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
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About This Item
Empirical Formula (Hill Notation):
C19H15N3O3S2
CAS Number:
Molecular Weight:
397.47
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥94% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze, protect from light
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
SMILES string
[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+
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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
HER2
HER2
Product does not compete with ATP.
Reversible: yes
Target IC50: 0.35 µM against HER2
Preparation Note
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.
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
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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Global Trade Item Number
| SKU | GTIN |
|---|---|
| 121765-2MG | 07790788047917 |