|N'-(1-(吡啶-2-基)亚乙基)氮杂环丁烷-1-硫代碳酰肼|CsnPharm

CAS No.: 71555-25-4

NSC319726 Catalog No. CSN16560

Synonyms: ZMC1

NSC319726 is a mutant p53R175 reactivator inhibiting growth of fibroblasts expressing the p53R175 mutation (IC50 = 8 nM) and showing no inhibition for p53 wild-type cells.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述NSC319726 is a p53^R175 mutant reactivator, which can restores WT structure and function to the p53^R175 mutant. Cell lines with p53^R175 mutant, including MEF cell lines from p53^R172H/R172H mice, HOP92 (R175L), TOV112D (R175H), AU565 (R175H), SK-BR-3 (R175H), exhibited more sensitivity to cell lines with p53 WT, p53^R248, or p53^R273. NSC319726 could induce a ''WT-like'' conformational change in the p53-175 mutant protein and reactivate its function as p53 WT, as treatment with 1μM NSC319726 led a significant decrease of p53 protein level in TOV112D cells (R175 mutant) within 8h and restored p53 protein level to normal level at 12h later, which can be eliminated by Mdm2 antagonist Nutlin-3. Administration of NSC319726 at dose of 5 or 10mg/kg, i.p., for 7 days, selectively killed p53^R172H knockin mice with extensive apoptosis. Daily intravenous administration of NSC319726 at 1 or 0.1mg/kg selectively inhibited xenograft tumor growth in a 175-allele-specific mutant p53-dependent manner.
作用机制NSC319726 induced a ‘‘WT-like’’ conformational change in the p53-175 mutant protein. This activity depends upon the zinc ion chelating properties of the compound as well as redox changes.^[1]
动物研究
剂量
Mice: 5 mg/kg, 10 mg/kg^[1] (i.p.); 0.1 mg/kg, 1 mg/kg^[1] (i.v.)

给药途径
i.p., i.v.
参考文献

动物研究
剂量	Mice: 5 mg/kg, 10 mg/kg^[1] (i.p.); 0.1 mg/kg, 1 mg/kg^[1] (i.v.)
给药途径	i.p., i.v.

[1] Yu X, Vazquez A, et al. Allele-specific p53 mutant reactivation. Cancer Cell. 2012 May 15;21(5):614-25.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 4.2677 mL
- 21.3383 mL
- 42.6766 mL
- 5 mM
- 0.8535 mL
- 4.2677 mL
- 8.5353 mL
- 10 mM
- 0.4268 mL
- 2.1338 mL
- 4.2677 mL

技术信息

CAS号

71555-25-4

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C11H14N4S

运输

蓝冰

分子量

234.32

别名

ZMC1

溶解度

DMSO	57.0 mg/mL (243.3 mM) warming
Water	insoluble

动物实验配方

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