PI-103

The phosphatidylinositol 3-kinases (PI3K) family of enzymes is comprised of 15 members that are divided into 3 classes according to their structure, substrate specificity, and mode of regulation. PI-103 is a potent, cell-permeable, ATP-competitive inhibitor of phosphatidylinositol 3-kinase (PI3K) family members with selectivity toward DNA-PK, PI3K (p110alpha), and mTOR. The IC50 values are 2, 8, 20, 26, 48, 83, 88, 150 nM for DNA-PK, p110alpha, mTORC1, PI3-KC2beta, p110delta, mTORC2, p110beta, and p110gamma, respectively. PI-103 exhibits antiproliferative activity against a panel of glioma cell lines in vitro at a concentration of 0.5 µM. It also inhibits growth of established human glioma tumor xenografts in vivo with no observable toxicity.Formal Name: 3-[4-(4-morpholinyl)pyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl]-phenol. CAS Number: 371935-74-9. Molecular Formula: C19H16N4O3. Formula Weight: 348.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 15 mg/ml, DMSO:PBS (pH 7.2) (1:2): 0.25 mg/ml. lambdamax: 221, 258, 285, 292 nm. SMILES: Oc1cccc(c1)c1nc(N2CCOCC2)c2oc3ncccc3c2n1. InChi Code: InChI=1S/C19H16N4O3/c24-13-4-1-3-12(11-13)17-21-15-14-5-2-6-20-19(14)26-16(15)18(22-17)23-7-9-25-10-8-23/h1-6,11,24H,7-10H2. InChi Key: TUVCWJQQGGETHL-UHFFFAOYSA-N.