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| Product Name: | AG 213 | | Synonyms: | ALPHA-CYANO-3,4-DIHYDROXYTHIOCINNAMAMIDE;ALPHA-CYANO-(3,4-DIHYDROXY)THIOCINNAMIDE;AG 213;3,4-DIHYDROXY-ALPHA-CYANOTHIOCINNAMAMIDE;(E)-2-CYANO-3-(3,4-DIHYDROXYPHENYL)-2-PROPENTHIOAMIDE;TYRPHOSTIN A47 99+%;AG 213 (Tyrphostin AG 213);ZGHQGWOETPXKLY-XVNBXDOJSA-N | | CAS: | 122520-86-9 | | MF: | C10H8N2O2S | | MW: | 220.25 | | EINECS: | | | Product Categories: | Intracellular Signaling;Protein Kinase | | Mol File: | 122520-86-9.mol |  |
| | AG 213 Chemical Properties |
| Melting point | 213 °C | | Boiling point | 474.5±55.0 °C(Predicted) | | density | 1.512±0.06 g/cm3(Predicted) | | storage temp. | 2-8°C | | solubility | DMSO: 50 mg/mL, clear, orange | | form | Orange solid. | | pka | 8.82±0.10(Predicted) |
| | AG 213 Usage And Synthesis |
| 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. |
| | AG 213 Preparation Products And Raw materials |
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