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Nutlin-3 是一种 MDM2 拮抗剂,抑制 MDM2-p53 相互作用 (Ki=90 nM),并激活 p53。Nutlin-3 优先与 MDM2 的 p53 结合口袋结合,导致 p53 的稳定和 p53 通路的激活。Nutlin-3 具有抗肿瘤活性。
Nutlin-3 是一种 MDM2 拮抗剂,抑制 MDM2-p53 相互作用 (Ki=90 nM),并激活 p53。Nutlin-3 优先与 MDM2 的 p53 结合口袋结合,导致 p53 的稳定和 p53 通路的激活。Nutlin-3 具有抗肿瘤活性。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
2 mg | ¥ 468 | 现货 | |
5 mg | ¥ 721 | 现货 | |
10 mg | ¥ 997 | 现货 | |
25 mg | ¥ 1,944 | 现货 | |
50 mg | ¥ 3,787 | 现货 | |
100 mg | ¥ 4,310 | 现货 | |
200 mg | ¥ 6,140 | 现货 | |
500 mg | ¥ 9,310 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 934 | 现货 |
产品描述 | Nutlin-3 is an MDM2 antagonist that inhibits MDM2-p53 interaction (Ki=90 nM) and activates p53. Nutlin-3 binds preferentially to the p53-binding pocket of MDM2, leading to stabilization of p53 and activation of the p53 pathway. Nutlin-3 has antitumor activity. |
靶点活性 | MDM2-p53:0.09 μM |
体外活性 | 方法: 22RV1 (p53 WT)、DU145 (p53 Mut) 和 PC-3 (p53 Null) 细胞用 Nutlin-3 (2-10 µM) 处理 48 h,通过 Hoechst 33342 染色检测细胞凋亡。 结果: Nutlin-3 诱导 22RV1 细胞凋亡显著增加,而 p53 缺陷型 DU145 或 PC-3 细胞凋亡没有显著增加。Nutlin-3 在表达 WT p53 的细胞中优先增加凋亡。[1] 方法: H460 和 HCT116 p53+/+ 细胞用 Nutlin-3 (0-100 µM) 和 Inauhzin (0-100 µM) 处理 72 h,通过 WST assay 检测细胞活力。 结果: Inauhzin 和 Nutlin-3 在抑制这两种肿瘤细胞系的生长方面显示出明显的协同作用,因为在有效剂量范围内的 CI 值明显小于 1,特别是在使用较低剂量的 Nutlin-3 时。[2] |
体内活性 | 方法: 为检测体内抗肿瘤活性,将 Nutlin-3 (150 mg/kg,EtOH: Tween: 5% Glucose = 5:5:90;口服给药,每天两次,连续四天停止两天) 和 Inauhzin (15 mg/kg,腹腔注射,每天一次) 给药给携带 HCT116 p53+/+ 异种移植物的 SCID 小鼠,持续 21 天。 结果: 每种化合物在治疗 21 天后可以单独将平均肿瘤体积减少不到 20%。然而,当以相同剂量组合两种治疗方法时,肿瘤的最终平均体积减少了 60%。Inauhzin 和 Nutlin-3 可以激活 p53 并抑制动物异种移植物肿瘤的生长。[2] |
激酶实验 | Biacore study: Competition assay is performed on a Biacore S51. A Series S Sensor chip CM5 is utilized for the 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. Nutlin-3 is dissolved in DMSO at 10 mM and further diluted to make a concentration series of Nutlin-3 in each MDM2 test sample. The assay is run at 25°C in running buffer (10 mM Hepes, 0.15 M NaCl, 2% DMSO). MDM2-p53 binding in the presence of Nutlin-3 is calculated as a percentage of binding in the absence of Nutlin-3 and IC50 is calculated |
细胞实验 | Nutlin-3 (NUT) is dissolved with DMSO (100 mM) and diluted with appropriate media[2]. Human non-small-cell lung carcinoma wild type p53-containing H460 and A549, human non-small-cell lung carcinoma p53-null H1299, and human colon cancer HCT116 (p53+/+ and p53-/-) cells are used. Cells (1.5×105) are plated into 6-well plates, and incubated at 37°C overnight. After treatment of Inauhzin and Nutlin-3 at the indicated concentrations for 48 h, cells are harvested, fixed in 70% ice-cold ethanol overnight at -20°C, resuspended in propidium iodide-solution (50 μg/mL PI, 0.1 mg/mL RNase A, 0.05% Tritin X-100 in PBS) for 40 min at 37°C, then analyzed for DNA content using a flow cytometer and proprietary software[2]. |
别名 | Nutlin3 |
分子量 | 581.49 |
分子式 | C30H30Cl2N4O4 |
CAS No. | 548472-68-0 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 55 mg/mL (94.58 mM) | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
DMSO
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