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EGFR inhibitor 57

Chemical Structure : EGFR inhibitor 57

CAS No.: 2781912-10-3

EGFR inhibitor 57

货号: PC-49365Not For Human Use, Lab Use Only.

EGFR inhibitor 57 is a novel potent, selective, allosteric fourth-generation EGFR L858R inhibitor, overcomes EGFRC797S-mediated resistance in NSCLC harboring the activating EGFRL858R mutation.

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

    生物&药学活性

    EGFR inhibitor 57 is a novel potent, selective, allosteric fourth-generation EGFR L858R inhibitor, overcomes EGFRC797S-mediated resistance in NSCLC harboring the activating EGFRL858R mutation.
    EGFR inhibitor 57 is the first allosteric EGFR inhibitor that demonstrates robust tumor regression in a mutant EGFRL858R/C797S tumor model.
    EGFR inhibitor 57 is active in an H1975 EGFRL858R/T790M NSCLC xenograft model and shows superior efficacy in combination with osimertinib compared to the single agents.

    物理化学性质&存储条件

    分子量 681.81
    分子式 C37H37F2N7O2S
    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

    2-(4-(difluoromethyl)-6-((4-((4-(hydroxymethyl)piperidin-1-yl)methyl)phenyl)ethynyl)-7-methyl-2H-indazol-2-yl)-2-(6',7'-dihydrospiro[cyclopropane-1,5'-pyrrolo[1,2-c]imidazol]-1'-yl)-N-(thiazol-2-yl)acetamide

    参考文献

    1. Ulrike Obst-Sander, Journal of Medicinal Chemistry, 2022.

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