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| | TYRPHOSTIN B46 Basic information |
| Product Name: | TYRPHOSTIN B46 | | Synonyms: | N-(3-PHENYLPROPYL)-3,4-DIHYDROXY-ALPHA CYANOCINNAMIDE;N-(3'-PHENYLPROPYL)-3,4-DIHYDROXYBENZYLIDENECYANOACETAMIDE;TYRPHOSTIN AG 555;TYRPHOSTIN B46;(E)-2-CYANO-3-(3,4-DIHYDROXYPHENYL)-N-(3-PHENYLPROPYL)-2-PROPENAMIDE;AG 555;ALPHA-CYANO-(3,4-DIHYDROXY)-N-(3-PHENYLPROPYL)CINNAMIDE;Tyrphostin B46, N-(3μ-Phenylpropyl)-3,4-dihydroxybenzylidenecyanoacetamide | | CAS: | 133550-34-2 | | MF: | C19H18N2O3 | | MW: | 322.36 | | EINECS: | | | Product Categories: | Protein Kinase;Intracellular Signaling | | Mol File: | 133550-34-2.mol |  |
| | TYRPHOSTIN B46 Chemical Properties |
| 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 |
| | TYRPHOSTIN B46 Usage And Synthesis |
| 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. |
| | TYRPHOSTIN B46 Preparation Products And Raw materials |
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