Nutlin-3a

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Chemical Structure| 675576-98-4 同义名 : Rebemadlin;(−)-Nutlin-3;(-)-Nutlin-3
CAS号 : 675576-98-4
货号 : A809136
分子式 : C30H30Cl2N4O4
纯度 : 99%+
分子量 : 581.49
MDL号 : MFCD14636430
存储条件：

Pure form Sealed in dry,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(180.57 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

5% DMSO+55% PEG 300+water 8 mg/mL

生物活性
描述 Nutlin-3a, the active enantiomer of Nutlin-3, is a robust inhibitor of murine double minute (MDM2) with an IC50 of 90 nM. It blocks the interactions between MDM2 and p53, thereby stabilizing the p53 protein, and leads to the induction of cell autophagy and apoptosis. Nutlin-3a is considered promising for research into TP53 wild-type ovarian carcinomas[1][2]. Nutlin-3a serves as a therapeutic agent that inhibits MDM2, activates wild-type p53, and triggers apoptosis, making it a potential treatment for TP53 wild-type ovarian carcinomas. Three cell lines with wild-type TP53—HOC-7, OVCA429, and A2780—show high sensitivity to Nutlin-3a, with IC50 values ranging from 4 to 6 μM. SKOV3 cells present an IC50 of 38 μM in response to Nutlin-3a. Additionally, the two other ovarian clear cell lines with TP53 wild-type, TOV21G and OVAS, exhibit relatively higher sensitivity to Nutlin-3a-induced growth inhibition, with IC50 values of 14 μM and 25 μM, respectively, compared to TP53 mutant cell lines[1]. After seven days of incubation with 10 μM Nutlin-3a, there is more than 90% inhibition of NIH/3T3 cells' growth, while the proliferation of MEF cells, which lack both targets of the drug, remains unaffected. Nutlin-3a effectively halts cell-cycle progression across all cell lines, reducing the S-phase compartment to 0.2-2% and enlarging the G1- and G2/M-phase compartments, indicative of G1 and G2 arrest. The p53 targets, p21 and MDM2, show a significant increase just 3 hours after the addition of Nutlin-3a and reach peak levels at 8 hours. Nutlin-3a triggers apoptosis in approximately 60% of SJSA-1 and MHM cells after 40 hours, with the percentage rising after 60 hours to 85% and 65%, respectively[2].
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
22RV1 Growth Inhibition Assay IC50=12.8059 μM SANGER
697 Growth Inhibition Assay IC50=5.4455 μM SANGER
A101D Growth Inhibition Assay IC50=2.3501 μM SANGER
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.72mL

0.34mL

0.17mL

8.60mL

1.72mL

0.86mL

17.20mL

3.44mL

1.72mL
参考文献

[1]Crane EK, et al. Nutlin-3a: A Potential Therapeutic Opportunity for TP53 Wild-Type Ovarian Carcinomas. PLoS One. 2015 Aug 6;10(8):e0135101.

[2]Tovar C, et al. Small-molecule MDM2 antagonists reveal aberrant p53 signaling in cancer: implications for therapy. Proc Natl Acad Sci U S A. 2006 Feb 7;103(6):1888-93.