PI-103, Free Base (PI Kinase alpha Inhibitor 1; PIK-103, 371935-74-9), >99%

LC Laboratories' Product Number P-9099 - PI-103, Free Base (PI Kinase alpha Inhibitor 1; PIK-103, 371935-74-9), >99% - for research use only. PI-103 is a dual inhibitor of class IA phosphatidylinositide 3-kinase (PI3K) and mTOR. PI3K is a class of lipid kinases that phosphorylate phosphatidylinositol 4,5-bisphosphate (PIP2) to generate phosphatidylinositol 3,4,5-trisphosphate (PIP3). PIP3 activates Akt and mTOR, and plays important roles in cell growth and survival. This research compound is the free base form of PI-103. We also offer the HCl salt form; please see PI-103, Hydrochloride Salt, Cat. No. P-9088. PI-103 is a potent and selective PI3K inhibitor with low IC50 values against PI3K isoforms p110α (2 nM), p110β (3 nM), p110δ (3 nM), and p110γ (15 nM). PI-103 at 0.5 µM also inhibited TORC1 by 84% and demonstrated an IC50 of 14 nM against DNA-PK. PI-103 potently inhibited proliferation and invasion of a wide variety of human cancer cells in vitro and induced tumor growth delay in eight different human cancer xenograft models. PI-103 also demonstrated antiangiogenic potential. PI-103 had antitumor activity in two gefitinib-resistant (please see Cat. No. G-4408, Gefitinib, Free Base) non-small cell lung cancer cell lines, A549 and H460, possibly by simultaneously inhibiting p70s6k phosporylation and Akt phosphorylation due to mTOR inhibition. PI-103 was mainly cytostatic for human leukemic cell lines and induced cell cycle arrest in the G1 phase. In blast cells from AML patients, PI-103 inhibited leukemic proliferation and the clonogenicity of leukemic progenitors, and induced mitochondrial apoptosis. PI-103 inhibited the proliferation of glioma cells, possibly by its ability to inhibit both PI3 kinaseα and mTOR. It showed significant inhibitory activity in xenografted tumors with no observable toxicity. A combined treatment with arsenic disulfide and PI-103 synergistically killed non-acute promyelocytic leukemia cells and promoted their differentiation in vitro. PI-103 inhibited endothelial cell proliferation and survival in vitro and tumor growth in vivo possibly by blocking activation of both PI3K and mTOR in vGPCR-expressing endothelial cells. This PI-103 product is the free base form, whose CAS number is 371935-74-9. The CAS number of the hydrochloride salt form is 371935-79-4.

• Supplier: LC Laboratories
• Product #: P-9099
• Sku #: P-9099-5mg