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首页-小分子抑制剂&激动剂-Tyrosine Kinase-Focal Adhesion Kinase (FAK)-BJG-03-025
BJG-03-025

Chemical Structure : BJG-03-025

CAS No.: 2553213-90-2

BJG-03-025

货号: PC-72153Not For Human Use, Lab Use Only.

BJG-03-025 is a potent, highly selective FAK tyrosine kinase inhibitor with biochemical IC50 of 20.2 nM.

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

    生物&药学活性

    BJG-03-025 is a potent, highly selective FAK tyrosine kinase inhibitor with biochemical IC50 of 20.2 nM.
    BJG-03-025 demonstrates excellent kinome selectivity was profiled by KINOMEscan screening, PLK1 proved to be a false positive with IC50 of 8.3 uM, 100-300-fold selective for FAK.
    BJG-03-025 displays antiproliferative activity in three-dimensional (3D)-breast and gastric cancer models and impacts cellular signaling and migration.
    BJG-03-025 decreased phosphorylated FAK (pFAK Y397) in gastric cancer CDH1–/–RHOAY42C/+ organoid model, decreased aberrant signaling and proliferation of gastric cancer organoids.

    物理化学性质&存储条件

    分子量 563.725
    分子式 C28H37N9O2S
    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

    6-((2-methoxy-4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)amino)-2,4,9-trimethyl-4,9-dihydro-10H-pyrimido[5,4-b]thiazolo[5,4-e][1,4]diazepin-10-one

    参考文献

    1. Brian J Groendyke, et al. ACS Med Chem Lett. 2020 Dec 14;12(1):30-38.

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