| S8611 |
Vorasidenib (AG-881)
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Vorasidenib (AG-881) is an orally available inhibitor of mutated forms of both isocitrate dehydrogenase 1 and 2 (IDH1 and IDH2).
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EBioMedicine, 2024, 102:105090
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Cancer Res Commun, 2024, 4(3):876-894
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Cancer Discov, 2023, 13(1):170-193
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| S8205 |
AG-221 (Enasidenib)
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Enasidenib (AG-221) is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzyme.
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iScience, 2025, 28(2):111833
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iScience, 2024, 27(10):110862
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Hematol Oncol, 2024, 42(6):e3316
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| E7887 |
Mutant IDH1-IN-1
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Mutant IDH1-IN-1 is a mutant-selective IDH1 inhibitor with with IC50s of 4, 42, 80 and 143 nM against mutant IDH1 R132C/R132C, IDH1 R132H/R132H, IDH1 R132H/WT and wild type IDH1, respectively.
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| S7185 |
AGI-5198
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AGI-5198 (IDH-C35) is the first highly potent and selective inhibitor of IDH1 R132H/R132C mutants with IC50 of 0.07 μM/0.16 μM.
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EMBO Mol Med, 2025, 10.1038/s44321-025-00296-2
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EBioMedicine, 2024, 102:105090
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Cancers -Basel), 2023, 15(19)4772
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| S7241 |
AGI-6780
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AGI-6780 is a potent and selective inhibitor of IDH2 R140Q mutant with IC50 of 23 nM.
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Nat Commun, 2025, 16(1):8083
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Nat Commun, 2025, 16(1):6913
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EMBO Mol Med, 2025, 10.1038/s44321-025-00296-2
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| S8206 |
AG-120 (Ivosidenib)
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Ivosidenib (AG-120) is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1), with potential antineoplastic activity.
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EBioMedicine, 2024, 102:105090
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Biomed Pharmacother, 2024, 180:117533
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iScience, 2024, 27(10):110862
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| S8530 |
BAY 1436032
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BAY-1436032 is a highly selective, potent and orally available inhibitor of mutant Isocitrate Dehydrogenase 1 (mIDH1). It is a double-digit nanomolar and selective pan-inhibitor of the enzymatic activity of various IDH1-R132X mutants in vitro and displays potent inhibition of 2-HG release (nanomolar range) in patient derived and engineered cell lines expressing different IDH1 mutants.
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Yonsei University Medical Library, 2022,
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Haematologica, 2020, 2 pii: haematol
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| S8881 |
DS-1001b (DS 1001)
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DS-1001b is an oral selective inhibitor of mutant IDH1 R132X with potential antineoplastic activity and is designed to penetrate the blood-brain barrier.
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EBioMedicine, 2024, 102:105090
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| S8949 |
Olutasidenib
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Olutasidenib is a potent, orally bioavailable, brain penetrant and selective mutant IDH1 (mIDH1) inhibitor with IC50 of 21.1 nM, 114 nM for IDH1-R132H, IDH1-R132C, respectively.
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