Shelf life (days): 1095.0
Formulation: A solid
Formal Name: 1-[7-[[2-[[4-(4-ethyl-1-piperazinyl)phenyl]amino]-4-pyridinyl]amino]-2,3-dihydro-1H-indol-1-yl]-ethanone
Purity: ≥98%
Formula Markup: C27H32N6O
Formula Weight: 456.58282
CAS Number: 2919575-27-0
Notes: UCL-TRO-1938 is an allosteric activator of PI3Kα.{65710} It binds to PI3Kα in a surface plasmon resonance (SPR) assay (Kd = 36 µM) and induces PI3Kα activation in a cell-free assay when used at concentrations of 25 and 50 µM, an effect that can be reversed by the PI3Kα inhibitor BYL719 (Item No. 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.