DC8051 |
AG-120 (Ivosidenib)
Featured
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AG-120 is a first-in-class, orally available, selective, potent inhibitor of the mutated IDH1 protein. |
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DC8374 |
AG-221(Enasidenib)
Featured
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AG-221 is an orally available, selective, potent inhibitor of the mutated IDH2 protein. |
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DC10439 |
Vorasidenib (AG881)
Featured
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AG-881 is a potent and selective orally available inhibitor of mutated forms of both isocitrate dehydrogenase type 1 (IDH1) in the cytoplasm and type 2 (IDH2). |
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DC5050 |
AGI-5198
Featured
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AGI-5198 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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DC7174 |
AGI-6780
Featured
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AGI-6780 is the first highly potent and selective small molecule inhibitor of isocitrate dehydrogenases, which binds in an allosteric manner at the dimer interface of mutant IDH2-R140Q (IC50=23 nM). |
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DC11719 |
BAY-1436032 |
BAY-1436032 (BAY1436032) is a potent, selective, orally available inhibitor of pan-mutant IDH1 with IC50 of 15 nM for both IDH1 R132H and R132C, respectively. |
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DC10538 |
IDH-305
Featured
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IDH305 is an inhibitor of the citric acid cycle enzyme isocitrate dehydrogenase [NADP] cytoplasmic (isocitrate dehydrogenase 1; IDH1) with mutations at residue R132 (IDH1(R132)), with potential antineoplastic activity. |
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DC10830 |
IDH-889
Featured
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IDH889 is a potent and selective inhibitors of IDH1. IDH899 shows IDH (R132H) IC50 = 20 nM; Cell 2-HG IC50 = 14 nM. |
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DC7982 |
Mutant IDH1-IN-1
Featured
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Mutant IDH1-IN-1 is a potent mutant IDH1 R132H inhibitor with IC50 < 0.1 uM(A level in Patent). |
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DC12281 |
Olutasidenib (FT-2102)
Featured
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Olutasidenib is a highly potent, selective inhibitor of mutant Isocitrate dehydrogenase (IDH)1 that could be used in the treatment of acute myeloid leukemia. |
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DC28343 |
Mutant IDH1-IN-4 |
Mutant IDH1-IN-4 (compound 434) is an inhibitor of mutant Isocitrate dehydrogenase 1 (IDH 1), with IC50 values of ≤ 0.5 μM for mutant IDH1 in R132H, HT1080 and U87R132H cells. |
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DC28576 |
DS-1001b
Featured
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DS-1001b is a mutant IDH-1 (Isocitrate Dehydrogenase-1) inhibitor extracted from patent WO2016052697A1, Example 168, and has antitumor activity. |
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DC44726 |
Enasidenib Mesylate
Featured
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Enasidenib (Idhifa, AG-221) mesylate is an orally available, selective and potent inhibitor of mutant isocitrate dehydrogenase 2 (IDH2). |
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DC45831 |
WT IDH1 Inhibitor 2 |
WT IDH1 Inhibitor 2 is a wild-type isocitrate dehydrogenase 1 (WT IDH1) inhibitor with an IC50 value of 120 nM. WT IDH1 Inhibitor 2 as a mutant R132H IDH1 inhibitor, is an isomer of GSK321 with some wild-type cross reactivity. |
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DC46300 |
IDH-C227 |
IDH-C227 is a potent and selective IDH1R132H inhibitor. IDH-C227 has anticancer effcts. |
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DC48219 |
Safusidenib |
Safusidenib is a novel IDH1 inhibitor for the treatment of IDH1-mutated tumors. |
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DC49742 |
AGI-12026 |
AGI-12026 is brain-penetrant dual inhibitor of mutant IDH1 and 2. AGI-12026 shows partial inhibition of the IDH1-R132H homodimer as allosteric modulators. AGI-12026 has the potential for research of glioma. |
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DC70642 |
NCATS-SM5637 |
NCATS-SM5637 (NSC 791985) is a potent, selective mutant IDH1 inhibitor with IC50 of 81/72 nM for IDH1 mutant R132H/R132C, respctively.NCATS-SM5637 showed higher tumoral concentrations that corresponded to lower 2-HG concentrations in engineered mIDH1-U87-xenograft mouse model, compared with the approved drug AG-120 (ivosidenib). |
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DC72374 |
(S,S)-GSK321 |
(S,S)-GSK321 is a (S,S)-enantiomer of GSK321. |
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