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首页-小分子抑制剂&激动剂-Tyrosine Kinase-EGFR-EGFR inhibitor 9
EGFR inhibitor 9

Chemical Structure : EGFR inhibitor 9

CAS No.:

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EGFR inhibitor 9

货号: PC-21316Not For Human Use, Lab Use Only.

EGFR inhibitor 9 is a potent, selective, brain-penetrant and orally bioavailable EGFR inhibitor, exhibits potent activity in osimertinib-resistant cell lines bearing L858R/C797S and exon19del/C797S EGFR resistance mutations.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

EGFR inhibitor 9 is a potent, selective, brain-penetrant and orally bioavailable EGFR inhibitor, exhibits potent activity in osimertinib-resistant cell lines bearing L858R/C797S and exon19del/C797S EGFR resistance mutations.
EGFR inhibitor 9 displays potent antiproliferative activity in patient-derived non-small-cell lung cancer cell lines HCC827 (EGFR mutation = exon19del), NCI-H3255 (EGFR mutation = L858R), and osimertinib-resistant engineered cell lines (Ba/F3-L858R/C797S; Ba/F3 del E746_A750/C797S) while displaying no activity in NCI-H1975 (EGFR mutation = L858R/T790M) and minimal activity in A431 cell line (overexpressed EGFRwt).
EGFR inhibitor 9 d isplays excellent activity against the NCI-H3255 NSCLC cell line bearing the common EGFRL858R mutation, with an IC50 of 7.2 nM.
EGFR inhibitor 9 also has potent activity against HCC827 NSCLC cells harboring EGFRdel E746_A750 with an IC50 of 3.1 nM.
EGFR inhibitor 9 exhibits strong activity in osimertinib-resistant engineered Ba/F3 cell lines bearing EGFRL858R/C797S and EGFRdel E746_A750/C797S.

物理化学性质&存储条件

分子量 461.92
分子式 C22H25ClFN5O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

N-(3-chloro-2-fluorophenyl)-7-methoxy-6-(2-((4-methylpiperazin-1-yl)oxy)ethoxy)quinazolin-4-amine

参考文献

1. Hill J, et al. J Med Chem. 2023 Nov 7. doi: 10.1021/acs.jmedchem.3c01669.

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