Size | Price | Stock |
---|---|---|
1mg | $142 | In-stock |
5mg | $300 | In-stock |
10mg | $580 | In-stock |
50 mg | Get quote | |
100 mg | Get quote | |
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Cat. No. : | HY-13314 |
M.Wt: | 491.39 |
Formula: | C24H25Cl2FN4O2 |
Purity: | >98 % |
Solubility: | DMSO : 100 mg/mL (203.50 mM; Need ultrasonic) |
Tesevatinib (XL-647; EXEL-7647; KD-019) 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. IC50 & Target:IC50: 0.3 nM (EGFR), 16 nM (EGFR), 1.5 nM (EGFR), 8.7 nM (EGFR), 1.4 nM (EGFR)[1] In Vitro: 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]. In Vivo: 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].
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