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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。


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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 | |
| 1 mL x 10 mM (in DMSO) | ¥ 338 | 现货 |
| 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 |
| 分子量 | 185.22 |
| 分子式 | C9H15NO3 |
| CAS No. | 5608-24-2 |
| Smiles | OCC1(CO)N2CCC(CC2)C1=O |
| 密度 | 1.32g/cm3 |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||||||||||||
| 溶解度信息 | Ethanol: 35 mg/mL (188.96 mM), Sonication is recommended. H2O: 18.5 mg/mL (99.88 mM), Sonication is recommended. DMSO: 50 mg/mL (269.95 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||||||||||||
| 体内实验配方 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (10.8 mM), Sonication is recommended. 请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。 | ||||||||||||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||||||||||||
H2O/Ethanol/DMSO
Ethanol/DMSO
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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。
对于不同动物的给药剂量换算,您也可以参考 更多