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首页-小分子抑制剂&激动剂-Tyrosine Kinase-EGFR-NS-062
NS-062

Chemical Structure : NS-062

CAS No.: 2226257-92-5

NS-062 (NS062, NS 062)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    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.

    物理化学性质&存储条件

    分子量 623.483
    分子式 C28H30Cl2F2N6O4
    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

    (2R)-1-(2-chloro-2-fluoroacetyl)-N-(4-((3-chloro-4-fluorophenyl)amino)-7-(3-morpholinopropoxy)quinazolin-6-yl)pyrrolidine-2-carboxamide

    参考文献

    1. Shindo N, et al. Nat Chem Biol. 2019 Jan 14. doi: 10.1038/s41589-018-0204-3.

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