Tyrphostin AG 879
Tyrphostin AG 879 structure
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Common Name | Tyrphostin AG 879 | ||
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| CAS Number | 148741-30-4 | Molecular Weight | 316.461 | |
| Density | 1.1±0.1 g/cm3 | Boiling Point | 432.7±55.0 °C at 760 mmHg | |
| Molecular Formula | C18H24N2OS | Melting Point | 232 °C | |
| MSDS | Chinese USA | Flash Point | 215.5±31.5 °C | |
Use of Tyrphostin AG 879TyrphostinAG879 is a tyrosine kinase inhibitor that inhibits TrKA phosphorylation, but not TrKB and TrKC.[1] also a ErbB2 kinase inhibitor, has at least 500-fold higher selectivity to ErbB2 (IC50 = 1 μmol/L) than EGFR (IC50 >500 μmol/L).target: TrKA [1], ErbB2 [2].IC 50: ErbB2 1 μmol/L [2].In vitro: TyrphostinAG879 significantly inhibit the A-type potassium currents in the cultured hippocampus neurons.[2] TyrphostinAG879 can reduce gephyrin puncta in GABAergic neurons and PSD-95 puncta in glutamatergic neurons where ErbB4 expression was low. [3] In vivo: Treatment with TyrphostinAG879 in immunodepressed mice graft with leiomyosarcoma or promyelocytic leukemia cells result in dramatic reductions in tumor sizes. [1] |
| Name | (E)-3-amino-2-[(3,5-ditert-butyl-4-oxocyclohexa-2,5-dien-1-ylidene)methyl]-3-sulfanylprop-2-enenitrile |
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| Synonym | More Synonyms |
| Description | TyrphostinAG879 is a tyrosine kinase inhibitor that inhibits TrKA phosphorylation, but not TrKB and TrKC.[1] also a ErbB2 kinase inhibitor, has at least 500-fold higher selectivity to ErbB2 (IC50 = 1 μmol/L) than EGFR (IC50 >500 μmol/L).target: TrKA [1], ErbB2 [2].IC 50: ErbB2 1 μmol/L [2].In vitro: TyrphostinAG879 significantly inhibit the A-type potassium currents in the cultured hippocampus neurons.[2] TyrphostinAG879 can reduce gephyrin puncta in GABAergic neurons and PSD-95 puncta in glutamatergic neurons where ErbB4 expression was low. [3] In vivo: Treatment with TyrphostinAG879 in immunodepressed mice graft with leiomyosarcoma or promyelocytic leukemia cells result in dramatic reductions in tumor sizes. [1] |
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| Related Catalog | |
| References |
| Density | 1.1±0.1 g/cm3 |
|---|---|
| Boiling Point | 432.7±55.0 °C at 760 mmHg |
| Melting Point | 232 °C |
| Molecular Formula | C18H24N2OS |
| Molecular Weight | 316.461 |
| Flash Point | 215.5±31.5 °C |
| Exact Mass | 316.160919 |
| PSA | 102.13000 |
| LogP | 4.76 |
| Vapour Pressure | 0.0±1.1 mmHg at 25°C |
| Index of Refraction | 1.600 |
| Storage condition | Store at -20°C |
| Water Solubility | DMSO: at 26 mg/mlsoluble |
| Personal Protective Equipment | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
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| RIDADR | NONH for all modes of transport |
| WGK Germany | 3 |
| HS Code | 2930909090 |
| HS Code | 2930909090 |
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| Summary | 2930909090. other organo-sulphur compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0% |
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Initiation of testicular tubulogenesis is controlled by neurotrophic tyrosine receptor kinases in a three-dimensional Sertoli cell aggregation assay.
Reproduction 136 , 459-69, (2008) The first morphological sign of testicular differentiation is the formation of testis cords. Prior to cord formation, newly specified Sertoli cells establish adhesive junctions, and condensation of so... |
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Comparison of delphinidin, quercetin and (-)-epigallocatechin-3-gallate as inhibitors of the EGFR and the ErbB2 receptor phosphorylation.
Mol. Nutr. Food. Res. 52(7) , 815-22, (2008) In the present study, delphinidin was found to suppress the phosphorylation of the epidermal growth factor receptor (EGFR) within human tumour cells (human colon carcinoma cell line (HT29), human vulv... |
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The Tyr-kinase inhibitor AG879, that blocks the ETK-PAK1 interaction, suppresses the RAS-induced PAK1 activation and malignant transformation.
Cancer Biol. Ther. 3(1) , 96-101, (2004) AG 879 has been widely used as a Tyr kinase inhibitor specific for ErbB2 and FLK-1, a VEGF receptor. The IC(50) for both ErbB2 and FLK-1 is around 1 microM. AG 879, in combination of PP1 (an inhibitor... |
| AG 879 |
| 2-Propenethioamide, 3-(3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl)-2-cyano-, (E)- |
| BMK1-D4 |
| 2-Propenethioamide, 3-[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]-2-cyano-, (2E)- |
| (2E)-2-Cyano-3-[4-hydroxy-3,5-bis(2-methyl-2-propanyl)phenyl]-2-propenethioamide |
| 2-Propenethioamide,3-[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]-2-cyano-,(2E) |
| Lopac-T-2067 |
| Tyrphostin AG 879 |
| (2E)-2-Cyano-3-(3,5-di-tert-butyl-4-hydroxyphenyl)prop-2-enethioamide |