| Identification | Back Directory | [Name]
TYRPHOSTIN B46 | [CAS]
133550-34-2 | [Synonyms]
AG 555
AG 555, >98%
TYRPHOSTIN B46
TYRPHOSTIN AG 555
TYRPHOSTIN AG 555, >98%
AG 555 (Tyrphostin AG 555)
TYRPHOSTIN AG 555;TYRPHOSTIN AG-555;TYRPHOSTIN AG555
N-(3-PHENYLPROPYL)-3,4-DIHYDROXY-ALPHA CYANOCINNAMIDE
ALPHA-CYANO-(3,4-DIHYDROXY)-N-(3-PHENYLPROPYL)CINNAMIDE
N-(3'-PHENYLPROPYL)-3,4-DIHYDROXYBENZYLIDENECYANOACETAMIDE
(E)-2-CYANO-3-(3,4-DIHYDROXYPHENYL)-N-(3-PHENYLPROPYL)-2-PROPENAMIDE
2-Propenamide,2-cyano-3-(3,4-dihydroxyphenyl)-N-(3-phenylpropyl)-, (2E)-
Tyrphostin B46, N-(3μ-Phenylpropyl)-3,4-dihydroxybenzylidenecyanoacetamide | [Molecular Formula]
C19H18N2O3 | [MDL Number]
MFCD00209865 | [MOL File]
133550-34-2.mol | [Molecular Weight]
322.36 |
| Chemical Properties | Back Directory | [Boiling point ]
621.1±55.0 °C(Predicted) | [density ]
1.273±0.06 g/cm3(Predicted) | [storage temp. ]
Inert atmosphere,Store in freezer, under -20°C | [solubility ]
DMSO or ethanol: soluble
| [form ]
Powder | [pka]
8.82±0.10(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Description]
AG-555 is a tyrphostin inhibitor of the EGF receptor (EGFR; IC50 = 0.7 μM). It selectively inhibits EFGR over ErbB2 (IC50 = 35 μM). AG-555 inhibits EGF-dependent growth of HER 14 cells (IC50 = 2.5 μM) as well as the growth of psoriatic keratinocytes isolated from patients with psoriasis when used at concentrations ranging from 1 to 50 μM. It also inhibits Moloney murine leukemia virus (Mo-MuLV) reverse transcriptase activity (IC50 = 10.8 μM) without affecting Mo-MuLV-infected NIH3T3 cell growth (IC50 = 210 μM). | [Uses]
Inhibitor of EGF receptor kinase activity | [Biological Activity]
Potent epidermal growth factor receptor (EGFR) kinase inhibitor (IC 50 = 0.7 μ M) that displays 50-fold and >140-fold selectivity over ErbB2 and insulin receptor kinase respectively. Induce G 1 growth arrest selectively in transformed cells (IC 50 values are 6.4 and 9.4 μ M in HPV16-immortalized and normal keratinocytes respectively). | [References]
[1]. ben-bassat h, rosenbaum-mitrani s, hartzstark z, et al. inhibitors of epidermal growth factor receptor kinase and of cyclin-dependent kinase 2 activation induce growth arrest, differentiation, and apoptosis of human papilloma virus 16-immortalized human keratinocytes. cancer res, 1997, 57(17): 3741-3750.
[2]. kleinberger-doron n, shelah n, capone r, et al. inhibition of cdk2 activation by selected tyrphostins causes cell cycle arrest at late g1 and s phase. exp cell res, 1998, 241(2): 340-351.
[3]. sion-vardy n, vardy d, rodeck u, et al. antiproliferative effects of tyrosine kinase inhibitors (tyrphostins) on human bladder and renal carcinoma cells. j surg res, 1995, 59(6): 675-680.
[4]. seri i, aflalo e, gazit a, et al. tyrphostin ag-555 inhibits early and late stages of moloney murine leukemia virus replication cycle. int j oncol, 1997, 10(6): 1185-1189. |
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| Company Name: |
Spectrum Chemical Manufacturing Corp.
|
| Tel: |
021-021-021-67601398-809-809-809 15221380277 |
| Website: |
www.spectrumchemical.com/oa_html/index.jsp?minisite=10020&respid=22372&language=us |
| Company Name: |
SPIRO PHARMA
|
| Tel: |
|
| Website: |
www.spiropharma.com.cn |
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