store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Nutlin-3a ((−)-Nutlin-3) 是 Nutlin-3 的活性对映体,是一种 MDM2抑制剂,可抑制 MDM2-p53相互作用,稳定 p53 蛋白,从而诱导细胞自噬和凋亡,有潜力研究 TP53野生型卵巢癌。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 449 | 现货 | ||
2 mg | ¥ 658 | 现货 | ||
5 mg | ¥ 957 | 现货 | ||
10 mg | ¥ 1,180 | 现货 | ||
25 mg | ¥ 1,890 | 现货 | ||
50 mg | ¥ 2,890 | 现货 | ||
100 mg | ¥ 4,120 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,160 | 现货 |
产品描述 | Nutlin-3a ((−)-Nutlin-3), the active enantiomer of Nutlin-3, inhibits MDM2-p53 interactions and stabilizes the p53 protein. |
靶点活性 | MDM2-p53 interaction:90 nM |
体外活性 | 用10 μM nutlin-3a孵育7天导致NIH3T3细胞生长抑制> 90%。Nutlin-3α稳定并激活p53基因,剂量依赖性诱导p21的表达。Nutlin-3a取代MDM2结合口袋中的p53,从而释放p53抑制和蛋白酶体降解,导致诱导其下游靶点,细胞周期停滞和凋亡。Nutlin-3A有效地减少S期细胞至0.2-2%,并增加了G1-和G2/M期细胞。Nutlin-3a诱导约60%的SJSA-1和MHM细胞在40小时后发生凋亡,其在60小时后分别进一步增加(分别为85%和65%)。 |
体内活性 | Nutlin-3是体内p53途径的选择性激活剂,对SJSA-1骨肉瘤肿瘤具有高度的有效性.Nutlin-3α以剂量依赖性方式抑制异种移植物生长,其中最高剂量(200 mg/kg)表现出显著的肿瘤缩小.Nutlin-3α治疗对有野生型p53和MDM2基因扩增的肿瘤效果最佳. |
激酶实验 | Biacore studies: Competition assays are performed on a Biacore S51. A Series S Sensor chip CM5 is derivatized for immobilization of a PentaHis antibody for capture of the His-tagged p53. The level of capture is ~ 200 response units (1 response unit corresponds to 1 pg of protein per mm 2). The concentration of MDM2 protein is kept constant at 300 nM. Test compounds are dissolved in DMSO at 10 mM and further diluted to make a concentration series of inhibitor in each MDM2 test sample. The assays are run at 25 °C in running buffer (10 mM Hepes, 0.15 M NaCl, 2% DMSO). MDM2-p53 binding in the presence of inhibitor is calculated as a percentage of binding in the absence of inhibitor and IC50 is calculated using Microsoft Excel |
细胞实验 | SRB(Only for Reference) |
别名 | (-)-Nutlin-3, Nutlin-3a chiral, (−)-Nutlin-3 |
分子量 | 581.49 |
分子式 | C30H30Cl2N4O4 |
CAS No. | 675576-98-4 |
store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 58.2 mg/mL (100 mM)
DMSO: 58.2 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 1.7197 mL | 8.5986 mL | 17.1972 mL | 42.993 mL |
5 mM | 0.3439 mL | 1.7197 mL | 3.4394 mL | 8.5986 mL | |
10 mM | 0.172 mL | 0.8599 mL | 1.7197 mL | 4.2993 mL | |
20 mM | 0.086 mL | 0.4299 mL | 0.8599 mL | 2.1497 mL | |
50 mM | 0.0344 mL | 0.172 mL | 0.3439 mL | 0.8599 mL | |
100 mM | 0.0172 mL | 0.086 mL | 0.172 mL | 0.4299 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
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: 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 μL,一共给药动物10 只,您使用的配方为5% 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 μL DMSO (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:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Nutlin-3a 675576-98-4 Apoptosis Autophagy Ubiquitination E1/E2/E3 Enzyme E1 activating enzyme inhibit E3 ligating enzyme p53 carcinomas ovarian (-)-Nutlin-3 Nutlin-3 Ubiquitin ligase Ubiquitin conjugating enzyme Ubiquitin activating enzyme Nutlin 3a Inhibitor Nutlin3a Nutlin-3a chiral MDM-2/p53 (−)-Nutlin-3 Rebemadlin E2 conjugating enzyme inhibitor