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.

• Sinônimo(s): AG 825, 4-Hydroxy-3-methoxy-5-(benzothiazolylthiomethyl)benzylidenecyanoacetamide
• Fórmula empírica (Notação de Hill): C₁₉H₁₅N₃O₃S₂
• Número CAS: 149092-50-2
• Peso molecular: 397.47
• Número MDL: MFCD01074971
• Código UNSPSC: 12352200
• NACRES: NA.77

Propriedades

• Nível de qualidade: 100
• Ensaio: ≥94% (HPLC)
• Formulário: solid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: yellow
• solubilidade: DMSO: 10 mg/mL
• Condições de expedição: ambient
• temperatura de armazenamento: −20°C
• cadeia de caracteres SMILES: [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+
• chave InChI: KXDONFLNGBQLTN-WUXMJOGZSA-N

Descrição

Descrição geral

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.

Ações bioquímicas/fisiológicas

Cell permeable: yes

Primary Target
HER2

Product does not compete with ATP.

Reversible: yes

Target IC₅₀: 0.35 µM against HER2

Advertência

Toxicity: Standard Handling (A)

Reconstituição

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

Outras notas

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.

Informações legais

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

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable