中文名称: | NSC319726 | ||||
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英文名称: | NSC319726 | ||||
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 ZMC1 | ||||
CAS No: | 71555-25-4 | 分子式: | C11H14N4S | 分子量: | 234.32 |
CAS No: | 71555-25-4 | ||||
分子式: | C11H14N4S | ||||
分子量: | 234.32 | ||||
EINEC: | 319726 | ||||
EINEC: | 319726 |
基本信息
产品编号:N10635 |
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产品名称:NSC319726 |
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CAS: |
71555-25-4 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式: |
溶于液体 |
-80℃ |
六个月 |
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分子量 |
234.32 |
-20℃ |
一个月 |
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化学名: |
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Solubility (25°C) |
体外 |
DMSO |
32mg/mL (67.51mM) |
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Ethanol |
Insoluble |
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Water |
Insoluble |
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体内(现配现用) |
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<1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
4.2677mL |
21.3383mL |
42.6767mL |
5mM |
0.8535mL |
4.2677mL |
8.5353mL |
10mM |
0.4268mL |
2.1338mL |
4.2677mL |
50mM |
0.0854mL |
0.4268mL |
0.8535mL |
生物活性
产品描述 |
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。 |
靶点/IC50 |
IC50:8nM (mutant p53R175 reactivator) |
体外研究 |
For NSC319726, the effect was even greater as the IC50 for the 175 mutant was 8nM 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. |
体内研究 |
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 0.1mg/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. |
推荐实验方法(仅供参考)
激酶实验: |
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MTS |
TOV112D细胞按每孔5,000个细胞培养在96孔板中,孔中为100ml培养基,在实验第二天,达到50%-60%汇合,使用连续稀释的化合物处理。温育3天后,使用MTS 试剂和Victor酶标仪测量生长。 |
细胞实验: |
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细胞系 |
p53突变的MEF |
浓度 |
~10μM |
处理时间 |
3天 |
方法 |
进行细胞活力检测。细胞按每孔5×104个细胞培养在12孔板中,孔中为1ml培养基,在实验第二天,达到50%-60%汇合,使用连续稀释的化合物处理。温育3天后,使用Guava ViaCount 试剂和Guava PCA仪器测量生长。 |
动物实验: |
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动物模型 |
p53+/+, p53-/-和 p53 R172H 基因敲入小鼠 |
剂量 |
每天5-10mg/kg,长达7天 |
给药处理 |
腹腔注射 |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )