Flumatinib mesylate

Research use only, not for human use.

Flumatinib mesylate is a selective inhibitor of c-Abl PDGFRβ and c-Kit effectively overcomes drug resistance of certain KIT mutants.

Flumatinib mesylate is a selective inhibitor of c-Abl PDGFRβ and c-Kit effectively overcomes drug resistance of certain KIT mutants.

Flumatinib mesylate (HH-GV-678) (0-1000 μM; 4, 7 and 10 days) blocks cellular Bcr-Abl autophosphorylation and Stat5 and Erk1/2 phosphorylation in K562 leukemia cells.Flumatinib mesylate (HH-GV-678) (0-10 μM; 72 hours) remarkably decreases the number of cells in chronic myelogenous leukemia cell lines. Cell Proliferation Assay Cell Line:Chronic myelogenous leukemia cell line Concentration:0-10 μM Incubation Time:72 hours Result:The proliferation inhibitory activity was 32-to 58-fold more potent than that of imatinib and 2-to 5-fold more potent than that of nilotinib.Western Blot Analysis Cell Line:K562 cells Concentration:0, 1, 3, 10, 30, 100, 300 and 1000 μM Incubation Time:4, 7 and 10 days Result:Suppressed cellular Bcr-Abl autophosphorylation and Stat5 and Erk1/2 phosphorylation.

Flumatinib mesylate (HH-GV-678) (18-75 mg/kg; p.o.; Twice daily, for 14 days.) inhibits tumor growth in nude mice. Animal Model:Nude mice (subcutaneously injecting K562 cells)Dosage:18.75, 37.5, 75 mg/kg Administration:Oral administration; Twice daily, for 14 days. Result:Inhibited the growth of K562 xenografts in a dose-dependent manner and induced regression in all tumors at a daily dose of 75 mg/kg for nine days.

HHGV678 mesylate

Angiogenesis

PDGFR

PDGFRβ |c-Kit |c-Abl

Cancer

chronic phase chronic myelogenous leukemia

895519-91-2

658.69

C30H33F3N8O4S

>98% (HPLC)

DMSO:50 mg/mL (75.91 mM) ; H2O:50 mg/mL (75.91 mM)

CS(=O)(=O)O.Cc1ncc(NC(=O)c2ccc(CN3CCN(C)CC3)c(C(F)(F)F)c2)cc1Nc1nccc(-c2cccnc2)n1

——

(-20℃)

With Ice Pack

≥ 2 years