Nutlin-3a (Synonyms: Rebemadlin) 纯度: 98.07%
Nutlin-3a (Rebemadlin) 是 Nutlin-3 的活性对映体,是一种有效的 MDM2 抑制剂。Nutlin-3a 可抑制 MDM2-p53 相互作用,稳定 p53 蛋白,从而诱导细胞自噬 (autophagy) 和凋亡 (apoptosis)。Nutlin-3a 有潜力用于 TP53 野生型卵巢癌的研究。
Nutlin-3a Chemical Structure
CAS No. : 675576-98-4
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Free Sample (0.1-0.5 mg) | Apply now | ||
10 mM * 1 mL in DMSO | ¥1407 | In-stock | |
5 mg | ¥1100 | In-stock | |
10 mg | ¥1581 | In-stock | |
50 mg | ¥7114 | In-stock | |
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生物活性 |
Nutlin-3a (Rebemadlin), an active enantiomer of Nutlin-3, is a potent murine double minute (MDM2) inhibitor (IC50=90 nM). Nutlin-3a inhibits MDM2-p53 interactions and stabilizes the p53 protein, and induces cell autophagy and apoptosis. Nutlin-3a has the potential for the study of TP53 wild-type ovarian carcinomas[1][2]. |
IC50 & Target |
MDM2-p53[1] |
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体外研究 (In Vitro) |
Nutlin-3a is a therapeutic which inhibits MDM2, activates wild-type p53, and induces apoptosis-as a therapeutic compound for TP53 wild-type ovarian carcinomas. Three cell lines (HOC-7, OVCA429 and A2780) with wild-type TP53 are highly sensitive to Nutlin-3a (IC50=4 to 6 μM). SKOV3 cells have an IC50 of 38 μM to Nutlin-3a. The two remaining ovarian clear cell lines (TOV21G and OVAS), both with TP53 wild-type, are relatively more sensitive to growth inhibition with Nutlin-3a (IC50=14 and 25 μm respectively) than the TP53 mutant cell lines[1]. Nutlin-3a is the active enantiomer of Nutlin-3. Nutlin-3a is a highly selective MDM2 antagonist and p53 inducer. Seven days of incubation with 10 μM Nutlin-3a leads to >90% inhibition of NIH/3T3 cells’growth but does not affect the proliferation of MEF in which both targets of the drug are eliminated. Nutlin-3a effectively arrestes cell-cycle progression in all cell lines, depleting the S-phase compartment to 0.2-2% and increasing the G1– and G2/M-phase compartments, indicating G1 and G2 arrest. The p53 targets p21 and MDM2 are elevated significantly 3 h after Nutlin-3a addition and reach maximal levels at 8 h. Nutlin-3a induces apoptosis in ≈60% of SJSA-1 and MHM cells after 40 h, which increase further after 60 h (85% and 65%, respectively)[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 (In Vivo) |
Nutlin-3a is efficacious in all models with average tumor growth inhibition ≥98%. Nutlin-3a suppresses xenograft growth in a dose-dependent fashion with the highest dose (200 mg/kg) showing a substantial tumor shrinkage (eight partial and one full regressions). The established SJSA-1 and MHM osteosarcoma xenografts with Nutlin-3a causes extensive tumor regression[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
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分子量 |
581.49 |
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Formula |
C30H30Cl2N4O4 |
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CAS 号 |
675576-98-4 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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溶解性数据 |
In Vitro:
DMSO : ≥ 100 mg/mL (171.97 mM) * “≥” means soluble, but saturation unknown. 配制储备液
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
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参考文献 |
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Cell Assay [1] |
All 15 cell lines are plated at a density of 1×103 cells per well in 96-well plates. After 24h, media is exchanged and cells are treated with incremental concentrations of Nutlin 3a (1 μM, 5 μM, 10 μM, 25 μM, 50 μM, and 70 μM). After 72 h of incubation, WST-1 is added to each well, and a microplate reader is used at an absorbance of 450 nm to measure the number of remaining viable cells. Experiments are repeated with smaller titrations of Nutlin 3a as needed to determine the exact IC50 of cell lines. The IC50 is defined. Cell lines are again plated in a manner identical to above and treated with Nutlin 3a at their respective IC50, and WST-1 is added with cell viability measurement at 24, 48, and 72h[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
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Animal Administration [2] |
Mice[2] MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
参考文献 |
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