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GSK321

Chemical Structure : GSK321

CAS No.: 1816331-63-1

GSK321 (GSK-321;GSK 321)

Catalog No.: PC-70088Not For Human Use, Lab Use Only.

GSK321 is a highly potent, selective inhibitor of mutant IDH1 with IC50s of 4.6/3.8/2.9 nM for R132H/R132C/R132G respectively.

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    Biological Activity

    GSK321 is a highly potent, selective inhibitor of mutant IDH1 with IC50s of 4.6/3.8/2.9 nM for R132H/R132C/R132G respectively.
    GSK321 shows modest activity against WT IDH1 (IC50=46 nM) and exhibits no inhibitory activity against IDH2.
    GSK321 inhibits intracellular 2-HG production in HT1080 cells (EC50= 85 nM).

    Physicochemical Properties

    M.Wt 501.5624
    Formula C28H28FN5O3
    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

    (R)-1-(4-fluorobenzyl)-N-(3-((S)-1-hydroxyethyl)phenyl)-7-methyl-5-(1H-pyrrole-2-carbonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine-3-carboxamide

    References

    1. Okoye-Okafor UC, et al. Nat Chem Biol. 2015 Nov;11(11):878-86.

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