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首页-小分子抑制剂&激动剂-Tyrosine Kinase-c-Kit-CHMFL-KIT-031
CHMFL-KIT-031

Chemical Structure : CHMFL-KIT-031

CAS No.:

CHMFL-KIT-031

货号: PC-62536Not For Human Use, Lab Use Only.

CHMFL-KIT-031 is a highly selective KIT kinase primary V559D mutant inhibitor with IC50/Kd of 28/266 nM, 10-20 fold selectivity over KIT wt.

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

    生物&药学活性

    CHMFL-KIT-031 is a highly selective KIT kinase primary V559D mutant inhibitor with IC50/Kd of 28/266 nM, 10-20 fold selectivity over KIT wt.
    CHMFL-KIT-031 also displays 15-400-fold selectivity over other primary mutants such as L576P and secondary mutants including T670I, V654A as well as N822K and D816V.
    CHMFL-KIT-031 exhibits a selectivity S score (1) of 0.01 among 468 kinases/mutants in the KINOMEScan™ assay.
    CHMFL-KIT-031 inhibits the proliferation of BaF3-TEL-KIT-V559D cells with IC50 of 25 nM, shows potent inhibitory efficacy for KIT V559D mediated signaling pathways in cell and anti-tumor activity in vivo.

    物理化学性质&存储条件

    分子量 487.516
    分子式 C26H25N5O5
    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

    (E)-3,4,5-trimethoxy-N-(2-oxo-2-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)amino)ethyl)benzamide

    参考文献

    1. Yu K, et al. Oncotarget. 2017 Nov 15;8(67):111110-111118.

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