658401
AG 490
A cell-permeable, reversible, substrate competitive, and potent inhibitor of epidermal growth factor receptor kinase autophosphorylation (IC₅₀ = 100 nM).
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Synonym(s):
AG 490, α-Cyano-(3,4-dihydroxy)-N-benzylcinnamide, Tyrphostin B42, ( E)- N-benzyl-2-cyano-3-(3,4-dihydroxyphenyl)acrylamide, JAK1 Inhibitor II, JAK2 Inhibitor VI, JAK3 Inhibitor XI, α-Cyano-(3,4-dihydroxy)-N-benzylcinnamide, Tyrphostin B42, (E)-N-benzyl-2-cyano-3-(3,4-dihydroxyphenyl)acrylamide, JAK1 Inhibitor II, JAK2 Inhibitor VI, JAK3 Inhibitor XI
Empirical Formula (Hill Notation):
C17H14N2O3
CAS Number:
Molecular Weight:
294.30
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Recommended Products
Quality Level
Assay
≥98% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
yellow
solubility
DMSO: 100 mg/mL
shipped in
ambient
storage temp.
−20°C
InChI
1S/C17H14N2O3/c18-10-14(8-13-6-7-15(20)16(21)9-13)17(22)19-11-12-4-2-1-3-5-12/h1-9,20-21H,11H2,(H,19,22)/b14-8+
InChI key
TUCIOBMMDDOEMM-RIYZIHGNSA-N
General description
A cell-permeable, reversible, substrate competitive, and potent inhibitor of epidermal growth factor receptor kinase autophosphorylation (IC50 = 100 nM). 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 hematopoiesis. Inhibits the constitutive activation of STAT-3 DNA binding and IL-2-induced growth of MF tumor cells. AG 490 has also been shown to inhibit the autokinase activity of JAK3. A 100 mM (5 mg/170 µl) solution of AG490 (Cat. No. 658411) in DMSO is also available.
A cell-permeable, reversible, substrate competitive, and 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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
epidermal growth factor receptor kinase autophosphorylation
epidermal growth factor receptor kinase autophosphorylation
Product does not compete with ATP.
Reversible: yes
Target IC50: 100 nM against epidermal growth factor receptor kinase autophosphorylation
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-70°C). Stock solutions are 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.
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
WGK
WGK 3
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