CP-673451

CP-673451 is a potent and highly selective small-molecule inhibitor of the platelet-derived growth factor receptor (PDGFR) tyrosine kinases, specifically targeting PDGFR-α and PDGFR-β. Developed by Pfizer, it acts as an ATP-competitive inhibitor that suppresses the phosphorylation of these receptors and their downstream signaling pathways, such as PI3K/Akt and MAPK. Preclinical research has demonstrated its efficacy in a wide range of conditions, including various cancers (NSCLC, glioblastoma, AML, and cholangiocarcinoma), where it often acts to reverse chemotherapy resistance or induce apoptosis. Additionally, it has shown potential in non-oncological areas such as sepsis, rheumatoid arthritis, and fibrotic diseases by modulating pericyte function and vascular reactivity. Beyond its primary PDGFR targets, research has also identified a novel mechanism involving the activation of cofilin via slingshot phosphatases, which allows CP-673451 to inhibit centrosome clustering in cancer cells.

Other names

CP 673451CP673451CP-673451