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MRK-A

Chemical Structure : MRK-A

CAS No.: 1934301-68-4

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MRK-A (mutant IDH1 inhibitor)

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

    Biological Activity

    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.

    Physicochemical Properties

    M.Wt 454.574
    Formula C28H30N4O2
    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

    (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

    References

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

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