AS-605240

Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of phosphatidylinositol at the three position to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3. PI3Kgamma is a class 1B PI3K that is composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit, whereas PI3Kalpha, beta, and delta are class 1A enzymes composed of p110 and p85 subunits AS-605240 is an orally active inhibitor of PI3-kinase gamma that suppresses joint inflammation in mouse models of rheumatoid arthritis. It inhibits human recombinant PI3Kgamma, alpha, beta, and delta in an ATP-competitive manner with IC50 values of 8, 60, 270, and 300 nM, respectively. AS-605240 inhibits C5a-mediated phosphorylation of protein kinase B in RAW 264 cells with an IC50 value of 90 nM. In vivo, AS-605240 reduced RANTES-induced peritoneal neutrophil recruitment in a mouse model of leukocyte chemotaxis with an ED50 value of 9.1 mg/kg.Formal Name: 5-(6-quinoxalinylmethylene)-2,4-thiazolidinedione. CAS Number: 648450-29-7. Molecular Formula: C12H7N3O2S. Formula Weight: 257.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 0.2 mg/ml, DMSO: 0.5 mg/ml. lambdamax: 249, 297, 337, 352 nm. SMILES: O=C1NC(=O)/C(=C\c2ccc3nccnc3c2)\S1. InChi Code: InChI=1S/C12H7N3O2S/c16-11-10(18-12(17)15-11)6-7-1-2-8-9(5-7)14-4-3-13-8/h1-6H,(H,15,16,17)/b10-6-. InChi Key: SQWZFLMPDUSYGV-POHAHGRESA-N.