658411

AG490

InSolution, ≥98%, inhibitor of EGFR kinase autophosphorylation

• Synonym(s): InSolution AG490, JAK1 Inhibitor II, JAK2 Inhibitor VI, JAK3 Inhibitor XI
• Empirical Formula (Hill Notation): C₁₇H₁₄N₂O₃
• Molecular Weight: 294.30
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: liquid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; desiccated (hygroscopic); protect from light
• shipped in: wet ice
• storage temp.: −70°C

Description

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.

Packaging

Packaged under inert gas

Warning

Toxicity: Irritant (B)

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.

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.

Legal Information

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

Safety Information

• Storage Class Code: 10 - Combustible liquids
• WGK: WGK 3
• Flash Point(F): 188.6 °F - (Dimethylsulfoxide)
• Flash Point(C): 87 °C - (Dimethylsulfoxide)