trans-4-Dimethylaminocrotonic Acid Hydrochloride CAS 848133-35-7 Purity >98.0% (HPLC) Afatinib Dimaleate Intermediate
I-Ruifu Chemical Supply Intermediates ye-Afatinib
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Igama Lekhemikhali | I-trans-4-Dimethylaminocrotonic Acid Hydrochloride |
Omqondofana | i-trans 4-Dimethylaminocrotonic Acid HCl;(E) -4-(Dimethylamino) -2-Butenoic Acid Hydrochloride;(E)-4-Dimethylaminocrotonic Acid Hydrochloride;(2E) -4-(Dimethylamino) kodwa-2-Enoic Acid Hydrochloride;I-Afatinib int-2 |
Inombolo ye-CAS | 848133-35-7 |
Isimo Sesitoko | Esitokweni, Isikali Sokuhweba |
I-Molecular Formula | I-C6H12ClNO2 |
Isisindo samangqamuzana | 165.62 |
Ukuzwela | I-Hygroscopic.Kuyazwela Umswakama |
I-Melting Point | 160.0 ukuze 164.0 ℃ |
Ukuncibilika | I-DMSO (Kancane), i-Methanol (Kancane), Amanzi (Kancane) |
I-COA ne-MSDS | Iyatholakala |
Umsuka | Shanghai, China |
Ibhrendi | I-Ruifu Chemical |
Into | Imininingwane |
Ukubukeka | Impushana Emhlophe Kuya Kucishe Emhlophe |
Ukuhlanzeka / Indlela Yokuhlaziya | >98.0% (HPLC) |
Ukuhlanzeka / Indlela Yokuhlaziya | >98.0% (NMR) |
Umswakama (KF) | <0.50% |
Izinsalela ekushiseni | <0.20% |
Ukungcola Okukodwa | <0.50% |
Izinsimbi Ezisindayo (njenge-Pb) | <20ppm |
I-Infrared Spectrum | Ivumelana Nesakhiwo |
1 H NMR Spectrum | I-Proton NMR Spectrum |
Izinga Lokuhlola | I-Enterprise Standard |
Ukusetshenziswa | I-Intermediate ye-Afatinib, i-Afatinib Dimaleate |
Iphakheji:Ibhodlela, isikhwama se-Aluminium foil, 25kg/Cardboard Drum, noma ngokwezidingo zekhasimende.
Isimo Sesitoreji:Gcina ezitsheni ezivaliwe endaweni epholile neyomile;Vikela ekukhanyeni nakumswakama.
Ukuthumela:Zilethe emhlabeni wonke ngendiza, yi-FedEx/DHL Express.Nikeza ukulethwa okusheshayo nokuthembekile.
Ithuluzi: I-Agilent 1200 HPLC HPLC chromatograph, umtshina we-DAD.
Ikholomu: I-Agilent XDB-C18,250*4.6mm, 5μm
Isigaba seselula: B: 1.95g sodium octane sulfonate + 8ml phosphoric acid + 5ml triethylamine + 500ml amanzi
C: i-acetonitrile
Ukulungiswa kwesigaba seselula esixubile: thatha isixazululo esingu-400ml B kanye ne-100ml acetonitrile, hlanganisa kahle futhi ngokulinganayo, bese umpompa uketshezi ngesigaba esisodwa.
Izinga lokugeleza: 0.5ml/min54bar
Izinga lokushisa lekholomu: 25℃
Ubude begagasi: 210nm
Isixazululo sesampula: isigaba seselula sisetshenziswe njenge-solvent, isampula eqinile: 0.0040g/2ml, usayizi wesampula 2.0μl.
I-trans-4-Dimethylaminocrotonic Acid Hydrochloride (i-CAS: 848133-35-7) i-reagent esetshenziselwa ukulungiswa kwe-tyrosine kinase inhibiting antitumor agents.I-trans-4-Dimethylaminocrotonic Acid Hydrochloride ingasetshenziswa njenge-intermediate ye-Afatinib (CAS: 439081-18-2), i-Afatinib Dimaleate (CAS: 850140-73-7), i-Neratinib (CAS: 698387-09-6).I-Afatinib isidakamizwa esigunyazwe ukwelashwa kwe-non-small cell lung carcinoma (NSCLC), esakhiwe ngu-Boehringer Ingelheim.Isebenza njenge-angiokinase inhibitor.NjengeLapatinib neNeratinib, i-Afatinib iyi-tyrosine kinase inhibitor (TKI) ephinde ivimbele ngendlela engenakulungiseka i-epidermal growth factor receptor 2 (Her2) kanye ne-epidermal growth factor receptor (EGFR) kinases.I-Afatinib ayisebenzi kuphela ngokumelene ne-EGFRizinguquko eziqondiswe isizukulwane sokuqala se-TKIs likeerlotinib noma i-gefitinib, kodwa futhi ngokumelene nalezo ezingazweli kulezi zindlela zokwelapha ezijwayelekile.Ngenxa yomsebenzi wayo owengeziwe ngokumelene ne-Her2, kuphenywa umdlavuza webele kanye neminye imidlavuza eqhutshwa yi-EGFR kanye ne-Her2.I-Neratinib eyakhiwe inkampani yase-US Wyeth iyi-epidermal growth factor receptor (EGFR) inhibitor engalungiseki.Iphuzu eliqondiwe kaningi le-molecule encane i-tyrosine kinase inhibitors eya ku-HER 2 ne-HER1 ngemva kwe-Lapatinib, futhi iyi-ErbB receptor tyrosine kinase inhibitor engabuyiseleki emuva.I-Neratinib ingavimbela ngokukhetha i-HER-1 kanye ne-HER-2 yomndeni we-EGFR(IC50 yayingu-92 nmol/L kanye no-59 nmol/L, ngokulandelanayo).Ucwaningo lwezokwelapha lubonise ukuthi i-Neratinib ibe nomthelela omkhulu wokwelapha kumdlavuza wamaphaphu ongewona omncane, umdlavuza wekoloni, kanye nomdlavuza webele.Uhlolo lwe-phaseⅡclinical lubonise ukuthi i-Neratinib ibonise ukusebenza kahle nokubekezelelana ezigulini ezine-HER-2 ezinomdlavuza webele othuthukisiwe ezake zathola ukwelashwa kwe-Trastuzumab noma cha.Isigaba Ⅲ sokuhlolwa komtholampilo womdlavuza webele saqedwa ngoSepthemba 2014.