XL-647 |CAS:781613-23-8 Probechem Biochemicals

Chemical Structure : XL-647

CAS No.: 781613-23-8

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XL-647 (Tesevatinib; EXEL-7647; KD-019)

货号: 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.

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5 mg	￥2180	In stock
10 mg	￥3580	In stock
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生物&药学活性

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.

物理化学性质&存储条件

分子量	491.39
分子式	C24H25Cl2FN4O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	DMSO: ≥ 30 mg/mL
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]-

参考文献

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.

XL-647 (Tesevatinib; EXEL-7647; KD-019)

生物&药学活性

物理化学性质&存储条件

参考文献

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XL-647 (Tesevatinib; EXEL-7647; KD-019)

生物&药学活性

物理化学性质&存储条件

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