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121765

Sigma-Aldrich

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.

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Synonym(s):
AG 825, 4-Hydroxy-3-methoxy-5-(benzothiazolylthiomethyl)benzylidenecyanoacetamide
Empirical Formula (Hill Notation):
C19H15N3O3S2
CAS Number:
Molecular Weight:
397.47
MDL number:

Quality Level

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

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 p185neu.
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 p185neu.

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

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


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