428150

Lavendustin A

A cell-permeable, reversible, and substrate competitive inhibitor of EGF receptor tyrosine kinase and p60^c-src with little effect on protein kinase A or protein kinase C.

• Synonyme(s) : Lavendustin A, 5-Amino-[(N-2,5-dihydroxybenzyl)-Nʹ-2-hydroxybenzyl]salicylic Acid, RG14355
• Formule empirique (notation de Hill) : C₂₁H₁₉NO₆
• CAS Number: 125697-92-9
• Poids moléculaire : 381.38
• Numéro MDL: MFCD00153822
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Essai: ≥95% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: off-white
• Solubilité: ethanol: 10 mg/mL; DMSO: soluble
• Conditions d'expédition: ambient
• Température de stockage: −20°C
• Chaîne SMILES: N(Cc3c(ccc(c3)O)O)(Cc2c(cccc2)O)c1cc(c(cc1)O)C(=O)O
• InChI: 1S/C21H19NO6/c23-16-6-8-19(25)14(9-16)12-22(11-13-3-1-2-4-18(13)24)15-5-7-20(26)17(10-15)21(27)28/h1-10,23-26H,11-12H2,(H,27,28)
• Clé InChI: ULTTYPMRMMDONC-UHFFFAOYSA-N

Description

Description générale

A cell-permeable, reversible, and substrate competitive inhibitor of EGF receptor tyrosine kinase (IC₅₀ = 11 nM) and p60^c-src (IC₅₀ = 500 nM) with little effect on protein kinase A or protein kinase C (IC₅₀ >200 µM). Also inhibits NMDA-stimulated cGMP production (IC₅₀ = 30 nM). Exhibits anti-proliferative properties. Suppresses the angiogenic action of vascular endothelial growth factor (VEGF) in rats.

A cell-permeable, reversible, substrate competitive, and potent inhibitor of EGF receptor tyrosine kinase (IC₅₀ = 11 nM) and pp60^c-src (IC₅₀ = 500 nM) with little effect on protein kinase A or protein kinase C (IC₅₀ >200 µM). Also inhibits NMDA-stimulated cGMP production (IC₅₀ = 30 nM). Exhibits anti-proliferative properties. Suppresses the angiogenic action of vascular endothelial growth factor in rats.

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
EGF receptor tyrosine kinase

Product does not compete with ATP.

Reversible: yes

Target IC₅₀: 11 nM and 500 nM against EGF receptor tyrosine kinase and p60c-src, respectively

Avertissement

Toxicity: Standard Handling (A)

Notes préparatoires

Further dilute with aqueous buffer just prior to use.

Reconstitution

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

Autres remarques

Hu, D.E., and Fan, T.-P. 1995. Br. J. Pharmacol. 114, 262.
Rodriguez, J., et al. 1994. Neuropharmacology 33, 1267.
Hsu, C.-Y., et al. 1991. J. Biol. Chem.266, 21105.
O’Dell, T.J., et al. 1991. Nature 353, 558; Onoda, T., et al. 1989. J. Nat. Prod.52, 1252.
Bishop, J.M. 1983. Annu. Rev. Biochem. 52, 307.

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable