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Epertinib

Chemical Structure : Epertinib

CAS No.: 908305-13-5

Epertinib (S-222611;S222611)

Catalog No.: 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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Biological Activity

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.

Physicochemical Properties

M.Wt 560.026
Formula C30H27ClFN5O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
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

References

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.

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