Biochem/physiol Actions

Reversible: yes

Product competes with ATP.

Target IC₅₀: 500 nM against platelet-derived growth factor receptor tyrosine kinase

Primary TargetPlatelet-derived growth factor receptor tyrosine kinase

Cell permeable: yes

General description

A selective, cell-permeable, reversible, and substrate competitive inhibitor of the platelet-derived growth factor receptor tyrosine kinase (IC₅₀ = 500 nM). Anti-proliferative agent. Uncoupler of oxidative phosphorylation. Induces apoptosis in vitro and cell growth arrest in NHL cell lines.

Anti-proliferative agent that acts as a selective inhibitor of the platelet-derived growth factor receptor tyrosine kinase (IC₅₀ = 500 nM). A potent, cell-permeable, reversible, and substrate competitive inhibitor of TNF-induced tyrosine phosphorylation of PYK2. Uncouples oxidative phosphorylation and induces apoptosis and cell growth arrest in NHL cell lines. Inhibits Cdk2 activity in lymphoma cell lines.

Legal Information

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

Other Notes

Due to the nature of the Hazardous Materials in this shipment, additional shipping charges may be applied to your order. Certain sizes may be exempt from the additional hazardous materials shipping charges. Please contact your local sales office for more information regarding these charges.

Fuortes, M., et al. 1999. J. Clin. Invest.104, 327.Palumbo, G.A., et al. 1997. Cancer Res. 57, 2434.Burger, A.M., et al. 1995. Cancer Res.55, 2794.Palumbo, G.A., et al. 1994. Blood84, 296a.Bilder, G.E., et al. 1991. Am. J. Physiol. 260, C721.Levitzki, A., and Gilon, S. 1991. Trends Pharmacol. Sci. 12, 171.Terada, H. 1981. Biochim. Biophys. Acta639, 225

Packaging

5 mg in Alu drum

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

Warning

Toxicity: Toxic (F)