| Identification | Back Directory | [Name]
2H-Pyrimido[4,5-d][1,3]oxazin-2-one, 7-[[(1S)-1-[4-[(1S)-2-cyclopropyl-1-[4-(1-oxo-2-propen-1-yl)-1-piperazinyl]ethyl]phenyl]ethyl]amino]-1-ethyl-1,4-dihydro- | [CAS]
2230263-60-0 | [Synonyms]
Mutant IDH1-IN-6
2H-Pyrimido[4,5-d][1,3]oxazin-2-one, 7-[[(1S)-1-[4-[(1S)-2-cyclopropyl-1-[4-(1-oxo-2-propen-1-yl)-1-piperazinyl]ethyl]phenyl]ethyl]amino]-1-ethyl-1,4-dihydro- | [Molecular Formula]
C28H36N6O3 | [MOL File]
2230263-60-0.mol | [Molecular Weight]
504.62 |
| Hazard Information | Back Directory | [Uses]
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[1]. | [in vivo]
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]. | Animal Model: | Athymic nude mice (20-22 g) injected with TB08 cells[1] | | Dosage: | 1 mg/kg, 2 mg/kg, 4 mg/kg, 8 mg/kg, 16 mg/kg, 32 mg/kg | | Administration: | Oral gavage; twice daily; for 3 days | | Result: | Inhibitied of 2-hydroxyglutarate in IDHl mutant xenograft mice.
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| [IC 50]
IDH1; IDH2 | [References]
[1] Renato Alejandro BAUER, et al. 7-phenylethylamino-4h-pyrimido[4,5-d][1,3]oxazin-2-one compounds as mutant idh1 and idh2 inhibitors. WO2018111707A1. |
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