Dovitinib, Lactate Salt (CHIR-258, TKI-258, D08907, CAS 692737-80-7), >99%

LC Laboratories' Product Number D-3699 - Dovitinib, Lactate Salt (CHIR-258, TKI-258, D08907, CAS 692737-80-7), >99% - for research use only. Dovitinib is a small-molecule multitargeted receptor tyrosine kinase inhibitor. Dovitinib inhibited proliferation of ZNF198-FGFR1 and BCR-FGFR1 transformed Ba/F3 cells with IC50 values of 150 nM and 90 nM, respectively. The phosphorylation of each fusion gene, ERK, and STAT5 was inhibited as well at the same time. Dovitinib also inhibited proliferation of the FGFR1OP2-FGFR1-positive KG1 and KG1A cell lines and induced apoptosis. Furthermore, dovitinib significantly inhibited the growth of primary cells from 8p11 myeloproliferative syndrome (EMS) patients dose-dependently. Dovitinib potently inhibits receptor tyrosine kinases including FLT3, c-KIT, CSF-1R/c-fms, FGFR1, FGFR3, VEGFR1/Flt1,VEGFR2/Flk1, VEGFR3/Flt4, PDGFRβ, and PDGFRα with IC50 values of 1, 2, 36, 8, 9, 10, 13, 8, 27, and 210 nM, respectively. Dovitinib selectively blocked the growth of wild-type (WT) or activated mutant FGFR3-transformed B9 cells and human myeloma cell lines. Dovitinib was an effective treatment in a xenograft mouse model of FGFR3 multiple myeloma (MM). Dovitinib treatment showed antitumor and antiangiogenic activities in xenograft models of human colon cancer. Dovitinib inhibited vascular endothelial growth factor receptor 1/2, fibroblast growth factor receptor 1/3, platelet-derived growth factor receptor β (PDGFR-β), the phosphorylation of PDGFR-β and extracellular signal-regulated kinase (ERK) in tumors. Dovitinib was examined on two human leukemic cell lines with differing FLT3 mutational status in vitro and in vivo, including MV4;11 cells expressing FLT3 internal tandem duplications (ITD) and RS4;11 cells with wild-type (WT) FLT3. Antiproliferative activity of dovitinib against MV4;11 was about 24-fold greater than against RS4;11. Dovitinib significantly inhibited KMS-11-luc tumor growth and improved animal survival at doses that inhibited FGFR3 signaling in KMS-11-luc tumors in vivo. This dovitinib product is the lactate salt, whose CAS number is given above. We also offer the free base -- please see Cat. No. D-3608, Dovitinib, Free Base. The CAS number of dovitinib free base is 405169-16-6. The CAS number for the monohydrate of dovitinib lactate salt is 915769-50-5. Another CAS number previously assigned to dovitinib lactate, namely 1000873-96-0, has been deleted by CAS and is no longer in use.

• Supplier: LC Laboratories
• Product #: D-3699
• Sku #: D-3699_500mg