PP242

The mammalian target of rapamycin (mTOR) is a serine-threonine kinase that is central to two protein complexes, mTORC1 and mTORC2. These complexes are differentially regulated (e.g., only mTORC1 is sensitive to rapamycin) and regulate different pathways. PP242 is an inhibitor of the active site of mTOR kinase in both mTORC1 and mTORC2 (IC50 = 8 nM). It less effectively inhibits PKCalpha, PI3-kinase subunit p110gamma, JAK2, PKCbetaI, and PKCbetaII (IC50 = 49, 102, 110, 198, and 185, respectively). PP242 has been shown to cause the death of certain human and murine leukemia cells more potently than rapamycin and, in vivo, delays leukemia onset and augments the effects of tyrosine kinase inhibitors in suppressing leukemic expansion and extending survival.Formal Name: 2-[4-amino-1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]-1H-indol-5-ol. CAS Number: 1092351-67-1. Molecular Formula: C16H16N6O. Formula Weight: 308.3. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml, DMSO: 10 mg/ml, Ethanol: 0.5 mg/ml. lambdamax: 206, 262, 324 nm. SMILES: NC1=NC=NC2=C1C(C3=CC4=C(C=CC(O)=C4)N3)=NN2C(C)C. InChi Code: InChI=1S/C16H16N6O/c1-8(2)22-16-13(15(17)18-7-19-16)14(21-22)12-6-9-5-10(23)3-4-11(9)20-12/h3-8,20,23H,1-2H3,(H2,17,18,19). InChi Key: MFAQYJIYDMLAIM-UHFFFAOYSA-N.