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.

• Sinonimo/i: AG 825, 4-Hydroxy-3-methoxy-5-(benzothiazolylthiomethyl)benzylidenecyanoacetamide
• Formula empirica (notazione di Hill): C₁₉H₁₅N₃O₃S₂
• Numero CAS: 149092-50-2
• Peso molecolare: 397.47
• Numero MDL: MFCD01074971
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Livello qualitativo: 100
• Saggio: ≥94% (HPLC)
• Stato: solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; protect from light
• Colore: yellow
• Solubilità: DMSO: 10 mg/mL
• Condizioni di spedizione: ambient
• Temperatura di conservazione: −20°C
• Stringa SMILE: [s]1c2c(nc1SCc3c(c(cc(c3)\C=C(\C(=O)N)/C#N)OC)O)cccc2
• 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+; KXDONFLNGBQLTN-WUXMJOGZSA-N

Descrizione

Descrizione generale

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.

Azioni biochim/fisiol

Cell permeable: yes

Primary Target
HER2

Product does not compete with ATP.

Reversible: yes

Target IC₅₀: 0.35 µM against HER2

Attenzione

Toxicity: Standard Handling (A)

Ricostituzione

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

Altre note

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.

Note legali

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

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 3
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable