PF-04691502

PF-04691502 is an inhibitor of PI3Kalpha, -beta, -delta, and -gamma and mammalian target of rapamycin (mTOR, Kis = 1.8, 2.1, 1.6, 1.9, and 16 nM, respectively, for the human enzymes). It decreases the proliferation of BT-20 breast cancer, SKOV3 ovarian cancer, and U87MG glioblastoma cells (IC50s = 313, 188, and 179 nM, respectively). PF-04691502 (2.5 and 5 µM) inhibits capillary tube formation by, and migration of, human umbilical vein endothelial cells (HUVECs). It induces cell cycle arrest at the G1 phase in U87MG cells when used at concentrations of 500 and 1,000 nM. PF-04691502 (10 mg/kg per day) decreases tumor volume in NCI H1650 and H1975 non-small cell lung cancer (NSCLC) mouse xenograft models.Formal Name: 2-amino-8-[trans-4-(2-hydroxyethoxy)cyclohexyl]-6-(6-methoxy-3-pyridinyl)-4-methyl-pyrido[2,3-d]pyrimidin-7(8H)-one. CAS Number: 1013101-36-4. Synonyms: HNC-VP-L, PF-502. Molecular Formula: C22H27N5O4. Formula Weight: 425.5. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml, DMSO: 20 mg/ml, Ethanol: 1 mg/ml. lambdamax: 222, 302, 353 nm. SMILES: O=C1N([C@H]2CC[C@H](OCCO)CC2)C3=NC(N)=NC(C)=C3C=C1C4=CN=C(OC)C=C4. InChi Code: InChI=1S/C22H27N5O4/c1-13-17-11-18(14-3-8-19(30-2)24-12-14)21(29)27(20(17)26-22(23)25-13)15-4-6-16(7-5-15)31-10-9-28/h3,8,11-12,15-16,28H,4-7,9-10H2,1-2H3,(H2,23,25,26)/t15-,16-. InChi Key: XDLYKKIQACFMJG-WKILWMFISA-N.