658395

AG 18

A broad-spectrum protein tyrosine kinase inhibitor.

• Synonym(e): AG 18, α-Cyano-(3,4-dihydroxy)cinnamonitrile, Tyrphostin A23, RG-50810
• Empirische Formel (Hill-System): C₁₀H₆N₂O₂
• CAS-Nummer: 118409-57-7
• Molekulargewicht: 186.17
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD00133899
• Assay: ≥98% (HPLC)
• Form: solid
• Storage condition: OK to freeze, protect from light

Eigenschaften

• Quality Segment: 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
• SMILES string: N#CC(=Cc1cc(c(cc1)O)O)C#N
• 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

Beschreibung

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

Preparation Note

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

Disclaimer

Toxicity: Standard Handling (A)

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable