RO-5963

Modify Date: 2024-01-09 14:47:39

RO-5963 Structure
RO-5963 structure
Common Name RO-5963
CAS Number 1416663-77-8 Molecular Weight 518.90
Density N/A Boiling Point N/A
Molecular Formula C24H21ClF2N4O5 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of RO-5963


RO-5963 is a dual p53-MDM2 and p53-MDMX inhibitor with IC50s of ~17 nM and ~24 nM, respectively[1].

 Names

Name RO-5963

 RO-5963 Biological Activity

Description RO-5963 is a dual p53-MDM2 and p53-MDMX inhibitor with IC50s of ~17 nM and ~24 nM, respectively[1].
Related Catalog
Target

IC50: ~17 nM (p53-MDM2), ~24 nM (p53-MDMX)[1]

In Vitro RO-5963 (10-20 μM; 48 hours) shows much higher apoptotic activity than Nutlin in both MCF7 and ZR75-30 cell lines[1]. RO-5963 (10 μM, 24 hours) effectively activats p53 and elevates p21 and MDM2 levels[1]. Apoptosis Analysis[1] Cell Line: ZR75-30, MCF7 cells Concentration: 10, 20 μM Incubation Time: 48 hours Result: Potently showed apoptotic activity. Western Blot Analysis[1] 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.
References

[1]. Graves B, et al. Activation of the p53 pathway by small-molecule-induced MDM2 and MDMX dimerization. Proc Natl Acad Sci U S A. 2012 Jul 17;109(29):11788-93.

 Chemical & Physical Properties

Molecular Formula C24H21ClF2N4O5
Molecular Weight 518.90