258 (EC50 =315 nmol/L). The antiproliferative effect of CHIR-258 was also tested on the FLT3 ITD mutant cells, MOLM13 and MOLM14 with EC50 concentrations similar to those seen with MV4;11 (EC50,6 nmol/L; data not shown). These data suggest that CHIR-258 is active on both FLT3 ITD and WT leukemic cells, with the constitutively active receptor being more sensitive to inhibition.
References:
1.Trudel S, et al. CHIR-258, a novel, multitargeted tyrosine kinase inhibitor for the potential treatment of t(4;14) multiple myeloma. Blood. 2005, 105(7), 2941-2948. 2. Huynh H, et al. Dovitinib demonstrates antitumor and antimetastatic activities in xenograft models of hepatocellular carcinoma. J Hepatol. 2012, 56(3), 595-601.
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C13463 CHIR-258(Dovitinib,TKI258) (405169-16-6)