572650

SU9516

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

• Synonim(y): SU9516, 3-[1-(3H-Imidazol-4-yl)-meth-(Z)-ylidene]-5-methoxy-1,3-dihydro-indol-2-one
• Wzór empiryczny (zapis Hilla): C₁₃H₁₁N₃O₂
• Numer CAS: 666837-93-0
• Masa cząsteczkowa: 241.25
• Numer MDL: MFCD17010284
• Kod UNSPSC: 12352200
• NACRES: NA.77

Właściwości

• Poziom jakości: 100
• Próba: ≥95% (HPLC)
• Formularz: solid
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; protect from light
• kolor: yellow to orange
• rozpuszczalność: DMSO: 10 mg/mL
• Warunki transportu: ambient
• temp. przechowywania: 2-8°C
• ciąg SMILES: [nH]1cncc1C=C2c3c(ccc(c3)OC)NC2=O
• InChI: 1S/C13H11N3O2/c1-18-9-2-3-12-10(5-9)11(13(17)16-12)4-8-6-14-7-15-8/h2-7H,1H3,(H,14,15)(H,16,17)

Opis

Opis ogólny

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.

Działania biochem./fizjol.

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

Ostrzeżenie

Toxicity: Carcinogenic / Teratogenic (D)

Rekonstytucja

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

Inne uwagi

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

Informacje prawne

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

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Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 1
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable