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HMS-101

Chemical Structure : HMS-101

CAS No.: 1070690-06-0

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HMS-101 (HMS101)

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    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.

    Physicochemical Properties

    M.Wt 305.441
    Formula C18H28FN3
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20 °C 12 Months; 4°C 6 Months
    In Solvent
    -80 °C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO
    Chemical Name/SMILES

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

    References

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

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