UCL-TRO-1938

UCL-TRO-1938 is an allosteric activator of PI3Kalpha. It binds to PI3Kalpha in a surface plasmon resonance (SPR) assay (Kd = 36 µM) and induces PI3Kalpha activation in a cell-free assay when used at concentrations of 25 and 50 µM, an effect that can be reversed by the PI3Kalpha inhibitor BYL719 (Cay-16986). UCL-TRO-1938 increases PtdIns-(3,4,5)-P3 and phosphorylated Akt levels in mouse embryonic fibroblasts (MEFs, EC50s = 5 and 2-4 µM, respectively). Ex vivo, UCL-TRO-1938 increases tissue survival and decreases infarct size in perfused rat hearts. In vivo, UCL-TRO-1938 (10 mg/kg) reduces infarct size in a mouse model of ischemia-reperfusion injury induced by left anterior descending (LAD) coronary artery occlusion. It also increases the number of motor neurons and innervation of neuromuscular junctions in a rat model of sciatic nerve crush injury.Formal Name: 1-[7-[[2-[[4-(4-ethyl-1-piperazinyl)phenyl]amino]-4-pyridinyl]amino]-2,3-dihydro-1H-indol-1-yl]-ethanone. CAS Number: 2919575-27-0. Molecular Formula: C27H32N6O. Formula Weight: 456.6. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 1 mg/mL, DMSO: 1 mg/mL, Ethanol: Slightly Soluble, PBS (pH 7.2): Slightly soluble. lambdamax: 297 nm. SMILES: CCN(CC1)CCN1C(C=C2)=CC=C2NC3=CC(NC4=CC=CC5=C4N(C(C)=O)CC5)=CC=N3. InChi Code: InChI=1S/C27H32N6O/c1-3-31-15-17-32(18-16-31)24-9-7-22(8-10-24)30-26-19-23(11-13-28-26)29-25-6-4-5-21-12-14-33(20(2)34)27(21)25/h4-11,13,19H,3,12,14-18H2,1-2H3,(H2,28,29,30). InChi Key: RPOHONUDGBSZDK-UHFFFAOYSA-N.