CAS: 1639417-53-0

Tenalisib (RP6530) (RP6530) is a potent and selective inhibitor of PI3Kδ and PI3Kγ(IC50 values of 25 and 33 nM, respectively.)

Tenalisib is a protein inhibitor that blocks the protein kinase activity of the m2 phenotype. It has been shown to be clinically effective in treating primary T-cell lymphomas, skin cancer, and cancers of the hematopoietic system. Tenalisib inhibits the growth of cancer cells by blocking the transcriptional regulation of genes that promote cell proliferation and survival. Tenalisib is also a chemotherapeutic treatment for human macrophages and hematopoietic cells. The drug has also shown anti-tumor effects in mice with skin cancer as well as antitumor effects on human myeloid-derived suppressor cells. Tenalisib is metabolized by cytochrome P450 enzymes, which are found in high concentrations in hepatic tissue.

Tenalisib