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Key Documents

658411

Sigma-Aldrich

AG490

InSolution, ≥98%, inhibitor of EGFR kinase autophosphorylation

Synonym(s):

InSolution AG490, JAK1 Inhibitor II, JAK2 Inhibitor VI, JAK3 Inhibitor XI

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About This Item

Empirical Formula (Hill Notation):
C17H14N2O3
Molecular Weight:
294.30
UNSPSC Code:
12352200
NACRES:
NA.77

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

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

Storage Class Code

10 - Combustible liquids

WGK

WGK 3

Flash Point(F)

188.6 °F - closed cup - (Dimethylsulfoxide)

Flash Point(C)

87 °C - closed cup - (Dimethylsulfoxide)

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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