SU9516-CAS 666837-93-0-Calbiochem

C₁₃H₁₁N₃O₂

241.25

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.

Cell permeable: yes
Product competes with ATP.
Primary Target
Cdk2/A
Target IC₅₀: 22 nM for Cdk2/A; 40 nM for Cdk1/B; 200 nM for Cdk4/D1
Reversible: yes

Toxicity: Carcinogenic / Teratogenic (D)

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

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

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

100

≥95% (HPLC)

solid

Calbiochem^®

OK to freeze
protect from light

yellow to orange

DMSO: 10 mg/mL

ambient

2-8℃

5 mg in Plastic ampoule

11 - Combustible Solids

WGK 1