572650

SU9516

A cell-permeable 3-substituted indolinone compound that displays anti-proliferative and proapoptotic properties in tumor cells.

• Sinónimos: SU9516, 3-[1-(3H-Imidazol-4-yl)-meth-(Z)-ylidene]-5-methoxy-1,3-dihydro-indol-2-one
• Fórmula empírica (notación de Hill): C₁₃H₁₁N₃O₂
• Número de CAS: 666837-93-0
• Peso molecular: 241.25
• Código UNSPSC: 12352200
• NACRES: NA.77

Propiedades

• Nivel de calidad: 100
• Análisis: ≥95% (HPLC)
• formulario: solid
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze; protect from light
• color: yellow to orange
• solubilidad: DMSO: 10 mg/mL
• Condiciones de envío: ambient
• temp. de almacenamiento: 2-8°C

Descripción

Descripción general

A cell-permeable 3-substituted indolinone compound that displays anti-proliferative and proapoptotic properties in tumor cells. Acts as a potent, selective, reversible, and ATP-competitive inhibitor of cyclin dependent kinases (Cdks; IC₅₀ = 22 nM for Cdk2/A; 40 nM for Cdk1/B; 200 nM for Cdk4/D1). It shows no significant effect (IC₅₀ >10 µM) on the activities of PKC, p38, PDGFRβ, or EGFR. Inhibits the proliferation of growth factor-stimulated colon carcinoma cells by binding to Cdk2 and preventing the phosphorylation of pRb and its dissociation from E2F.

A cell-permeable, 3-substituted indolinone compound that displays anti-proliferative and pro-apoptotic properties in tumor cells. Acts as a potent, selective, reversible, and ATP-competitive inhibitor of cyclin dependent kinases (Cdks) (IC₅₀ = 22 nM for Cdk2/A; 40 nM for Cdk1/B; 200 nM for Cdk4/D1). Exhibits no significant effect on the activities of PKC, p38, PDGFRβ, or EGFR (IC₅₀ >10 µM). Reported to inhibit the proliferation of growth factor-stimulated colon carcinoma cells by binding to Cdk2 and preventing the phosphorylation of pRb and its dissociation from E2F.

Acciones bioquímicas o fisiológicas

Cell permeable: yes

Primary Target
Cdk2/A

Product competes with ATP.

Reversible: yes

Target IC₅₀: 22 nM for Cdk2/A; 40 nM for Cdk1/B; 200 nM for Cdk4/D1

Advertencia

Toxicity: Carcinogenic / Teratogenic (D)

Reconstitución

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

Otras notas

Yu, B., et al. 2002. Biochem. Pharmacol.64, 1091.
Lane, M.E., et al. 2001. Cancer Res.61, 6170.

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 1
• Punto de inflamabilidad (°F): Not applicable
• Punto de inflamabilidad (°C): Not applicable