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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Isocitrate Dehydrogenase (IDH)-MRK-A
MRK-A

Chemical Structure : MRK-A

CAS No.: 1934301-68-4

MRK-A (mutant IDH1 inhibitor)

货号: PC-35142Not For Human Use, Lab Use Only.

MRK-A is a potent, highly selective, brain penetrant inhibitor of mutant IDH1 with IC50 of 5 nM, displays a 10,000-fold mutant to wildtype selectivity ratio.

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

    生物&药学活性

    MRK-A is a potent, highly selective, brain penetrant inhibitor of mutant IDH1 with IC50 of 5 nM, displays a 10,000-fold mutant to wildtype selectivity ratio.
    MRK-A decreases ntracellular 2-HG levels both in vitro and in vivo, inhibits 2-HG production in both BT142 and GB10 intracranial xenografts, as well as tumor growth.

    物理化学性质&存储条件

    分子量 454.574
    分子式 C28H30N4O2
    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

    (8-morpholino-5,11-dihydro-6H-benzo[b]pyrido[2,3-e][1,4]diazepin-6-yl)(6,7,8,9-tetrahydro-5H-benzo[7]annulen-7-yl)methanone

    参考文献

    1. Kopinja J, et al. Sci Rep. 2017 Oct 23;7(1):13853.

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