For research use only. Not for therapeutic Use.
<p style=/line-height:25px/>Enasidenib is a oral potent, selective, reversible inhibitor of mutant IDH2.<br>Target: IDH2<br>in vitro: Enasidenib is a potent and selective IDH2 inhibitor with potential anticancer activity (IDH2 = Isocitrate dehydrogenase 2). The mutations of IDH2 present in certain cancer cells result in a new ability of the enzyme to catalyze the NAPH-dependent reduction of α-ketoglutarate to R(-)-2-hydroxyglutarate (2HG). The production of 2HG is believed to contribute to the formation and progression of cancer . The inhibition of mutant IDH2 and its neoactivity is therefore a potential therapeutic treatment for cancer.<br>in vivo: AG-221 is able to potently reduce 2HG found in the bone marrow, plasma and urine of engrafted mice. In an updated analysis of a dose-ecalation phase I trial that now includes 73 patients with advanced hematologic cancer, AG-221 was well tolerated and achieved more than 90% inhibition of its target (ie, 2-HG [2-hydroxyglutarate]) in patients with an IDH2mutation.</p>
| Catalog Number | I001718 |
| CAS Number | 1446502-11-9 |
| Synonyms | 2-methyl-1-((4-(6-(trifluoromethyl)pyridin-2-yl)-6-((2-(trifluoromethyl)pyridin-4-yl)amino)-1,3,5-triazin-2-yl)amino)propan-2-ol |
| Molecular Formula | C₁₉H₁₇F₆N₇O |
| Purity | ≥95% |
| Target | Isocitrate Dehydrogenase (IDH) |
| Solubility | 10 mM in DMSO |
| Storage | Store at -20°C |
| InChI | InChI=1S/C19H17F6N7O/c1-17(2,33)9-27-15-30-14(11-4-3-5-12(29-11)18(20,21)22)31-16(32-15)28-10-6-7-26-13(8-10)19(23,24)25/h3-8,33H,9H2,1-2H3,(H2,26,27,28,30,31,32) |
| InChIKey | DYLUUSLLRIQKOE-UHFFFAOYSA-N |
| SMILES | CC(C)(CNC1=NC(=NC(=N1)NC2=CC(=NC=C2)C(F)(F)F)C3=NC(=CC=C3)C(F)(F)F)O |
| Reference | <p style=/line-height:25px/> |
