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Merck
CN

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.

别名:

AG 825, 4-Hydroxy-3-methoxy-5-(benzothiazolylthiomethyl)benzylidenecyanoacetamide

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关于此项目

经验公式(希尔记法):
C19H15N3O3S2
化学文摘社编号:
分子量:
397.47
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
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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

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

Quality Level

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
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.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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