General description

Potent inhibitor of epidermal growth factor receptor kinase autophosphorylation (IC₅₀ = 100 nM). Jak family tyrosine kinase inhibitor. Inhibition of Jak2 by AG 490 selectively blocks leukemic cell growth in vitro and in vivo by inducing programmed cell death, with no harmful effect on normal haematopoiesis. Inhibits the constitutive activation of STAT-3 and IL-2-induced growth of MF tumor cells. AG 490 has also been shown to inhibit the autokinase activity of JAK3. Also reported to inhibit guanylyl cyclase.

Legal Information

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

Other Notes

Jaleel, M., et al. 2004. Biochemistry43, 8247.Eriksen, K.W., et al. 2001. Leukemia15, 787.Kirken, R.A., et al. 1999. Leukoc. Biol.65, 891.Nielsen, M., et al. 1997. Proc. Natl. Acad. Sci. USA 94, 6764.Meydan, N., et al. 1996. Nature 379, 645.Gazit, A., et al. 1991. J. Med. Chem.34, 1896.Levitzki, A. 1990. Biochem. Pharmacol.40, 913.

Packaging

Packaged under inert gas

5 mg in Plastic ampoule

Physical form

A 100 mM (5 mg/170 µl) solution of AG490 (Cat. No. 658401) in DMSO.

Reconstitution

Following initial thaw, aliquot and freeze (-70°C). Once opened, stock solution is stable for up to 6 months at -70°C.

Warning

Toxicity: Irritant (B)