Selleck Chemicals is one of the worlds leading suppliers of high-performance inhibitors and reference compounds for non-clinical research fields focusing on signaling pathways such as MAPK, PI3K/Akt, JAK/STAT and apoptosis.
PI3K/Akt/mTOR dependent signaling pathway contributes to many cellular processes such as cell growth, proliferation, differentiation, motility, survival and intracellular trafficking, which might be involved in oncogenesis under certain situations. When a growth factor or ligand such as human epidermal growth factor receptor 2 (HER2), epidermal growth factor receptor(EGFR), insulin-like growth factor receptor and vascular endothelial growth factor receptor, binds to the tyrosine kinase receptors (RTK), the PI3K is activated by G protein-coupled receptors. Activated PI3K generates phosphatidylinositol-3,4,5-triphosphate, which recruits PDK1 and Akt serine/threonine kinase at the plasma membrane. This results in the activation of Akt which activates multiple downstream targets, including the mTOR pathway.
In the following work, isoform-selective PI3K inhibitors were reported. PI 103 is able to inhibit both p110a and mTOR in glioma cells . A Phase I study showed that a selective inhibitor of p110δ called CAL 101 could be helpful with the treatment of hematologic malignancies in patients 
Akt is another potential target for the therapy of cancer for the reason that Akt is one of the most important downstream molecule of PI3Ks. There are three isoforms of Akt: Akt1, Akt2 and Akt3. A dual inhibitor of Akt1 and Akt2 named Akti 1/2 showed potent anti tumor activity in tumor xenograft models. MK2206, the analog of Akti 1/2, is now in the Phase I clinical trial for the treatment of locally advanced or metastatic solid tumors and a Phase II study in advanced hepatocellular carcinoma [5;6].
As one of the key components of PI3K pathway, mTOR exists in two different complexes, mTORC1 and mTORC2. Rapamycin or sirolimus (Rapamune®; Wyeth, NJ, USA), which mainly inhibits the activity of mTORC1, recently presented antitumor effects [7;8].
Under some conditions, inhibiting more than one target of PI3K pathway might lead to better effect. BEZ235, dual PI3K/mTOR inhibitor, inhibits Class I PI3K isoforms and mTOR kinase activity by binding to the ATP-binding pocket of PI3K. It has strong anti-proliferative effect on tumor xenografts and is now under Phase I/II clinical trials for breast cancer and endometrial cancer .
A unique collection of 7 inhibitors for a range of PI3K subtypes supplied as lyophilized powder
A unique collection of 9 inhibitors for the study of PI3K/Akt/mTOR signaling pathway supplied as lyophilized powder