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IDH1 Inhibitor 1 is a potent, orally bioavailable, brain-permeable, selective mutant IDH1 inhibitor that inhibits IDH1R132H, IDH1R132C, and IDH1WT with IC50s of 0.021 μM, 0.045 μM, and 2.52 μM, respectively. possesses antitumor activity.
| Molecular Weight | 450.39 |
| Formula | C20H18F4N6O2 |
| CAS Number | 2234285-81-3 |
| Form | Solid |
| Solubility (25°C) | DMSO >100 mg/mL |
| Storage | 4°C, protect from light, dry, sealed |
| Related Isocitrate Dehydrogenase (IDH) Products |
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AGI-5198 (IDH-C35) is the first highly potent and selective inhibitor of IDH1 R132H and R132C mutants in vitro with IC50 values of 0.07 μM and 0.16 μM, respectively. |
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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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Enasidenib is an oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes, with IC50s of 100 and 400 nM against IDH2R140Q and IDH2R172K, respectively. |
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