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Chemical Structure : NS-062
Catalog No.: PC-35996Not For Human Use, Lab Use Only.
NS-062 (NS062) is a novel, specific targeted covalent inhibitor that shows high reactivity toward Cys797 of EGFR.
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NS-062 (NS062) is a novel, specific targeted covalent inhibitor that shows high reactivity toward Cys797 of EGFR.
NS-062 showed higher target specificity for EGFR than the corresponding Michael acceptors in a wide concentration range (0.1-10 μM).
NS-062 showed strong antiproliferative activity (IC50=0.19 μM) against erlotinib-resistant H1975 cells (L858R T790M doublemutant EGFR).
NS-062 effectively inhibited EGFR (Y1068) autophosphorylation in H1975 cells at 0.5 uM, significantly suppressed tumor growth in a mouse xenograft model after oral administration.
| M.Wt | 623.483 | |
| Formula | C28H30Cl2F2N6O4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Shindo N, et al. Nat Chem Biol. 2019 Jan 14. doi: 10.1038/s41589-018-0204-3.
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