Epertinib |CAS:908305-13-5 Probechem Biochemicals

Chemical Structure : Epertinib

CAS No.: 908305-13-5

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Epertinib (S-222611;S222611)

货号: PC-63309Not For Human Use, Lab Use Only.

Epertinib (S-222611) is a novel potent, orally active, reversible EGFR and HER2 inhibitor with IC50 of 1.48, 7.15 and 2.49 nM for EGFR, HER2 and HER4, respectively.

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生物&药学活性

Epertinib (S-222611) is a novel potent, orally active, reversible EGFR and HER2 inhibitor with IC50 of 1.48, 7.15 and 2.49 nM for EGFR, HER2 and HER4, respectively.
Epertinib (S-222611) does not inhibit KDR, IGF1R, SRC, KIT, PDGFRβ.
Epertinib (S-222611) inhibits phosphorylation of EGFR and HER2 kinases in NCI-N87 cells with IC50 of 4.5 and 1.6 nM, shows growth inhibition of NCI-N87 cell with IC50 of 8.3 nM.
Epertinib (S-222611) shows potent antitumor activity over lapatinib in a variety of xenograft models, exhibits excellent activity and could be effective against bone and brain metastasis.

物理化学性质&存储条件

分子量	560.026
分子式	C30H27ClFN5O3
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	(R,Z)-1-(4-((3-chloro-4-((3-fluorobenzyl)oxy)phenyl)amino)quinazolin-6-yl)but-2-yn-1-one O-morpholin-3-ylmethyl oxime

参考文献

1. Tanaka H, et al. Cancer Sci. 2014 Aug;105(8):1040-8.

2. Spicer J, et al. Eur J Cancer. 2015 Jan;51(2):137-45.

3. Tanaka Y, et al. Sci Rep. 2018 Jan 10;8(1):343.

Epertinib (S-222611;S222611)

生物&药学活性

物理化学性质&存储条件

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Epertinib (S-222611;S222611)

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物理化学性质&存储条件

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