Catalog No.: PC-43486Not For Human Use, Lab Use Only.
XL-647 (Tesevatinib, EXEL-7647, KD-019) is a novel spectrum-selective kinase inhibitor that potently inhibits the EGFR, ErbB2, KDR and EphB4 with IC50 of 0.3, 16, 1.5 and 1.4 nM, respectively.
XL-647 (Tesevatinib, EXEL-7647, KD-019) is a novel spectrum-selective kinase inhibitor that potently inhibits the EGFR, ErbB2, KDR and EphB4 with IC50 of 0.3, 16, 1.5 and 1.4 nM, respectively.
XL-647 shows no inhibition on IGF1R and InsR, also is inactive against a panel of 55 serine-threonine kinases, including CDKs, stress-activated protein kinases, and PKC isoform.
XL-647 inhibits WT and mutant EGFR phosphorylation in cells with IC50 of 5 and 74 nM, inhibits mutant EGFR resistant to gefitinib and erlotinib, inhibits cellular proliferation and EGFR pathway activation in the erlotinib-resistant H1975 cell line that harbors double mutation L858R/T790M.
XL-647 inhibits H1975 xenograft tumors and reduces both tumor EGFR signaling and tumor vessel density in vivo.
