| Bioactivity | Ivosidenib (AG-120) is an orally active inhibitor of isocitrate dehydrogenase 1 mutant (mIDH1) enzyme, it exhibits profound d-2-hydroxyglutatrate (2-HG) lowering in vivo. Ivosidenib (AG-120) has the potential for AML therapy due to its acceptable safety profile and clinical activity[1]. | ||||||||||||
| Target | 12 nM (mouse IDH1R132H) | ||||||||||||
| Invitro | Ivosidenib (AG-120) (0-13 μM; 48 hours) inhibits several IDH1-R132 mutants with potency similar IC50 values: IDH1-R132H (IC50=12 nM); IDH1-R132C (IC50=13 nM); IDH1-R132G (IC50=8 nM); IDH1-R132L (IC50=13 nM); IDH1-R132S (IC50=12 nM), respectively[1]. | ||||||||||||
| In Vivo | AG-120 (gavage administration; 50 mg/kg and 150 mg/kg) declines tumor 2-HG concentration rapidly, with maximum inhibition (92.0% and 95.2% at the 50 mg/kg and 150 mg/kg doses, respectively) achieved at -12 h post dose[1]. Animal Model: | ||||||||||||
| Name | Ivosidenib | ||||||||||||
| CAS | 1448347-49-6 | ||||||||||||
| Formula | C28H22ClF3N6O3 | ||||||||||||
| Molar Mass | 582.96 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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| Reference | [1]. Popovici-Muller J, et al. Discovery of AG-120 (Ivosidenib): A First-in-Class Mutant IDH1 Inhibitor for the Treatment of IDH1Mutant Cancers. ACS Med Chem Lett. 2018 Jan 19;9(4):300-305. |
Ivosidenib
CAS: 1448347-49-6 F: C28H22ClF3N6O3 W: 582.96
Ivosidenib (AG-120) is an orally active inhibitor of isocitrate dehydrogenase 1 mutant (mIDH1) enzyme, it exhibits profo
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