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LQZ-7I

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Chemical Structure| 195822-23-2 同义名 : -
CAS号 : 195822-23-2
货号 : A1275711
分子式 : C20H14F2N4
纯度 : 99%+
分子量 : 348.349
MDL号 : MFCD00607076
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:
生物活性
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].
实验方案
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

参考文献

[1]Peery R, Kyei-Baffour K, Dong Z, et al. Synthesis and Identification of a Novel Lead Targeting Survivin Dimerization for Proteasome-Dependent Degradation. J Med Chem. 2020;63(13):7243-7251