(S,R)-GSK321

(S,R)-GSK321

• CAS Number: 1816272-18-0
• UNSPSC Description: (S,R)-GSK321 is a potent, selective mutant IDH1 inhibitor with IC50 values of 2.9, 3.8, 4.6 and 46 nM for R132G, R132C, R132H and WT IDH1, respectively, and >100-fold selectivity over IDH2. (S,R)-GSK321 induces decrease in intracellular 2-HG, abrogation of the myeloid differentiation block and induction of granulocytic differentiation at the level of leukemic blasts and more immature stem-like cells. (S,R)-GSK321can be used for research of acute myeloid leukemia (AML) and other cancers[1].
• Target Antigen: Isocitrate Dehydrogenase (IDH)
• Type: Reference compound
• Related Pathways: Metabolic Enzyme/Protease
• Field of Research: Cancer
• Assay Protocol: https://www.medchemexpress.com/s-r-gsk321.html
• Purity: 98.78
• Solubility: DMSO : 100 mg/mL (ultrasonic)
• Smiles: C[C@@H](O)C1=CC=CC(NC(C2=NN(C3=C2CN(C[C@@H]3C)C(C4=CC=CN4)=O)CC5=CC=C(C=C5)F)=O)=C1
• Molecular Weight: 501.55
• References & Citations: [1]Okoye-Okafor UC, et, al. New IDH1 mutant inhibitors for treatment of acute myeloid leukemia. Nat Chem Biol. 2015 Nov;11(11):878-86.
• Shipping Conditions: Room Temperature
• Storage Conditions: -20°C, 3 years; 4°C, 2 years (Powder)
• Clinical Information: No Development Reported