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Tesevatinib (XL-647) is an orally available, multi-target tyrosine kinase inhibitor; inhibits EGFR, ErbB2, KDR, Flt4 and EphB4 kinase with IC50s of 0.3, 16, 1.5, 8.7, and 1.4 nM.

Tesevatinib (XL-647) potently inhibits the EGF/ErbB2, VEGF, and ephrin RTK families. Tesevatinib (XL-647) is a reversible and ATP competitive inhibitor. Tesevatinib (XL-647) was inactive against a panel of 10 tyrosine kinases (including the insulin and the insulin-like growth factor-1 receptor) and 55 serine-threonine kinases (including cyclin-dependent kinases, stress-activated protein kinases, and protein kinase C isoforms). Tesevatinib (XL-647) inhibits cellular proliferation and EGFR pathway activation in the erlotinib-resistant H1975 cell line that harbors a double mutation (L858R and T790M) in the EGFR gene. In A431 cells, Tesevatinib (XL-647) reduces cell viability with IC50 values of 13 nM[1].

Tesevatinib (XL-647) shows potent and long-lived inhibition of the WT EGFR in vivo. Tesevatinib (XL-647) substantially inhibits the growth of H1975 xenograft tumors and reduces both tumor EGFR signaling and tumor vessel density[1].

[1]. Gendreau SB, et al. Inhibition of the T790M gatekeeper mutant of the epidermal growth factor receptor by EXEL-7647. Clin Cancer Res. 2007 Jun 15;13(12):3713-23.

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