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Cat.No.ABP000893 Chemical NameAZD4547/AZD-4547/ MolFormulaC26H33N5O3 MolWeight463.5719 Purity 98%

Chemical Name : AZD4547/AZD-4547/

CAS : 1035270-39-3

Synonyms: N-(5-(3,5-dimethoxyphenethyl)-1H-pyrazol-3-yl)-4-((3R,5S)-3,5-dimethylpiperazin-1-yl)benzamide

Storage:at -20℃ 2 years


WZ4002 is an irreversiblely inhibitor against EGFR T790M (mutation of the gatekeeper T790 residue) which is detected in 50% of clinically resistant patients to gefitinib or erlotinib. WZ4002 has a basic chemical framework (covalent pyrimidine) which is different from that of other EGFR inhibitors. [1]
This agent is 30- to 100-fold more potent against EGFR T790M, and up to 100-fold less potent against wildtype EGFR, than quinazoline-based EGFR inhibitors (HKI-272 and CL-387,785) in vitro. [1]
This agent has a 300-fold lower half-maximum inhibitory concentration (IC50<20nM) against the PC9GR(delE746_A750/T790M, gefitinib-resistant) cells compared with clinical-stage inhibitors such as HKI-272. [1]
In a 2-week efficacy study, WZ4002 treatment resulted in significant tumour regressions compared with vehicle alone in both T790M-containing murine models.


[1] Zhou W et al. Nature. 2009 Dec 24;462(7276):1070-4