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首页-小分子抑制剂&激动剂-Tyrosine Kinase-EGFR-GNS-1481
GNS-1481

Chemical Structure : GNS-1481

CAS No.: 1903008-81-0

GNS-1481 (GNS1481;GNS 1481)

货号: PC-60919Not For Human Use, Lab Use Only.

A novel potent, irreversible, T790M mutant-selective inhibitor of mutant EGFR with IC50 of 6.2, 3.4 and 4.2 nM for L858R-T790M, T790M and Del19-T790M, respectively.

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

    生物&药学活性

    GNS-1481 is a potent, irreversible, T790M mutant-selective inhibitor of mutant EGFR with IC50 of 6.2, 3.4 and 4.2 nM for L858R-T790M, T790M and Del19-T790M, respectively.
    GNS-1481 displays >5-fold selectivity over wild type EGFR (IC50=26.5 nM) and L858R mutant (IC50=25.8 nM).
    GNS-1481 demonstrates effectivity in multiple mouse xenograft models of human lung adenocarcinoma (T790M-positive or -negative), exhibiting less activity against wild-type EGFR than existing approved EGFR kinase inhibitors (including osimertinib).
    GNS-1481 also shows superior potency against intracranial metastasis of EGFR-mutant lung adenocarcinoma.

    物理化学性质&存储条件

    分子量 518.622
    分子式 C27H34N8O3
    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

    N-(5-((4-(3-cyclopropyl-4-((dimethylamino)methyl)-1H-pyrazol-1-yl)pyrimidin-2-yl)amino)-4-methoxy-2-morpholinophenyl)acrylamide

    参考文献

    1. Rho JK, et al. Cancer Res. 2017 Mar 1;77(5):1200-1211.

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