Apitolisib is an Orally Active Class I PI3K and mTORC1/2 Inhibitor
Activation of the pathway occurs following activating point mutations or amplification of the PIK3CA gene encoding the p110a PI3K isoform. Oncogenes such as PI3K, AKT, epidermal growth factor receptor (EGFR), and human epithelial growth factor receptor 2 (HER2) stimulate proliferation, growth, and survival by activating mTOR kinase. The mTOR...
PQR530 is an Orally Active and Brain-Penetrant Dual PI3K, mTORC1/2 Inhibitor
Several brain disorders, such as epilepsy, found dysregulation of the PI3K/Akt/mTOR pathway. The PI3K-AKT/mTOR pathway is a central player of intracellular signaling, regulating neuronal survival, growth, and plasticity. Aberrant activation of this signaling pathway drives the progression of malignant tumors. The mutation of growth factor receptors, PI3K, loss of...
JR-AB2-011, a Potential Inhibitor of mTORC2 Activity in Glioblastoma Multiforme (GBM)
Glioblastoma multiforme (GBM) are highly malignant and invasive tumors. It not only can prevent total surgical resection, but also render these neoplasms refractory to cheJR-AB2-011 is a selective mTORC2 inhibitor with an IC50 value of 0.36 μM. JR-AB2-011 inhibits mTORC2 activity by blocking Rictor-mTOR association (Ki: 0.19 μM). JR-AB2-011...