Nutlin-3a 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。

Nutlin-3a, the active enantiomer of Nutlin-3, inhibits MDM2-p53 interactions and stabilizes the p53 protein.

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.

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％）。

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

SRB(Only for Reference)

675576-98-4

C30H30Cl2N4O4

581.49

(–)-Nutlin-3;(-)-Nutlin-3;Nutlin-3a chiral

Ethanol:58.2 mg/mL (100 mM)
DMSO:58.2 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years