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Vorasidenib (AG-881) is a potent and selective, first-in-Class, brain-penetrant orally available inhibitor of mutated forms of both isocitrate dehydrogenase type 1 (IDH1, IDH1 [NADP+] soluble) in the cytoplasm and type 2 (IDH2, isocitrate dehydrogenase [NADP+], mitochondrial) in the mitochondria. Vorasidenib (AG-881) exhibits nanomolar inhibition of (D)-2-hydroxyglutarate (D-2-HG), and the IC50 ranges of 0.04~22 nM against IDH1 R132C, IDH1 R132G, IDH1 R132H and IDH1 R132S and 7~14 nM against IDH2 R140Q and 130 nM against IDH2 R172K. In a TS603-IDH1R132H mouse xenograft model, Vorsidenib reduces tumor growth at a dose of 50 mg/kg.
| Molecular Weight | 414.74 |
| Formula | C14H13ClF6N6 |
| CAS Number | 1644545-52-7 |
| Solubility (25°C) | DMSO 85 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Isocitrate Dehydrogenase (IDH) Products |
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| Mutant IDH1-IN-4
Mutant IDH1-IN-4 is an inhibitor of mutant isocitrate dehydrogenase 1 (IDH 1) with an IC50 value of ≤ 0.5 μM for mutant IDH 1 in R132H, HT1080 and U87R132H cells. |
| (S,S)-GSK321
(S,S)-GSK321 is the (S,S)-enantiomer of GSK321.GSK321 is a potent inhibitor of the mutant isocitrate dehydrogenase 1 (IDH1) enzyme. |
| IDH1 Inhibitor 1
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. |
| IDH1 Inhibitor 7
IDH1 Inhibitor 7 is an IDH1 inhibitor with an IC50 of less than 100 nM. |
| (R,R)-GSK321
(R,R)-GSK321 is an isomer of GSK321 and a wild-type isocitrate dehydrogenase 1 (WT IDH1) inhibitor with an IC50 value of 120 nM. |
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