572650

SU9516

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

• 別名: SU9516, 3-[1-(3H-Imidazol-4-yl)-meth-(Z)-ylidene]-5-methoxy-1,3-dihydro-indol-2-one
• 実験式（ヒル表記法）: C₁₃H₁₁N₃O₂
• CAS番号: 666837-93-0
• 分子量: 241.25
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥95% (HPLC)
• 形状: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: yellow to orange
• 溶解性: DMSO: 10 mg/mL
• 輸送温度: ambient
• 保管温度: 2-8°C

詳細

詳細

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.

生物化学的／生理学的作用

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

警告

Toxicity: Carcinogenic / Teratogenic (D)

再構成

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

その他情報

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

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 1
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable