LQZ-7I is a survivin inhibitor through inhibition of survivin dimerization. It effectively inhibited xenograft tumor growth and induced survivin loss in tumor when given orally.
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产品名称 | Survivin ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
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Sepantronium bromide |
+++
Survivin, IC50: 0.54 nM |
99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | Survivin, a homodimeric member of the inhibitor of apoptosis protein (IAP) family, is required for cancer cell survival and overexpressed in almost all solid tumors. LQZ-7I is a survivin inhibitor. It has improved cytotoxicity with an IC50 of 3.1 µM against C4-2 cells and 4.8 µM against PC-3 cells. LQZ-7I significantly decreased the SEAP (secreted alkaline phosphatase) reporter expression. Furthermore, it significantly inhibited survivin dimerization. In C4-2 and PC-3 cells, LQZ-7I treatment reduced the expression of survivin in a time-dependent manner. Specifically, LQZ-7I treatment reduced the half-life of survivin from 2.2 and 2.3 hrs to 50 and 25 minutes in C4-2 and PC-3 cells, respectively. Moreover, LQZ-7I induced cleavage of caspase 3 in a dose dependent manner in both cell lines. 3 µM LQZ-7I induced ~48% and ~39% apoptosis in C4-2 and PC-3 cells, respectively. In vivo, LQZ-7I treatment at 100 mg/kg significantly suppressed tumor growth without any notable adverse effect on the mice as indicated by lacking changes in body weight[1]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.87mL 0.57mL 0.29mL |
14.35mL 2.87mL 1.44mL |
28.71mL 5.74mL 2.87mL |
CAS号 | 195822-23-2 |
分子式 | C20H14F2N4 |
分子量 | 348.349 |
别名 | |
运输 | 蓝冰 |
存储条件 |
粉末 Keep in dark place,Inert atmosphere,Room temperature 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 120 mg/mL(344.48 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |