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658401

AG 490

A cell-permeable, reversible, substrate competitive, and potent inhibitor of epidermal growth factor receptor kinase autophosphorylation (IC50 = 100 nM).

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

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5 MG

$78.30

$78.30

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About This Item

Empirical Formula (Hill Notation):
C17H14N2O3
CAS Number:
133550-30-8
Molecular Weight:
294.30
MDL number:
MFCD00236452
UNSPSC Code:
12352200
NACRES:
NA.77

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Quality Level

100

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

SMILES string

N(Cc2ccccc2)C(=O)\C(=C\c1cc(c(cc1)O)O)\C#N

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

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This Item
658411658395420099
AG 490 A cell-permeable, reversible, substrate competitive, and potent inhibitor of epidermal growth factor receptor kinase autophosphorylation (IC50 = 100 nM).

Sigma-Aldrich

658401

AG 490

AG490 InSolution, ≥98%, inhibitor of EGFR kinase autophosphorylation

Sigma-Aldrich

658411

AG490

AG 18 A broad-spectrum protein tyrosine kinase inhibitor.

Sigma-Aldrich

658395

AG 18

JAK Inhibitor I JAK Inhibitor I, CAS 457081-03-7, is a potent, reversible, cell-permeable, and ATP-competitive inhibitor of JAK 1 (IC50 = 15 nM), JAK2 (IC50 = 1 nM), JAK3 (Ki = 5 nM) and Tyk2 (IC50 = 1 nM).

Millipore

420099

JAK Inhibitor I

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

form

solid

form

liquid

form

solid

form

solid

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

storage temp.

−20°C

storage temp.

−70°C

storage temp.

−20°C

storage temp.

−20°C

solubility

DMSO: 100 mg/mL

solubility

-

solubility

DMSO: 100 mg/mL, ethanol: 50 mg/mL, acetic acid: soluble

solubility

DMSO: 5 mg/mL

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.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
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

Preparation Note

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.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

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