CAS:548472-68-0Nutlin 3

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Nutlin 3 is an MDM2 antagonist which can activate p53 pathway through inhibition of p53-MDM2 interaction.

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18817579266

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18817579266

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实验数据

技术信息

CAS号

548472-68-0

储存条件

分子式

C30H30Cl2N4O4

运输

蓝冰

分子量

581.49

别名

溶解度

DMSO	50.0 mg/mL (86.0 mM)
Water	Insoluble

动物实验配方

生物活性

描述MDM2 binds the p53 tumor suppressor protein with high affinity and negatively modulates its transcriptional activity and stability. Overexpression of MDM2, found in many human tumors, effectively impairs p53 function. Therefore, inhibition of MDM2-p53 interaction can stabilize p53 and may offer a novel strategy for cancer therapy. Nutlin 3 effectively inhibits the MDM2-p53 interaction with IC_{50_{value of 90 nM, leading to the activation of the p53 pathway. In SJSA-1 cells, treatment with 10 μM nutlin 3 for 48 h significantly induced the apoptosis of caspase-dependent cells. In HCT116, RKO and SJSA-1 cells containing wild-type p53, Nutlin 3 induced the expression of MDM2 and p21 with effective anti-proliferative activity with IC₅₀ value of ~1.5 μM. In nude mice, Nutlin 3, administered orally at 200 mg/kg twice daily for 3 weeks, significantly inhibited the growth of human tumor xenografts by 90% ^[3].}}
作用机制 Nutlin 3 binds MDM2 in the p53-binding pocket ^[3].
动物研究
剂量
Mice: 5 mg/kg^[3] (i.p.), 40 mg/kg^[4] (i.p.), 200 mg/kg^[5] (p.o.)

给药途径
i.p., p.o.