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Chemical Structure : XL-647
CAS No.: 781613-23-8
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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 2 mg | $128 | In stock | |
| 5 mg | $218 | In stock | |
| 10 mg | $358 | In stock | |
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| 50 mg | Get quote | ||
| 100 mg | Get quote |
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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.
| M.Wt | 491.39 | |
| Formula | C24H25Cl2FN4O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
DMSO: ≥ 30 mg/mL |
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| Chemical Name/SMILES |
4-Quinazolinamine, N-(3,4-dichloro-2-fluorophenyl)-6-methoxy-7-[[(3aα,5β,6aα)-octahydro-2-methylcyclopenta[c]pyrrol-5-yl]methoxy]- |
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1. Pietanza MC, et al. J Thorac Oncol. 2012 Jan;7(1):219-26.
2. Gendreau SB, et al. Clin Cancer Res. 2007 Jun 15;13(12):3713-23.
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