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Nutlin-3a

CAS号

675576-98-4

分子式

C30H30Cl2N4O4

主要靶点

Apoptosis|E1/E2/E3 Enzyme|Autophagy

仅限科研使用

Cat No : CM05040

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Synonyms

Rebemadlin|Nutlin-3|Nutlin 3a|Nutlin3a|Nutlin-3a|Nutlin-3a chiral|ovarian|p53/MDM2|p53|Inhibitor|MDM-2/p53|Ubiquitin activating enzyme|Ubiquitin conjugating enzyme|Ubiquitin ligase|inhibit|E1 activating enzyme|E3 ligating enzyme|E3Enzyme|E1/E2/E3 Enzyme|E1 Enzyme|E1Enzyme|E2 Enzyme|E2 conjugating enzyme|E3 Enzyme|E2Enzyme|Apoptosis|(?)-Nutlin-3|(-)-Nutlin-3|Autophagy|carcinomas

验证数据展示

  • CAS No.: 675576-98-4

    Nutlin-3a
    CAS#: 675576-98-4

产品信息

CAS号 675576-98-4
分子式 C30H30Cl2N4O4
主要靶点 Apoptosis|E1/E2/E3 Enzyme|Autophagy
主要通路 凋亡|泛素化|自噬
分子量 581.49
纯度 99.05%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 Rebemadlin|Nutlin-3|Nutlin 3a|Nutlin3a|Nutlin-3a|Nutlin-3a chiral|ovarian|p53/MDM2|p53|Inhibitor|MDM-2/p53|Ubiquitin activating enzyme|Ubiquitin conjugating enzyme|Ubiquitin ligase|inhibit|E1 activating enzyme|E3 ligating enzyme|E3Enzyme|E1/E2/E3 Enzyme|E1 Enzyme|E1Enzyme|E2 Enzyme|E2 conjugating enzyme|E3 Enzyme|E2Enzyme|Apoptosis|(?)-Nutlin-3|(-)-Nutlin-3|Autophagy|carcinomas

靶点活性

MDM2-p53 interaction:90 nM

体内活性

方法：为检测体内抗肿瘤活性，将 Nutlin-3a (25 mg/kg) 腹腔注射给携带 U-2 OS (wt p53) 异种移植物的 SCID 小鼠，每天一次，持续两周。 结果：治疗 2 周后，对于 U-2 OS 细胞，Nutlin-3a 治疗组的平均肿瘤体积为 480 mm3，而对照组为 1751 mm3。此外，两只接受 Nutlin-3a 治疗的小鼠在治疗结束时没有明显的肿瘤。[2]

体外活性

方法：人胶质母细胞瘤细胞 U87MG (p53 wild-type) 和 T98G (p53-mutant) 用 Nutlin-3a (0.6-20 μM) 处理 96 h，通过 MTT assay 检测细胞活力。 结果：与 Nutlin-3a 孵育 96 h 导致野生型 p53 U87MG 细胞系中细胞存活率呈剂量依赖性降低，而突变型 p53 T98G 细胞系中没有观察到细胞存活率的显著降低。[1] 方法：U-2 OS 细胞用 Nutlin-3a (2-10 μM) 处理 48 h，通过 flow cytometry 检测细胞凋亡和细胞周期。 结果：在 U-2 OS 细胞中检测到约 37% 的凋亡细胞。我们还发现，Nutlin-3a 处理的 U-2 OS 细胞以剂量依赖的方式阻滞在 G1 期。[2]

溶解度

Ethanol:58.2 mg/mL (100 mM);DMSO:55 mg/mL (94.58 mM)

细胞实验

SRB(Only for Reference)

参考文献

1.Villalonga-Planells R, et al. Activation of p53 by nutlin-3a induces apoptosis and cellular senescence in human glioblastoma multiforme. PLoS One. 2011 Apr 5;6(4):e18588.
2.Wang B, et al. MDM2 inhibitor Nutlin-3a suppresses proliferation and promotes apoptosis in osteosarcoma cells. Acta Biochim Biophys Sin (Shanghai). 2012 Aug;44(8):685-91.
3.Vassilev LT, et al. Science, 2004, 303(5659), 844-848.

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