Description: Pyrotinib Racemate is the racemate of Pyrotinib (SHR-1258) which is a selective and orally bioavailable, dual kinase inhibitor of EGFR/HER2 [(epidermal growth factor receptor, or HER-1) and the human epidermal growth factor receptor 2 (ErbB2 or HER-2)] with IC50s of 13 and 38 nM, respectively. It has potential antineoplastic activity. After oral administration, pyrotinib binds to and inhibits both EGFR and HER2, which may result in the inhibition of tumor growth and angiogenesis, and tumor regression in EGFR/HER2-expressing tumor cells. EGFR and HER2 are receptor tyrosine kinases that are upregulated in various tumor cell types and play major roles in tumor cell proliferation and tumor vascularization.

References: Discovery and development of Pyrotinib: A novel irreversible EGFR/HER2 dual tyrosine kinase inhibitor with favorable safety profiles for the treatment of breast cancer. Eur J Pharm Sci. 2017 Jan 21. pii: S0928-0987(17)30043-X.; Metabolic characterization of pyrotinib in humans by ultra-performance liquid chromatography/quadrupole time-of-flight mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci. 2016 Oct 15;1033-1034:117-27.

Related CAS #:1269662-73-8 (free base) 1397922-61-0 (maleate) 1246089-97-3 (racemate)