Recent reports indicate that breast tumor-stroma paracrine signaling between platelet-derived growth factor-B (PDGFB), a known oncogene, and the receptor tyrosine kinase platelet-derived growth factor receptor-beta (PDGFRβ) mediates primary tumor growth and metastatic spread to distant sites, specifically the brain. Following this discovery, the PDGFRβ specific tyrosine kinase inhibitor CP-868596 (crenolanib) was found to mitigate the growth of established brain metastases in mice. Although evidence indicates that crenolanib is able to diminish the growth of brain tumors, it is not confirmed experimentally that crenolanib is able to cross the blood-brain barrier and enter the brain. Previous research has used tandem HPLC-MS to quantitate crenolanib in human serum, but to date, no process has been reported for detecting crenolanib using HPLC-UV. Here we report the development of appropriate chromatographic conditions to detect and quantitate crenolanib and an internal standard, tyrphostin AG-1478, on an HPLC-UV system. Chromatographic parameters were determined for the quantitation of crenolanib in brain, lung, liver and serum of crenolanib-treated mice.

Development of HPLC-UV conditions for the detection of the small molecule platelet-derived growth factor receptor inhibitor crenolanib in mouse serum and tissues

ACS Spring 2022

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.