Mutant IDH1-IN-6 is a potent, selective and orally activemutantisocitrate dehydrogenase (IDH)inhibitor withIC₅₀s of 6.27 nM, 3.71 nM, 36.9 nM and 11.5 nM forIDH1R132H,IDH1R132C,IDH2 R140QandIDH2 R172K mutant enzymes, respectively. Mutant IDH1-IN-6 is less active at inhibiting the IDH wild-type enzymes^[1].

IC50: 6.27 nM (IDH1 R132H), 3.71 nM (IDH1 R132C), 36.9 nM (IDH2 R140Q), 11.5 nM (IDH2 R172K), 105 nM (IDH1 wild-type) and 884 nM (IDH2 wild-type)^[1]

Mutant IDH1-IN-6 (example 2) inhibits production of 2-hydroxyglutarate in HT1080 cells with an IC50 of 1.28 nM, indicating the inhibition of mutant IDHl R132C in cells. aKG, a metabolite generated by wild-type IDHl is not affected by Mutant IDH1-IN-6, indicating Mutant IDH1-IN-6 is selective for mutant IDHl over wild type IDHl in cells^[1].

Mutant IDH1-IN-6 (Example 2; 0-32 mg/kg; oral gavage; twice daily; for 3 days) treatment inhibitis of 2-hydroxyglutarate in a dose-dependent manner in IDHl mutant xenograft mice^[1].

504.62

C₂₈H₃₆N₆O₃

2230263-60-0

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