444153

MDM2/MDMX Dual Inhibitor, RO-5963

• Sinónimos: 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
• Fórmula empírica (notación de Hill): C₂₄H₂₁ClF₂N₄O₅
• Peso molecular: 518.90
• Código UNSPSC: 12352200

Propiedades

• Ensayo: ≥98% (HPLC)
• Nivel de calidad: 100
• Formulario: solid
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze; desiccated (hygroscopic); protect from light
• color: orange-brown
• solubilidad: DMSO: 100 mg/mL
• Condiciones de envío: ambient
• temp. de almacenamiento: −20°C

Descripción

Descripción general

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.

Acciones bioquímicas o fisiológicas

Cell permeable: yes

Primary Target
MDMX

Reversible: yes

Secondary Target
MDM2

Envase

Packaged under inert gas

Advertencia

Toxicity: Standard Handling (A)

Reconstitución

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

Otras notas

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

Información legal

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

Información de seguridad

• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 3
• Punto de inflamabilidad (°F): Not applicable
• Punto de inflamabilidad (°C): Not applicable