Description
A dual inhibitor of PI3K and mTORC (IC50s = 9, 110, 43, 9, 160, and 910 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, mTORC1, and mTORC2, respectively); is selective for these kinases over VPS34 (IC50 = 9,100 nM) and a panel of 130 additional protein kinases at 1.5 µM but does inhibit DNAPK (IC50 = 150 nM); decreases EGF-induced PIP3 production in PC3 prostate cancer cells (IC50 = 290 nM); reduces Akt and S6RP phosphorylation in the same model (IC50s = 250 and 120 nM, respectively); inhibits proliferation and colony formation of PC3 cells (IC50s = 1,800 and 270 nM, respectively); reduces tumor growth and increases survival in a GBM-39 mouse xenograft model at 30 mg/kg twice per day either alone or in combination with temozolomide
Formal name: 2-amino-8-ethyl-4-methyl-6-(1H-pyrazol-3-yl)-pyrido[2,3-d]pyrimidin-7(8H)-one
Synonyms: SAR245409|XL765
Molecular weight: 270.3
CAS: 934493-76-2
Purity: ≥98%
Formulation: A crystalline solid
