G-749 (C09-0901-942)

InformationG-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.TargetsFLT3 (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 nMIn vitroIn 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 vivoIn 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 Concentrations：~1 μM Incubation Time：72 hours. Specification: 0.98 Molecular Formula: C25H25BrN6O2 Molecular Weight: 521.41 PubChem CID: 78357765 Isomeric SMILES: CN1CCC(CC1)NC2=NC3=C(C(=O)NC=C3Br)C(=N2)NC4=CC=C(C=C4)OC5=CC=CC=C5 Related Documents: https://ald-pub-files.oss-cn-shanghai.aliyuncs.com/aladdinsci/pdp/sds/1/G413776-SCI_400819bd7d99e3be98d9356618856493.pdf