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G-749 is a novel and effective FLT3 inhibitor, with IC50 values of 0.4 nM,0.6nM and 1nM for FLT3(WT),FLT3(D835Y), and Mer, respectively, with low effect on other tyrosine kinases.
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.
Brand: BCM
pKa: 8.32±0.40(Predicted)
Solubility: Soluble in DMSO. Insoluble in Water and Ethanol.
Attribute [CAS No.] 1457983-28-6 [Formula] C25H25BrN6O2 [Molecular] 521.41 [Chem Name] Pyrido[4,3-d]pyrimidin-5(6H)-one, 8-bromo-2-[(1-methyl-4-piperidinyl)amino]-4-[(4-phenoxyphenyl)amino]- [Synonym] G-749 [MDL No.] MFCD28167815 [Form] Solid
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