Description
AG-213 is an inhibitor of protein tyrosine kinases (PTKs) and epidermal growth factor (EGF) receptor kinase [1,2]. Protein tyrosine kinases (PTKs) have been involved in regulating cell proliferation, cell differentiation, and signaling processes in the immune system. Dysfunction of protein tyrosine kinases result in inflammatory responses and diseases including cancer, atherosclerosis, and psoriasis . The epidermal growth factor receptor (EGFR) is a transmembrane glycoprotein. Activation of EGFR results in autophosphorylation of receptor tyrosine kinase and has been involved in regulating cellular proliferation, differentiation, and survival. Overexpression of EGFR has been identified in a variety of tumor cell lines and has been associated with poor prognosis and decreased survival . Administration of AG 213(100 μM) interfered with HUVEC focal adhesion and stress fiber formation. Pretreatment of monolayers with AG 213 (25, 50, and 75 μM) produced partial and incremental inhibition of HUVEC migration. In HUVEC, treatment with tyrphostin AG 213 (25 and 50 μM) demonstrated partial inhibition of stress fiber assembly compared with cells treated with 100 μM AG 213 . AG 213 inhibited adhesion-associated tyrosine phosphorylation of pp125FAK activity in HUVEC . AG-213 inhibited the activity of epidermal growth factor (EGF) receptor kinase with an IC50 value of 2.4 μM in the human epidermoid carcinoma cell line A431 .
Product information
CAS Number: 122520-86-9
Molecular Weight: 220.25
Formula: C10H8N2O2S
Chemical Name: (2E)-2-cyano-3-(3,4-dihydroxyphenyl)prop-2-enethioamide
Smiles: NC(=S)/C(=C/C1=CC(O)=C(O)C=C1)/C#N
InChiKey: ZGHQGWOETPXKLY-XVNBXDOJSA-N
InChi: InChI=1S/C10H8N2O2S/c11-5-7(10(12)15)3-6-1-2-8(13)9(14)4-6/h1-4,13-14H,(H2,12,15)/b7-3+
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
Products are for research use only. Not for human use.
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