tesevatinib

Tesevatinib (XL-647) is an oral, multi-targeted tyrosine kinase inhibitor with IC50 values ​​of 0.3, 16, 1.5, 8.7, and 1.4 nM for EGFR, ErbB2, KDR, Flt4, and EphB4.

Tesevatinib tosylate (XL-647 tosylate) is an orally administered epidermal growth factor receptor (EGFR) inhibitor that can cross the blood-brain barrier. It significantly reduces cell viability with IC50 values of 11 nM and 102 nM in GBM12 and GBM6, respectively. Additionally, Tesevatinib tosylate inhibits HER2 (IC50=16.1 nM), VEGFR2 (IC50=1.5 nM), and Src (IC50=10.3 nM), demonstrating antitumor activity by inhibiting tumor proliferation.