Lapatinib(free base)
爱闪购- GW572016;GW-572016;GW 572016
货号: abs812860
货号-规格 | 货期 | 价格 | 数量 |
abs812860-25mg | 现货 | - + | |
abs812860-100mg | 现货 | - + |

产品描述 | ||
描述 | Lapatinib,以 Lapatinib Ditosylate的形式使用,是一种有效的EGFR和ErbB2抑制剂,在无细胞试验中IC50分别为10.2和9.8 nM。 | |
纯度 | >98% | |
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. | |
基本信息 | ||
别名 | GW572016;GW-572016;GW 572016 | |
外观 | Powder | |
可溶性/溶解性 | DMSO:100 mg/mL (172.09 mM) | |
生物活性 | ||
靶点 | ErbB2 ,EGFR ,ErbB4 | |
In vitro(体外研究) | Lapatinib weakly inhibits the activity of ErbB4 with IC50 of 367 nM, and displays >300-fold selectivity for EGFR and ErbB2 over other kinases such as c-Src, c-Raf, MEK, ERK, c-Fms, CDK1, CDK2, p38, Tie-2, and VEGFR2. Lapatinib significantly inhibits receptor autophosphorylation of EGFR and ErbB2 in a dose-dependent manner with IC50 of 170 nM and 80 nM, respectively in HN5 cells; as well as 210 nM and 60 nM, respectively in BT474 cells. Unlike OSI-774 and Iressa (ZD1839) which preferentially inhibit the growth of the EGFR-overexpressing cells, Lapatinib inhibits the growth of both EGFR- and ErbB2-overexpressing cells. Lapatinib displays higher inhibitory activity against EGFR- or ErbB2-overexpressing cells with IC50 of 0.09-0.21 μM, compared with cells expressing low levels of EGFR or ErbB2 with IC50 of 3-12 μM, and exhibits ~100-fold selectivity over the normal fibroblast cells. Lapatinib potently inhibits the outgrowth of EGFR-overexpressing HN5 and A-431 cells, as well as ErbB2-overexpressing BT474 and N87 cells, and significantly induces G1 arrest of HN5 cells and apoptosis of BT474 cells, which are associated with inhibition of AKT phosphorylation. | |
In vivo(体内研究) | Oral administration of Lapatinib (~100 mg/kg) twice daily significantly inhibits the growth of BT474 and HN5 xenografts in a dose-dependent manner. | |
参考文献 | ||
参考文献 | [1] Rusnak DW, et al. Mol Cancer Ther, 2001, 1(2), 85-94. | |
温馨提示:本产品仅作科研实验使用,不支持临床等研究 |
- 实验方法 实验条件
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