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首页-小分子抑制剂&激动剂-Tyrosine Kinase-EGFR-BIBU1361 dihydrochloride
BIBU1361 dihydrochloride

Chemical Structure : BIBU1361 dihydrochloride

CAS No.: 1643609-75-9

BIBU1361 dihydrochloride (BIBU 1361)

货号: PC-62999Not For Human Use, Lab Use Only.

BIBU1361 is a potent, selective, orally active EGFR inhibitor with IC50 of 3 nM, shows weak activity against HER2 (IC50=280 nM) and no inhibition on IGF1R, HGFR, Src, and VEGFR2 (IC50>10 uM).

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

    生物&药学活性

    BIBU1361 dihydrochloride is a potent, selective, orally active EGFR inhibitor with IC50 of 3 nM, shows weak activity against HER2 (IC50=280 nM) and no inhibition on IGF1R, HGFR, Src, and VEGFR2 (IC50>10 uM).
    BIBU1361 inhibits EGF-induced phosphorylation of EGFR in a dose-dependent manner in A431 cells (EC50=122 nM).
    BIBU1361 demonstrates effectivity in tumour xenografts mice.

    物理化学性质&存储条件

    分子量 516.871
    分子式 C22H29Cl3FN7
    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-(3-Chloro-4-fluorophenyl)-6-[4-[(diethylamino)methyl]-1-piperidinyl]-pyrimido[5,4-d]pyrimidin-4-amine dihydrochloride

    参考文献

    1. Solca FF, et al. J Pharmacol Exp Ther. 2004 Nov;311(2):502-9.

    2. Ghildiyal R, et al. Mol Carcinog. 2013 Dec;52(12):970-82.

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