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RO-5963

Chemical Structure : RO-5963

CAS No.: 1416663-77-8

RO-5963 (RO 5963;RO5963)

Catalog No.: PC-60443Not For Human Use, Lab Use Only.

RO-5963 is a potent, dual MDM2/MDMX-p53 interaction inhibitor with IC50 of 17 and 24 nM, respectively.

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Biological Activity

RO-5963 is a potent, dual MDM2/MDMX-p53 interaction inhibitor with IC50 of 17 and 24 nM, respectively.
RO-5963 stabilizes p53 and activates the p53 pathway in cancer cells, inhibits the binding of p53 to MDM2 and MDMX.
RO-5963 restores p53 transcriptional activity, elevates protein levels of its transcription targets, p21 and MDM2, and overcomes the apoptotic resistance of MDMX-overexpressing cell line, SJSA-X, to nutlin-3.
RO-5963 decreases cell viability and induces cell death.

Physicochemical Properties

M.Wt 518.902
Formula C24H21ClF2N4O5
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(Z)-2-(4-((6-Chloro-7-methyl-1H-indol-3-yl)methylene)-2,5-dioxoimidazolidin-1-yl)-2-(3,4-difluorophenyl)-N-(1,3-dihydroxypropan-2-yl)acetamide

References

1. Graves B, et al. Proc Natl Acad Sci U S A. 2012 Jul 17;109(29):11788-93.

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