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.

• Synonym(s): AG 825, 4-Hydroxy-3-methoxy-5-(benzothiazolylthiomethyl)benzylidenecyanoacetamide
• Empirical Formula (Hill Notation): C₁₉H₁₅N₃O₃S₂
• CAS Number: 149092-50-2
• Molecular Weight: 397.47
• MDL number: MFCD01074971
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥94% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: yellow
• solubility: DMSO: 10 mg/mL
• shipped in: ambient
• storage temp.: −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+
• InChI key: KXDONFLNGBQLTN-WUXMJOGZSA-N

Description

General description

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.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
HER2

Product does not compete with ATP.

Reversible: yes

Target IC₅₀: 0.35 µM against HER2

Warning

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.

Other Notes

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.

Legal Information

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable