NSC319726 (Synonyms: ZMC1)
目录号: PL07015 纯度: ≥98%
CAS No. :71555-25-4
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中文名称
NSC319726
中文别名
1-吖丁啶硫代羧酸[1-(2-吡啶基)亚乙基]酰肼;NSC319726 抑制剂;p53(R175)突变型活化剂NSC319726;N'-(1-(吡啶-2-基)亚乙基)氮杂环丁烷-1-硫代碳酰肼
英文名称
NSC319726
英文别名
NSC 319726;Azetidinecarbothioic acid, [1-(2-pyridinyl)ethylidene] hydrazide;NSC-319726;1-AZETIDINESULFONAMIDE;32371-EP2301933A1;AG-G-46200;azetidine-1-sulphonamide;Azetidine-1-thiocarboxylic acid 2-[1-(2-pyridinyl)ethylidene]hydrazide;Azetidine-1-thiocarboxylic acid 2-[1-(2-pyridyl)ethylidene]hydrazide;CTK5C2671;KB-64890;QC-4196;SureCN1486989;1-Azetidinecarbothioic acid 2-[1-(2-pyridinyl)ethylidene]hydrazide;1-Azetidinecarbothioic acid;ZMC1;NSC319726;N'-(1-(Pyridin-2-yl)ethylidene)azetidine-1-carbothiohydrazide;(E)-N'-(1-(pyridin-2-yl)ethylidene)azetidine-1-carbothiohydrazide;MLS002703052;AZETIDINE CARBOTHIOIC ACID, [1-(2-PYRIDINYL)ETHYLIDENE]HYDRAZIDE;1-Azetidinecarbothioic acid [1-(2-pyridinyl)ethylidene]hydrazide;2597AH;s7149;SB19405;CID 5351307;CS-981;1-Azetidinecarbothioic acid, 2-[1-(2-pyridinyl)ethylidene]hydrazide;1-Azetidinecarbothioic acid [1-(2-pyridinyl)ethylidene]hydrazide NSC319726;(E)-N'-(1-(Pyridin-2-yl)ethylidene)azetidine-1-carbothiohydrazide
Cas No.
71555-25-4
分子式
C11H14N4S
分子量
234.32
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
NSC319726 (ZMC1) 是突变型p53R175再活化剂,能抑制表达p53R175的成纤维细胞增殖,IC50值为8nM,对野生型p53细胞无抑制作用。
生物活性
NSC319726 (ZMC1) is a mutant p53R175 reactivator; inhibits growth of fibroblasts expressing the p53R175 mutation (IC50 = 8 nM); shows no inhibition for p53 wild-type cells.
性状
Solid
IC50 & Target[1][2]
IC50: 8 nM (mutant p53R175 reactivator)
体外研究(In Vitro)
For NSC319726, the effect was even greater as the IC50 for the 175 mutant was 8 nM while the IC50 of the WT was not reached. NSC319726 did not induce WT p53 protein levels or transcriptional activity as common cytotoxic agents such as etoposide do in vitro. NSC319726 exhibited a much higher sensitivity for the MEF-p53R172H/R172H cell line as compared to the p53+/+ and p53-/- controls. NSC319726 treatment of a MEF cell line derived from p53R172H/R172H mice resulted in aloss of PAB240 immunoflouresence staining. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
At a dose of 1mg/kg, tumor growth of the H460 (p53+/+) and MDAMB468 (p53R273W) xenografts was not inhibited relative to the vehicle control whereas tumor growth was significantly inhibited in the TOV112D (p53R175H) xenografts. When we lowered the dose ten-fold to 0.1 mg/kg in the TOV112D mice, we observed only a small difference in tumor growth inhibition demonstrating both a dosage effect of the drug and a larger therapeutic window.Taken together, these findings provide in vivo evidence for allele specific p53 mutant reactivation. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Yu X, et al. Allele-specific p53 mutant reactivation. Cancer Cell. 2012 May 15;21(5):614-25.
溶解度数据
In Vitro: DMSO : 31.25 mg/mL (133.36 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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