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首页-小分子抑制剂&激动剂-Tyrosine Kinase-Anaplastic Lymphoma Kinase (ALK)-M4K2234
M4K2234

Chemical Structure : M4K2234

CAS No.: 2421141-51-5

M4K2234 (ALK1/2 inhibitor)

货号: PC-72014Not For Human Use, Lab Use Only.

M4K2234 is a potent, selective ALK1 (ACVRL1) and ALK2 (ACVR1) protein kinase inhibitor with IC50 of 7 and 14 nM, respectively.

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

    生物&药学活性

    M4K2234 is a potent, selective ALK1 (ACVRL1) and ALK2 (ACVR1) protein kinase inhibitor with IC50 of 7 and 14 nM, respectively.
    M4K2234 inhibits only ALK1/2 and one additional off target (TNIK) by kinome-wide screening against 375 protein kinases at 1 uM.
    M4K2234 demonstrated in cell based target engagement assays with an IC50 of 83nM for ALK1 and 13 nM for ALK2.
    M4K2234 exhibits only very weak potency against ALK4/5.
    M4K2234 affects phosphorylation of SMAD1/5/8 that corresponds to BMP branch of signalling which is mediated, besides others, also by ALK1/2 kinases.
    M4K2234 has only a very weak effect on SMAD2/3 phosphorylation that corresponds to TGF beta branch of signalling which is mediated mostly via ALK4/5/7.

    物理化学性质&存储条件

    分子量 462.57
    分子式 C27H31FN4O2
    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

    Benzamide, 2-fluoro-6-methoxy-4-[4-methyl-5-[4-[4-(1-methylethyl)-1-piperazinyl]phenyl]-3-pyridinyl]-

    参考文献

    1. Ensan D, et al. J Med Chem. 2020 May 14;63(9):4978-4996.

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