| Identification | Back Directory | [Name]
AG 213 | [CAS]
122520-86-9 | [Synonyms]
AG 213
RG-50864
TYRPHOSTIN 47
TYRPHOSTIN A47
AG 213 USP/EP/BP
TYRPHOSTIN AG 213
TYRPHOSTIN RG 50864
TYRPHOSTIN A47 99+%
AG 213 (Tyrphostin AG 213)
ZGHQGWOETPXKLY-XVNBXDOJSA-N
3,4-DIHYDROXY-ALPHA-CYANOTHIOCINNAMAMIDE
ALPHA-CYANO-3,4-DIHYDROXYTHIOCINNAMAMIDE
ALPHA-CYANO-(3,4-DIHYDROXY)THIOCINNAMIDE
(E)-2-CYANO-3-(3,4-DIHYDROXYPHENYL)-2-PROPENTHIOAMIDE
3-amino-2-[(3-hydroxy-4-oxocyclohexa-2,5-dien-1-ylidene)methyl]-3-sulfanylprop-2-enenitrile | [Molecular Formula]
C10H8N2O2S | [MDL Number]
MFCD00133902 | [MOL File]
122520-86-9.mol | [Molecular Weight]
220.25 |
| Hazard Information | Back Directory | [Description]
Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds that act as PTK blockers. PTK inhibitors which preferentially inhibit the epidermal growth factor (EGF) receptor kinase block EGF-dependent cell proliferation. AG-213 is an inhibitor of epidermal growth factor (EGF) receptor kinase with an IC50 value of 2.4 μM in the human epidermoid carcinoma cell line A431. | [Uses]
Tyrphostin 47 is a potent inhibitor of EGFR kinase activity. | [Definition]
ChEBI: 3-amino-2-[(3-hydroxy-4-oxo-1-cyclohexa-2,5-dienylidene)methyl]-3-mercapto-2-propenenitrile is a member of quinomethanes. | [Biological Activity]
Epidermal growth factor receptor (EGFR) and platelet-derived growth factor receptor (PDGFR) kinase inhibitor (IC 50 values are 2.4 and 3 μ M respectively). Stimulates microtubule polymerization and promotes neurite outgrowth > 17-fold over basal conditions in vitro . Also weakly inhibits protein kinase C (IC 50 = 60 μ M). | [References]
[1] romer l h, mclean n, turner c e, et al. tyrosine kinase activity, cytoskeletal organization, and motility in human vascular endothelial cells[j]. molecular biology of the cell, 1994, 5(3): 349-361.
[2] gazit a, yaish p, gilon c, et al. tyrphostins i: synthesis and biological activity of protein tyrosine kinase inhibitors[j]. journal of medicinal chemistry, 1989, 32(10): 2344-2352.
[3] levitzki a, gazit a. tyrosine kinase inhibition: an approach to drug development[j]. science, 1995, 267(5205): 1782.
[4] herbst r s. review of epidermal growth factor receptor biology[j]. international journal of radiation oncology biology physics, 2004, 59(2): s21-s26. |
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