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抑制剂描述:

产品名称:Nutlin-3a

产品别名:见爱必信官网

英文别名:Nutlin-3a

靶点:MDM2

CAS:675576-98-4

纯度:98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

Nutlin-3a, the active enantiomer of Nutlin-3, inhibits the p53/MDM2 interaction with IC50 of 90 nM.

溶解性:Ethanol :58.2 mg/mL (100 mM)
DMSO :58.2 mg/mL (100 mM)

体外研究:

Nutlin-3a displaces p53 from the binding pocket of MDM2 and thereby releases p53 from inhibition and proteasomal degradation, leading to induction of its downstream targets, cell cycle arrest, and apoptosis. Seven days of incubation with 10 μM nutlin-3a led to >90% inhibition of NIH3T3 cells’ growth. Nutlin-3a stabilizes and activates p53, and induces p21 expression in a dose-dependent manner. Nutlin-3a effectively depletes the S-phase compartment to 0.2-2% and increases the G1- and G2/M-phase compartments. Nutlin-3a induces apoptosis in ~60% of SJSA-1 and MHMcells after 40 h, which increased further after 60 h (85% and 65%, respectively) .

体内研究:Nutlin-3a suppresses xenograft growth in a dose-dependent fashion with the highest dose (200 mg/kg) showing a substantial tumor shrinkage . Nutlin-3 is a selective activator of the p53 pathway in vivo and highly efficacious against SJSA-1 osteosarcoma tumors. Tumors with wild-type p53 and mdm2 gene amplification will respond best to therapy with Nutlin-3a.

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