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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Isocitrate Dehydrogenase (IDH)-HMS-101
HMS-101

Chemical Structure : HMS-101

CAS No.: 1070690-06-0

HMS-101 (HMS101)

货号: PC-35141Not For Human Use, Lab Use Only.

HMS-101 (HMS101) is a potent, selective mutant IDH1 inhibitor, the IC50 is significantly lower in mouse bone marrow cells transduced with IDH1mut compared with IDH1wt (1 uM vs 12 uM, respectively).

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

    生物&药学活性

    HMS-101 (HMS101) is a potent, selective mutant IDH1 inhibitor, the IC50 is significantly lower in mouse bone marrow cells transduced with IDH1mut compared with IDH1wt (1 uM vs 12 uM, respectively).
    HMS-101 binds to the isocitrate-binding pocket of mutant IDH1, significantly reduces intracellular R-2HG levels in vitro HoxA9+IDH1mut cells at 10 uM.
    HMS-101 induces apoptosis in IDH1mut cells, markedly reduces phospho-ERK1/2 and the ratio of phospho-ERK/total-ERK, inhibits human AML cell growth.

    物理化学性质&存储条件

    分子量 305.441
    分子式 C18H28FN3
    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

    2-[2-[3-(4-fluorophenyl)pyrrolidin-1-yl]ethyl]-1,4-dimethylpiperazine

    参考文献

    1. Chaturvedi A, et al. Blood. 2013 Oct 17;122(16):2877-87.

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