See personalized New Product recommendations! Get personalized New Product recommendations! Register or Login for personalized New Product recommendations!

Join us! · InformexUSA 2012 · New Orleans, Louisiana · February 14-17, 2012 · Booth 2514

AG-825

Cayman Chemical Item Number 10010243

Tyrphostin AG-825 (CAS 149092-50-2)

AG-825 (CAS 149092-50-2)

See more

Description

The HER-2/neu proto-oncogene is a member of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases (RTK) which includes EGFR, HER-2/neu, HER-3 and HER-4.1 Overexpression of HER-2/neu occurs in 25-30% of human breast and ovarian cancer. AG-825 is a selective ATP-competitive inhibitor of the tyrosine kinase activity of HER-2/neu. In cell-free assays, AG-825 inhibits Her-2/neu, EGFR, and PDGFR autophosphorylation with IC50 values of 0.35, 19, and 40 µM, respectively.2 However, in select whole cells, the high concentration of ATP prevents inhibition of kinase activity by AG-825.2 Concentrations of 50 µM AG-825, however, consistently inhibit Her-2/neu signalling and promote killing of human LNCaP, C4, and C4-2 prostate cancer cells.3

1 Reese, D.M., and Slamon, D.J. HER-2/neu signal transduction in human breast and ovarian cancer. Stem Cells 15 1-8 (1997).

2 Osherov, N., Gazit, A., Gilon, C., et al. Selective inhibition of the epidermal growth factor and HER2/Neu receptors by tyrphostins. J Biol Chem 268(15) 11134-11142 (1993).

3 Murillo, H., Schmidt, L.J., and Tindall, D.J. Tyrphostin AG825 triggers p38 mitogen-activated protein kinase-dependent apoptosis in androgen-independent prostate cancer cells C4 and C4-2. Cancer Res 61 7408-7412 (2001).

Synonyms
  • Tyrphostin AG-825
Formal Name 3-​[3-​[(2-​benzothiazolylthio)methyl]-​4-​hydroxy-​5-​methoxyphenyl]-​2-​cyano-​2-​propenamide
CAS Number 149092-50-2
Molecular Formula C19H15N3O3S2
Formula Weight 397.5
Formulation A crystalline solid
Purity >98%
λmax 225, 361 nm
Stability 2 years
Storage -20°C
Shipping Wet ice in continental US; may vary elsewhere
SMILES
Copy SMILES to clipboard
N#C/C(=C\c1cc(CSc2nc3ccccc3s2)​c(O)​c(OC)​c1)​/C(=O)​N

Background Reading

Reese, D.M., and Slamon, D.J. HER-2/neu signal transduction in human breast and ovarian cancer. Stem Cells 15 1-8 (1997).

Osherov, N., Gazit, A., Gilon, C., et al. Selective inhibition of the epidermal growth factor and HER2/Neu receptors by tyrphostins. J Biol Chem 268(15) 11134-11142 (1993).

Murillo, H., Schmidt, L.J., and Tindall, D.J. Tyrphostin AG825 triggers p38 mitogen-activated protein kinase-dependent apoptosis in androgen-independent prostate cancer cells C4 and C4-2. Cancer Res 61 7408-7412 (2001).

AG-825 is available in the following screening library:

Size Price Quantity Subtotal
1 mg $62.00 $0.00
5 mg $279.00 $0.00
10 mg $496.00 $0.00
50 mg $2,170.00 $0.00
Bulk Contact
Cart Total $0.00

This product is available in custom sizes and/or larger quantities.

Please contact our Sales Department for a quote or to purchase.

Pricing updated 2012-02-12. Prices are subject to change without notice.

To ask for assistance with one of our products please contact a Technical Support Scientist.

Warning This product is not for human or veterinary use.

Related Products

AG-1296
AG-1478
AG-17
AG-18
AG-183
AG-490
AG-494
AG-82
AG-879
AG-99
LFM-A13
RG-13022
RG-14620
ZM 336372
Show all 14 Hide all but first 3

Downloads

Batch-specific Information

Login to access batch-specific information

Cayman Chemical is a manufacturer, supplier and vendor of biochemical reagents, assay kits, antibodies, and proteins.

Other Resources
Management Team Company Profile Company History ChemAssistant Tools FAQs Cayman Europe Cayman Pharma CaBRI Cayman Gear Press Releases Illustrations and Charts Key Research Area Posters Article Library Analysis Tools Conference Schedule Order Terms Browser Recommendation Privacy Statement Site Map

Cayman Chemical Company · 1180 East Ellsworth Road · Ann Arbor, Michigan 48108 · USA

Toll Free: (800) 364-9897 (USA and Canada Only) · Fax: (734) 971-3640

Copyright 2012 Cayman Chemical Company

Lost password?