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444153

MDM2/MDMX Dual Inhibitor, RO-5963

Name: MDM2/MDMX Dual Inhibitor, RO-5963
Brand: MM

Synonym(s):

MDM2/MDMX Dual Inhibitor, RO-5963, MDM2 Inhibitor VIII, MDMX Inhibitor III, ( 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, MDM2 Antagonist V, MDM2 Inhibitor VIII, MDMX Inhibitor III, (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, MDM2 Antagonist V

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About This Item

Empirical Formula (Hill Notation):

C₂₄H₂₁ClF₂N₄O₅

Molecular Weight:

518.90

UNSPSC Code:

12352200

Assay:

≥98% (HPLC)

Form:

solid

Quality level:

100

Storage condition:

OK to freeze, desiccated (hygroscopic), protect from light

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Properties

assay

≥98% (HPLC)

Quality Level

100

form

solid

manufacturer/tradename

Calbiochem^®

storage condition

OK to freeze, desiccated (hygroscopic), protect from light

color

orange-brown

solubility

DMSO: 100 mg/mL

shipped in

ambient

storage temp.

−20°C

Description

General description

A cell-permeable indolyl-hydantoin compound that simultaneously inhibits the interaction of both, MDM2 and MDMX with p53 (IC₅₀ = 17.3 and 24.7 nM, respectively, in vitro). Releases p53 from MDMX inhibition, stabilizes it, and fully restores its function. Shown to be far more superior to Nutlin-3a (>Cat. No. 444152) in blocking p53 interaction with MDMX. Binds to Phe, Trp, and Leu sub-pockets on the surface of MDMX and MDM2, and promotes MDMX and MDM2 dimer formation. Shown to induce cell cycle arrest in G1 and G2 phases. Also reported to induce apoptosis in several tumor cell lines expressing wild-type p53/MDMX (~ 10 to 20 µM). Its actions are not believed to be due to any genotoxic stress.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
MDMX

Reversible: yes

Secondary Target
MDM2

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Graves, B., et al. 2012. Proc. Natl. Acad. Sci. USA109, 11788.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c