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658395

Sigma-Aldrich

AG 18

A broad-spectrum protein tyrosine kinase inhibitor.

Synonym(s):

AG 18, α-Cyano-(3,4-dihydroxy)cinnamonitrile, Tyrphostin A23, RG-50810

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About This Item

Empirical Formula (Hill Notation):
C10H6N2O2
CAS Number:
118409-57-7
Molecular Weight:
186.17
MDL number:
MFCD00133899
UNSPSC Code:
12352200
NACRES:
NA.77

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
ethanol: 50 mg/mL
acetic acid: soluble

shipped in

ambient

storage temp.

−20°C

InChI

1S/C10H6N2O2/c11-5-8(6-12)3-7-1-2-9(13)10(14)4-7/h1-4,13-14H

InChI key

VTJXFTPMFYAJJU-UHFFFAOYSA-N

General description

A broad-spectrum protein tyrosine kinase inhibitor. Inhibits epidermal growth factor receptor autophosphorylation (IC50 = 40 µM) and the GTPase activity of transducin (IC50 = 10 µM). Inhibits aldosterone secretion in response to Angiotensin II (Cat. No. 05-23-0101). Suppresses the activation of MAP kinases by cholecystokinin in pancreatic acini.
A cell-permeable, reversible, substrate competitive protein tyrosine kinase inhibitor. Inhibits epidermal growth factor receptor autophosphorylation (IC50 = 40 µM) and the GTPase activity of transducin (IC50 = 10 µM). Inhibits aldosterone secretion in response to angiotensin II. Suppresses the activation of MAP kinases by cholecystokinin in pancreatic acini. Also reported to inhibit guanylyl cyclase.

Biochem/physiol Actions

Cell permeable: no
Primary Target
epidermal growth factor receptor autophosphorylation
Product does not compete with ATP.
Reversible: no
Target IC50: 40 µM against epidermal growth factor receptor autophosphorylation; 10 µM against GTPase activity of transducin

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

Other Notes

Jaleel, M., et al. 2004. Biochemistry43, 8247.
Kapas, S., et al. 1995. Biochem. J. 305, 433.
Seger, R., et al. 1995. J. Biol. Chem.270, 28325.
Williams, J.A. 1994. Am. J. Physiol.267, G401.
Geissler, J.F., et al. 1990. J. Biol. Chem.265, 22255.
Levitzki, A. 1990. Biochem. Pharmacol.40, 913.
Gazit, A., et al. 1989. J. Med. Chem. 32, 2344.
Lyall, R.M., et al. 1989. J. Biol. Chem. 264, 14503.

Legal Information

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

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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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