CZC-24832

CZC-24832 is an inhibitor of PI3Kgamma (IC50 = 0.025 µM in a binding assay). It is selective for PI3Kgamma over PI3Kdelta, PI3Kalpha, and PI3Kbeta (IC50s = 7.9, >10, and 1.26 µM, respectively, in binding assays), as well as a panel of 154 lipid and protein kinases. CZC-24832 inhibits phosphorylation of Akt induced by complement component 5a (C5a) in RAW 264.7 macrophages (IC50 = 1.2 µM) and migration of isolated human granulocytes induced by fMLP (Cay-21495, IC50 = 1 µM). It decreases disease severity in a mouse model of collagen-induced arthritis when administered at doses of 3 and 10 mg/kg.Formal Name: 5-(2-amino-8-fluoro[1,2,4]triazolo[1,5-a]pyridin-6-yl)-N-(1,1-dimethylethyl)-3-pyridinesulfonamide. CAS Number: 1159824-67-5. Molecular Formula: C15H17FN6O2S. Formula Weight: 364.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 5 mg/ml, DMSO: 5 mg/ml, DMSO:PBS (pH 7.2)(1:5): 0.2 mg/ml. lambdamax: 218, 254, 292 nm. SMILES: O=S(C1=CC(C2=CN3C(C(F)=C2)=NC(N)=N3)=CN=C1)(NC(C)(C)C)=O.Cl. InChi Code: InChI=1S/C15H17FN6O2S.ClH/c1-15(2,3)21-25(23,24)11-4-9(6-18-7-11)10-5-12(16)13-19-14(17)20-22(13)8-10,/h4-8,21H,1-3H3,(H2,17,20),1H. InChi Key: GTDFAYLFDOPVIV-UHFFFAOYSA-N.