121765

AG 825

A potent, cell-premeable, reversible, substrate competitive, and selective inhibitor of HER2 (neu/ErbB2; IC₅₀ = 0.35 µM) relative to HER1 (IC₅₀= 19 µM) autophosphorylation.

• Synonyme(s) : AG 825, 4-Hydroxy-3-methoxy-5-(benzothiazolylthiomethyl)benzylidenecyanoacetamide
• Formule empirique (notation de Hill): C₁₉H₁₅N₃O₃S₂
• Numéro CAS: 149092-50-2
• Poids moléculaire : 397.47
• Numéro MDL: MFCD01074971
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Pureté: ≥94% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: yellow
• Solubilité: DMSO: 10 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: −20°C
• InChI: 1S/C19H15N3O3S2/c1-25-15-8-11(6-12(9-20)18(21)24)7-13(17(15)23)10-26-19-22-14-4-2-3-5-16(14)27-19/h2-8,23H,10H2,1H3,(H2,21,24)/b12-6+
• Clé InChI: KXDONFLNGBQLTN-WUXMJOGZSA-N

Description

Description générale

A potent, cell-premeable, reversible, substrate competitive, and selective inhibitor of HER-2 (neu/erbB-2, IC₅₀ = 0.35 µM) relative to HER-1 (IC₅₀ = 19 µM) autophosphorylation. The inhibition is competitive with respect to ATP binding. Enhances the chemosensitivity in non-small cell lung cancer (NSCLC) cell lines expressing high levels of p185^neu.

A potent, cell-premeable, reversible, substrate competitive, and selective inhibitor of HER2 (neu/ErbB2; IC₅₀ = 0.35 µM) relative to HER1 (IC₅₀ = 19 µM) autophosphorylation. The inhibition is competitive with respect to ATP binding. Enhances chemosensitivity in non-small cell lung cancer (NSCLC) cell lines expressing high levels of p185^neu.

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
HER2

Product does not compete with ATP.

Reversible: yes

Target IC₅₀: 0.35 µM against HER2

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 2-3 months at -20°C.

Autres remarques

Ashton, J.M., et al. 2012. Cell Stem Cell11, 359.
Tsai, C.M., et al. 1996. Cancer Res.56, 1068.
Levitzki, A., and Gazit, A. 1995. Science267, 1782.
Osherov, N., et al. 1993. J. Biol. Chem. 268, 11134.

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