详情描述
Enasidenib, also known as AG-221 and CC-90007, 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.
Product information
CAS Number: 1446502-11-9
Molecular Weight: 473.38
Formula: C19H17F6N7O
Chemical Name: 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
Smiles: CC(C)(O)CNC1N=C(NC2C=C(N=CC=2)C(F)(F)F)N=C(N=1)C1=CC=CC(=N1)C(F)(F)F
InChiKey: DYLUUSLLRIQKOE-UHFFFAOYSA-N
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)
Technical Data
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 50 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
In Vitro:
AG-221 was used at 1 µM in vitro and cellular assays.
In Vivo:
AG-221 was dosed orally to mice bearing IDH2 mutant tumors at 5-50 mg/Kg once per day.
References:
- Chong-Hui Gu, et al. Crystalline forms of therapeutically active compounds and use thereof. (2015) PCT WO 2015018060
Products are for research use only. Not for human use.