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PRIMA-1

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产品编号 T6954Cas号 5608-24-2
别名 PRIMA 1, NSC-281668, 2,2-Bis(hydroxymethyl)-3-quinuclidinone

PRIMA-1 (NSC-281668) 是一种突变型 p53复活剂,可恢复 TP53 突变型甲状腺癌细胞对组蛋白甲基化抑制剂 3-Deazaneplanocin A 的敏感性。

PRIMA-1
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PRIMA-1

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产品编号 T6954 别名 PRIMA 1, NSC-281668, 2,2-Bis(hydroxymethyl)-3-quinuclidinoneCas号 5608-24-2

PRIMA-1 (NSC-281668) 是一种突变型 p53复活剂,可恢复 TP53 突变型甲状腺癌细胞对组蛋白甲基化抑制剂 3-Deazaneplanocin A 的敏感性。

规格价格库存数量
1 mg¥ 161现货
5 mg¥ 369现货
10 mg¥ 533现货
25 mg¥ 987现货
50 mg¥ 1,650现货
100 mg¥ 2,560现货
200 mg¥ 3,790现货
500 mg¥ 5,900现货
1 mL x 10 mM (in DMSO)¥ 397现货
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产品介绍

生物活性
产品描述
PRIMA-1 (NSC-281668) is a mutant p53 reactivator. It induces apoptosis and inhibits growth of human tumors with mutant p53.
体外活性
PRIMA-1 is converted to compounds that form adducts with thiols in mutant p53. Modification of thiol groups in mutant p53 by PRIMA-1 conversion products is sufficient to restore its tumor suppressor activity.[2]. PRIMA-1 inhibits the growth of pancreatic cancer cell lines and induces cell cycle arrest and decreases DNA synthesis. It selectively induces apoptosis and cell death in mutant p53-expressing pancreatic cancer cells and also leads to activation of p53-dependent apoptotic pathways. PRIMA-1 enhances the cytotoxicity of chemotherapeutic agents active against mutant p53 pancreatic cancer cells[1]. PRIMA-1 has antileukemic properties in acute promyelocytic leukemia-derived NB4 cells. PRIMA-1-triggered apoptosis is in a dose-dependent and time-dependent manner as indicated by the MTT assay and annexin-V staining. Apoptosis induction by PRIMA-1 is associated with caspase-9, caspase-7 activation and PARP cleavage. PRIMA-1 does not show any significant apoptotic effect in normal human peripheral blood mononuclear cells[4].
体内活性
Intravenous (i.v.) injections of PRIMA-1 in mice does not cause any obvious changes in weight or behavior compared with untreated animals. PRIMA-1 has in vivo antitumor activity in this animal tumor model. It suppresses in vivo tumor growth in a mutant p53-dependent manner[3].
细胞实验
Cells are kept at a temperature of 37 °C, a minimum relative humidity of 95 %, and an atmosphere of 5 % CO2 in air. Cell viability is measured by MTT assay after treatment with PRIMA-1. Briefly, cells are seeded in each well of 96-well plates in 100 μl culture medium and incubated overnight at 37 °C in an atmosphere of 5 % CO2. The next day, the medium is removed and cells washed with PBS and treated with vehicle control(DMSO, dimethylsulfoxide) or different concentrations of PRIMA-1 for 12 to 48 h; the medium is replaced with MTT solution diluted in medium once the treatment is completed. The plates are further incubated at 37 °C under 5 % CO2 for 4 h and then left at room temperature until completely dry. DMSO was then added and the absorbance is read at 492 nm using a microplate enzyme-linked immunoassay reader (ELISA). The relative growth activity is determined as the percentage absorbance of treated cells compared to that of vehicle treated cells (control).(Only for Reference)
别名PRIMA 1, NSC-281668, 2,2-Bis(hydroxymethyl)-3-quinuclidinone
化学信息
分子量185.22
分子式C9H15NO3
CAS No.5608-24-2
SmilesOCC1(CO)N2CCC(CC2)C1=O
密度1.32g/cm3
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
Ethanol: 35 mg/mL (189 mM)
H2O: 18.5 mg/mL (100 mM)
DMSO: 50 mg/mL (269.95 mM)
溶液配制表
H2O/Ethanol/DMSO
1mg5mg10mg50mg
1 mM5.3990 mL26.9949 mL53.9898 mL269.9492 mL
5 mM1.0798 mL5.3990 mL10.7980 mL53.9898 mL
10 mM0.5399 mL2.6995 mL5.3990 mL26.9949 mL
20 mM0.2699 mL1.3497 mL2.6995 mL13.4975 mL
50 mM0.1080 mL0.5399 mL1.0798 mL5.3990 mL
100 mM0.0540 mL0.2699 mL0.5399 mL2.6995 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments比如您的给药剂量是 10 mg/kg ,每只动物体重 20 g ,给药体积 100 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
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g
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2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
%Tween 80
%ddH2O

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