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Chemical Structure : Epertinib
CAS No.: 908305-13-5
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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $238 | In stock | |
| 10 mg | $378 | In stock | |
| 25 mg | $588 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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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.
| M.Wt | 560.026 | |
| Formula | C30H27ClFN5O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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 |
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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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