G-749

Base Information

• Chemical Name: G-749
• CAS No.: 1457983-28-6
• Molecular Formula: C25H25BrN6O2
• Molecular Weight: 521.409
• Mol file: 1457983-28-6.mol

Synonyms:G-749;8-Bromo-2-[(1-methyl-4-piperidinyl)amino]-4-[(4-phenoxyphenyl)amino]pyrido[4,3-d]pyrimidin-5(6H)-one;8-Bromo-2-[(1-methyl-4-piperidinyl)amino]-4-[(4-phenoxyphenyl)amino]pyrido[4,3-d]pyrimidin-5(6H)-one G749;G-749, >=98%;G-49;G-749 (Free base)

Chemical Property of G-749

Chemical Property:

• PKA: 8.32±0.40(Predicted)
• PSA: 95.17000
• Density: 1.487±0.06 g/cm3(Predicted)
• LogP: 5.20650
• Solubility.: ≥26.05 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O

Purity/Quality:

99% ^*data from raw suppliers

G-749 ^*data from reagent suppliers

Safty Information:

• Pictogram(s):  
• Hazard Codes: 

MSDS Files:

SDS file from LookChem

Useful:

• Description: 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. G-749 is an inhibitor of Fms-like tyrosine receptor kinase 3 (FLT3) with IC50 values ranging from 2.1 to 38.1 nM for wild-type and mutant (constitutively active) FLT3s in Ba/F3 cells expressing recombinant receptors. It also inhibits growth of human leukemia cell lines that express FLT3-ITD mutant kinase (IC50s = 3.5 and 7.5 nM for MV4-11 and Molm-14 cells, respectively) but has no effect on cells that lack FLT3 expression or that express wild-type FLT3. G-749 reduces tumor growth and increases survival in a dose-dependent manner in MV4-11 and Molm-14 murine leukemia xenograft models. It reduces growth of bone marrow blasts derived from acute myeloid leukemia patients, showing more potent inhibition of blasts expressing the FLT3-ITD mutant receptor.
• Uses: G-749 is a potent FLT3 inhibitor. It shows lower potency against other tyrosine kinases.