Inhibitor of fms related receptor tyrosine kinase 3;Inhibitor of MER proto-oncogene; tyrosine kinase
Product Description
Information
G-749 G-749 is a novel and potent FLT3 inhibitor with IC50 of 0.4 nM, 0.6 nM and 1 nM for FLT3 (WT), FLT3 (D835Y), and Mer, respectively, showing lower potency against other tyrosine kinases.
Targets
FLT3 (Cell-free assay); FLT3 (D835Y) (Cell-free assay); Mer (Cell-free assay); Aurora B (Cell-free assay); RET (Cell-free assay) 15501,0.4 nM; 0.6 nM; 1 nM; 6 nM; 9 nM
In vitro
In FLT3-WT-bearing RS4-11 cells and FLT3-ITD-harboring MV4-11 and Molm-14 cells, G-749 potently inhibits autophosphorylation of FLT3 with IC50 of ≤8 nM. In leukemia cells, G-749 shows antiproliferative activity by inducing apoptosis. In BaF3 cell lines that stably express FLT3-ITD/N676D, FLT3-ITD/F691L, FLT3-D835Y, or FLT3-D835Y/N676D, G-749 shows strong inhibitory activity with IC50 of <10 nM, and thus overcomes drug resistance. In blasts of AML patients, G-749 also exhibits potent antileukemia activity.
In vivo
In MV4-11 xenograft mice, G-749 (30 mg/kg p.o.) effectively inhibits the FLT3 pathway and significant inhibits tumor growth. In an orthogonal model of bone marrow engraftment using Molm-14 cells, G-749 (20 mg/kg p.o.) also inhibits tumor growth and increases survival.
Cell Research(from reference)
Cell lines：MV4-11, RS4-11, K562, HEL, and Molm-14 cells
1.Lee HK, Kim HW, Lee IY, Lee J, Lee J, Jung DS, Lee SY, Park SH, Hwang H, Choi JS et al.. (2014) G-749, a novel FLT3 kinase inhibitor, can overcome drug resistance for the treatment of acute myeloid leukemia.. Blood, 123 (14):(2209-19). [PMID:24532805]
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K2218427