PI-103 is a potent, cell-permeable, ATP-competitive PI3K family members inhibitor with IC50 of 2, 8, 20, 26, 48, 83, 88, 150 nM for DNA-PK, p110α, mTORC1, PI3-KC2β, p110δ, mTORC2, p110β and p110γ, respectively. It shows little activity against a wide array of protein kinases at 10 mM [1]. 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 [2].In blast cells, PI-103 suppresses leukemic proliferation, the clonogenicity of leukemic progenitors and induced mitochondrial apoptosis, especially in the compartment containing leukemic stem cells [3].
Chemical Properties
Cas No.: 371935-74-9
M. Wt.: 348.36
Formula: C19H16N4O3
Purity: >99%
Synonym: PI 103
Chemical Name: 3-(4-(4-Morpholinyl)pyrido[3’,2’:4,5]furo[3,2-d]pyrimidin-2-yl)phenol
Appearance: Off white to white solid
Solubility: Soluble in DMSO at 10 mg/ml, slightly soluble in water.
Storage: Store powder at -20 ºC for the stability up to two years, keep desiccated.