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AZD3759 Home您现在的位置:HOME >> PRODUCTS >> Inhibitors

AZD3759

所属类别:Inhibitors 点击次数:675次 发布时间:2017-04-13

AZD3759
详情
 AZD3759 
AZD3759 Basic Info.
Synonyms:4-((3-chloro-2-fluorophenyl)amino)-7-methoxyquinazolin-6-yl (2R)-2,4-dimethylpiperazine-1-carboxylate; (R)-4-((3-chloro-2-fluorophenyl)amino)-7-methoxyquinazolin-6-yl 2,4-dimethylpiperazine-1-carboxylate; 
CAS:1626387-80-1 
MF:C22H23ClFN5O3 
MW:459.90100 
Appearance:white to off-white solid
Assay:above 99%  Pharmaceutical grade
Usage:Lung cancer drug research
 
 
AZD3759 Application:
 
AZD3759 is a potent, oral active, central nervous system-penetrant, EGFR inhibitor. At Km ATP concentrations, the IC50 values were 0.3, 0.2, and 0.2 nM for EGFR TK wild-type, L858R mutant, and Exon 19Del enzymes, respectively.
IC50 value: 7.2 nM (L858R pEGFR)
Target: EGFR
in vitro: The inhibition of AZD3759 against EGFR tyrosine kinase (EGFR TK) wild type and mutant enzymes was tested at their corresponding Km and 2mM ATP concentrations. AZD3759 demonstrated inhibitory effects on both the pEGFR pathway and cell proliferation of EGFR mutation-derived cells PC-9 and H3255. AZD3759 was selected as the candidate for comprehensive biological profiling.
in vivo: AZD3759 exhibits the best pharmacokinetic profile with moderate blood clearance at 17 mL/min/kg and volume of distribution of 5.2 L/kg. The intrinsic clearance (Clint) of AZD3759 is 11.4 μL/min 106 cells in human hepatocytes, and the predicted clearance of the agent in humans is 7.7 mL/min/kg by extrapolation (IVIVe).

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