A selective ATP-competitive inhibitor of the tyrosine kinase activity of HER2/neu (IC50 = 0.35 µM)

AG-825 – 50 mg

Brand:
Cayman
CAS:
149092-50-2
Storage:
-20
UN-No:
Non-Hazardous - /

The HER2/Neu proto-oncogene is a member of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases (RTK) which includes EGFR, HER2/Neu, HER3 and HER4.{15161} Overexpression of HER2/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 HER2/Neu. In cell-free assays, AG-825 inhibits Her2/Neu, EGFR, and PDGFR autophosphorylation with IC50 values of 0.35, 19, and 40 µM, respectively.{15151} However, in select whole cells, the high concentration of ATP prevents inhibition of kinase activity by AG-825.{15151} Concentrations of 50 µM AG-825, however, consistently inhibit Her2/Neu signalling and promote killing of human LNCaP, C4, and C4-2 prostate cancer cells.{15152}  

 

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SKU: 10010243 - 50 mg Category:

Description

A selective ATP-competitive inhibitor of the tyrosine kinase activity of HER2/neu (IC50 = 0.35 µM)

Formal name: 3-[3-[(2-benzothiazolylthio)methyl]-4-hydroxy-5-methoxyphenyl]-2-cyano-2-propenamide

Synonyms:  Tyrphostin AG-825

Molecular weight: 397.5

CAS: 149092-50-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|EGFR/ErbB/HER Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling

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