XL-647CAS号: 781613-23-8分子式: C24H25Cl2FN4O2分子量: 491.39描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
产品描述 | |
描述 |
XL647 is a novel spectrum-selective kinase inhibitor for EGFR, ErbB2, KDR, Flt-4 and EphB4 with IC50 of 0.3 nM, 16 nM, 1.5 nM, 8.7 nM and 1.4 nM, respectively. |
纯度 |
>98%
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储存/保存方法 |
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
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基本信息 | |
别名 |
EXEL-7647,xl-647,xl 647
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外观 |
Powder
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可溶性/溶解性 |
DMSO : ≥ 30 mg/mL (61.05 mM)
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生物活性 | |
靶点 |
Ephrin Receptor
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In vitro(体外研究) |
XL-647 potently inhibits the EGF/ErbB2, VEGF, and ephrin RTK families. XL-647 is a reversible and ATP competitive inhibitor. 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). 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, XL-647 reduces cell viability with IC50 values of 13 nM.
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In vivo(体内研究) |
XL-647 shows potent and long-lived inhibition of the WT EGFR in vivo. XL-647 substantially inhibits the growth of H1975 xenograft tumors and reduces both tumor EGFR signaling and tumor vessel density.
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分子结构图