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| | TYRPHOSTIN AG 879 Basic information |
| Product Name: | TYRPHOSTIN AG 879 | | Synonyms: | 2-Propenethioamide, 3-[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]-2-cyano-, (E)-;AG-879 100MG;TYRPHOSTIN 879;TYRPHOSTIN AG 879;(3,5-DI-T-BUTYL-4-HYDROXYBENZYLIDENE)THIOCYANOACETAMIDE;AG 879;ALPHA-CYANO-(3,5-DI-T-BUTYL-4-HYDROXY)THIOCINNAMIDE;ALPHA-CYANO-(3,5-DI-TERT-BUTYL-4-HYDROXY)THIOCINNAMAMIDE | | CAS: | 148741-30-4 | | MF: | C18H24N2OS | | MW: | 316.46 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 148741-30-4.mol |  |
| | TYRPHOSTIN AG 879 Chemical Properties |
| Boiling point | 432.7±55.0 °C(Predicted) | | density | 1.127±0.06 g/cm3(Predicted) | | storage temp. | Keep in dark place,Sealed in dry,Store in freezer, under -20°C | | solubility | DMSO: at 26 mg/mlsoluble | | pka | 9.63±0.70(Predicted) | | form | Orange-yellow solid | | color | Yellow | | Stability: | Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months. |
| WGK Germany | 3 | | HS Code | 29309090 |
| | TYRPHOSTIN AG 879 Usage And Synthesis |
| Description | AG-879 (148741-30-4) inhibits NGF-induced neurite growth in PC12 cells via selective inhibition of NGF receptor(pp140c-trk) autophosphorylation (IC50 = 10 μM). No inhibition of EGF, or PDGF receptor phosphorylation is observed at typical working concentrations. | | Uses | Tyrphostin AG 879 is a dual EGFR/HER2 inhibitor that was administered together with androgen withdrawal therapy and was shown to sensitize prostate cancer cells to apoptosis. | | Definition | ChEBI: 3-amino-2-[(3,5-ditert-butyl-4-oxo-1-cyclohexa-2,5-dienylidene)methyl]-3-mercapto-2-propenenitrile is a monoterpenoid. | | in vitro | ag 879 has been widely used as a tyr kinase inhibitor specific for erbb2 and flk-1, a vegf receptor. the ic50 value for erbb2 and flk-1 was approximately 1 μm. ag 879 at 10 nm blocked the specific interaction between the tyr-kinase etk and pak1 (a cdc42/rac-dependent ser/thr kinase) in cell culture. ag 879 (10 nm) showed no inhibitory effects on the purified etk and pak1 directly in vitro, suggesting that this drug blocked the etk-pak1 pathway by targeting the highly sensitive kinase upstream of etk. src was insensitive to ag 879. fak was inhibited by 100 nm ag 879, but not by 10 nm ag879 [2]. ag 879 inhibited proliferation of human breast cancer cells through an effect involving inhibition of map kinase activation. ag 879 markedly inhibited the expression of the raf-1 gene, which encoded an upstream mapkkk. additionally, ag 879 inhibited the expression of her-2[3]. treatment with ag879 (20 μm) dramatically decreased proliferation with a variable increase in apoptosis in cell lines from human leiomyosarcoma (htb-114, htb-115, htb-88), rhabdomyosarcoma (htb-82, te-671), prostatic adenocarcinoma (pc-3), acute promyelocytic leukemia (hl-60) and histiocytic lymphoma (u-937) [4]. | | in vivo | in athymic nod/scid mice grafted with htb-114 or hl-60, administration of ag879 at 2 mg induced a decrease in cancer growth [4]. ag 879 administration (20 mg/kg) kept 50% of mice absolutely free of ras-induced sarcomas. in the nude mice carrying v-ha-ras transformed nih 3t3 cells, ag 879 dramatically reduced the size of the growing sarcomas [5]. | | References | 1) Ohmichi et al. (1993), The tyrosine kinase inhibitor tyrphostin blocks the cellular actions of nerve growth factor; Biochemistry, 32 4650 |
| | TYRPHOSTIN AG 879 Preparation Products And Raw materials |
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