RO-5963

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

RO-5963 是 p53-MDM2 和 p53-MDMX 互相作用的双抑制剂，IC50 值分别约为 17 nM 和 24 nM。

RO-5963 is a dual p53-MDM2 and p53-MDMX inhibitor with IC50s of ~17 nM and ~24 nM, respectively.

RO-5963 (10-20 μM; 48 hours) shows much higher apoptotic activity than Nutlin in both MCF7 and ZR75-30 cell lines.RO-5963 (10 μM, 24 hours) effectively activats p53 and elevates p21 and MDM2 levels.Apoptosis Analysis Cell Line:ZR75-30, MCF7 cells Concentration:10, 20 μM Incubation Time:48 hours Result:Potently showed apoptotic activity.Western Blot Analysis Cell Line:LNCap, U2OS, RKO, A489, 22Rv1, HCT116, H460, LOX, MCF7, A549, G401 cells Concentration:10 μM Incubation Time:24 hour Result:Effectively activated p53 and elevated p21 and MDM2 levels.

——

——

Apoptosis

MDM2-p53

Mdm2 | p53

——

——

1416663-77-8

518.9

C24H21ClF2N4O5

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 150 mg/mL (289.07 mM; 超声助溶 )

C(C(NC(CO)CO)=O)(N1C(=O)C(=CC=2C=3C(NC2)=C(C)C(Cl)=CC3)NC1=O)C4=CC(F)=C(F)C=C4

——

(-20℃)

With Ice Pack

≥ 2 years