Formulation: A crystalline solid
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
Purity: ≥95%
Formula Markup: C22H27N5O4
Formula Weight: 425,5
Shelf life (days): 1460
CAS Number: 1013101-36-4
Notes: PF-04691502 is an inhibitor of PI3Kα, -β, -δ, and -γ and mammalian target of rapamycin (mTOR; Kis = 1.8, 2.1, 1.6, 1.9, and 16 nM, respectively, for the human enzymes).{22526} 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).{69429} It induces cell cycle arrest at the G1 phase in U87MG cells when used at concentrations of 500 and 1,000 nM.{22526} PF-04691502 (10 mg/kg per day) decreases tumor volume in NCI H1650 and H1975 non-small cell lung cancer (NSCLC) mouse xenograft models.