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IDH1R132C

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-112601

    Isocitrate Dehydrogenase (IDH) Cancer
    IDH1 Inhibitor 1 is a potent, orally bioavailable, brain-penetrant and selective mutant IDH1 inhibitor with IC50s of 0.021 μM, 0.045 μM, and 2.52 μM for IDH1 R132H, IDH1 R132C, and IDH1 WT, respectively . Anticancer activity .
    <em>IDH1</em> Inhibitor 1
  • HY-114226
    Olutasidenib
    1 Publications Verification

    FT-2102

    Isocitrate Dehydrogenase (IDH) Inflammation/Immunology Cancer
    Olutasidenib (FT-2102) is a highly potent, orally active, brain penetrant and selective inhibitor of mutant Isocitrate dehydrogenase 1 (IDH1), with IC50 values of 21.2 nM and 114 nM for IDH1- R132H and IDH1- R132C, respectively . Olutasidenib (FT-2102) is under the study in the treatment of acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS) .
    Olutasidenib
  • HY-104036

    Isocitrate Dehydrogenase (IDH) Cancer
    IDH-305 is an orally available, mutant-selective and brain-penetrant IDH1 inhibitor that targets IDH1 (R132) mutation. IDH-305 exhibits greater than 200 fold selectivity for mutant IDH1 isoforms vs. WT (IC50= 27 nM (IDH1 R132H), 28 nM (IDH1 R132C), 6.14 µM (IDH1 WT)) .
    IDH-305
  • HY-145594

    AB-291; DS-1001

    Isocitrate Dehydrogenase (IDH) Cancer
    Safusidenib (AB-291; DS-1001) is an orally bioavailable, selective mutant IDH1 inhibitor. Safusidenib strongly inhibits mutant IDH1 but not wild-type IDH1. Safusidenib impairs tumor activity in chondrosarcoma . Safusidenib exhibits activity against IDH1R132H, and IDH1R132C with IC50s of 15, and 130 nM in assays without any preincubation, respectively .
    Safusidenib
  • HY-131312

    Mutant IDH1-IN-6

    Isocitrate Dehydrogenase (IDH) Cancer
    Mutant IDH1-IN-6 is a potent, selective and orally active mutant isocitrate dehydrogenase (IDH) inhibitor with IC50s of 6.27 nM, 3.71 nM, 36.9 nM and 11.5 nM for IDH1 R132H, IDH1 R132C, IDH2 R140Q and IDH2 R172K mutant enzymes, respectively. Mutant IDH1-IN-6 is less active at inhibiting the IDH wild-type enzymes .
    LY3410738
  • HY-112289

    Isocitrate Dehydrogenase (IDH) Cancer
    IDH889 is an orally available, brain penetrant, allosteric and mutant specific inhibitor of isocitrate dehydrogenase 1 (IDH1). IDH889 has potent selectivity for IDH1 R132* mutations, with IC50s of 0.02 μM, 0.072 μM and 1.38 μM for IDH1 R132H, IDH1 R132C and IDH1 wt, respectively. IDH889 shows potent cellular inhibition of R-2-hydroxyglutarate (2-HG) production with an IC50 of 0.014 μM .
    IDH889
  • HY-104042
    Vorasidenib
    3 Publications Verification

    AG-881

    Isocitrate Dehydrogenase (IDH) Cancer
    Vorasidenib (AG-881) is an orally available, brain penetrant second-generation dual mutant isocitrate dehydrogenases 1 and 2 (mIDH1/2) inhibitor. Vorasidenib (AG-881) exhibits nanomolar inhibition of (D)-2-hydroxyglutarate (D-2-HG), and the IC50 ranges of 0.04~22 nM against IDH1 R132C, IDH1 R132G, IDH1 R132H and IDH1 R132S and 7~14 nM against IDH2 R140Q and 130 nM against IDH2 R172K .
    Vorasidenib
  • HY-112289B

    Isocitrate Dehydrogenase (IDH) Cancer
    (1R)-IDH889 is the isomer of IDH889 (HY-112289), and can be used as an experimental control. IDH889 is an orally available, brain penetrant, allosteric and mutant specific inhibitor of isocitrate dehydrogenase 1 (IDH1). IDH889 has potent selectivity for IDH1 R132* mutations, with IC50s of 0.02 μM, 0.072 μM and 1.38 μM for IDH1 R132H, IDH1 R132C and IDH1 wt, respectively. IDH889 shows potent cellular inhibition of R-2-hydroxyglutarate (2-HG) production with an IC50 of 0.014 μM .
    (1R)-IDH889

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