产品信息
抗原名称
MEK
商品描述
Selumetinib (AZD6244)是一种有效,高选择性的MEK1抑制剂,无细胞试验中IC50为14 nM,也抑制ERK1/2磷酸化,IC50为10 nM,对p38α, MKK6, EGFR, ErbB2, ERK2, B-Raf等没有抑制作用。
分子量
457.68
纯度
>98%
可溶性
DMSO : 10 mg/mL (21.85 mM; Need ultrasonic)
外观
White to off white powder
In vitro(体外研究)
Selumetinib (AZD6244) causes a time- and dose-dependent reduction in DNA synthesis and cell viability in primary, induces growth arrest and apoptosis associated with the inactivation of ERK in primary 2-1318 cells.
In vivo(体内研究)
Selumetinib (AZD6244, 50 and 100 mg/kg, p.o.) decreases the growth rate of 4-1318 xenografts in a dose-dependent manner; AZD6244 when given at the dose of 50 mg/kg also significantly suppresses the growth of the 5-1318, 2-1318, 26-1004, and 29-1104 xenografts. Selumetinib (ARRY-142886, 10, 25, 50, or 100 mg/kg, p.o.) is capable of inhibiting both ERK1/2 phosphorylation and growth of HT-29 xenograft tumors in nude mice. Tumor regressions are also seen in a BxPC3 xenograft model.
背景
别名
司美替尼
分子式
C17H15BrClFN4O3
CAS号
606143-52-6
制备和贮存
保存方式
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
参考图片
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