Tag: PI3K

COTI-2 is an Orally Available Mutant p53 Activator

TP53 (p53) is the single most frequently altered gene in human cancers, with mutations being present in approximately 50% of all invasive tumors. Besides, p53 is mutated in at least 80% of samples in some of the most difficult-to-treat cancers. Therefore, the mutant p53 protein is an important candidate...

PI-828 is a Dual PI3K and Casein Kinase 2 Inhibitor

PI3Ks (phosphatidylinositol 3-kinases) are lipid kinases responsible for the phosphorylation of phosphatidylinositols on the D3 position of their inositol ring. Specifically, The PI3Ks regulate cellular signaling networks. The processes involved these linked to the survival, growth, proliferation, metabolism and specialized differentiated functions of cells. Besides, The subversion of this...

Alpelisib is a Selective and Orally Active PI3Kα Inhibitor for Metastatic Breast Cancer

Phosphatidylinositol-3-kinases (PI3Ks) are a family of important lipid kinases. PI3Ks are important in controlling the signaling pathways involved in cell proliferation, motility, cell death, and cell invasion. Moreover, PI3Ks control and deliver cellular signals in the PI3K/Akt/mTOR pathway by phosphorylating phosphatidylinositol 4,5-bisphosphate (PIP2) to phosphatidylinositol 3,4,5-trisphosphate (PIP3) on the...

CGS 15943 is an Orally Active Adenosine Receptor Antagonist

Hepatocellular carcinoma (HCC) is primary liver cancer and the third most common cause of cancer mortality worldwide. CGS 15943 blocks proliferation in hepatocellular carcinoma (HCC) and pancreatic cancer adenocarcinoma (PDAC) cell lines by inhibiting the PI3K/Akt pathway. Researchers test the adenosine A2 receptor antagonist CGS 15943 for cerebroprotective activity in...

KU-0060648 is a Dual PI3K and DNA-PK Inhibitor

DNA double-strand breaks (DSBs) are the principal cytotoxic lesions induced by topoisomerase II poisons. And DSB inhibitors are widely applied in the treatment of a variety of human solid malignancies and leukemia. Cells defective in DSB repair by virtue of the inactivation of a component of the NHEJ pathway...

SAR-260301 is an Orally Active PI3Kβ Inhibitor for Melanoma Treatment

The phosphoinositide 3-kinase (PI3K) pathway activation plays a major role in cancer. The PI3K-AKT pathway is one of the most important signaling networks in cancer. Activation of PI3K-AKT pathway plays a significant role in melanoma. PI3K family divides into three classes (I, II, and III). In melanoma, PI3K pathway...

SPP-86 is a Potent and Selective Inhibitor of RET Tyrosine Kinase

The REarranged during Transfection (RET) receptor tyrosine kinase (RTK) regulates key aspects of cellular proliferation and survival by regulating the activity of the mitogen- activated protein kinase (MAPK) and PI3K/Akt signaling pathways. The RET tyrosine kinase receptor has emerged as a target in thyroid and endocrine resistant breast cancer....