trans-4-Dimethylaminocrotonic Acid Hydrochloride CAS 848133-35-7 Ubunyulu >98.0% (HPLC) Afatinib Dimaleate Intermediate
I-Ruifu Chemical Supply Intermediates ye-Afatinib
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Igama leMchiza | i-trans-4-Dimethylaminocrotonic Acid Hydrochloride |
Izithethantonye | 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;Afatinib int-2 |
Inombolo yeCAS | 848133-35-7 |
Ubume beStokhwe | Kwisitokhwe, isikali soRhwebo |
Ifomula yeemolekyuli | I-C6H12ClNO2 |
Ubunzima beMolekyuli | 165.62 |
Uvakalelo | Hygroscopic.Ukungenwa kukufuma |
Indawo yokunyibilika | 160.0 ukuba 164.0℃ |
Ukunyibilika | I-DMSO (Kancinci), iMethanol (Kancinci), Amanzi (Kancinci) |
I-COA kunye ne-MSDS | Iyafumaneka |
Imvelaphi | Shanghai, China |
Uphawu | Ruifu Chemical |
Into | Iinkcukacha |
Imbonakalo | Mhlophe ukuya Phantse uMhlophe |
Ubunyulu / Indlela yokuHlalutya | >98.0% (HPLC) |
Ubunyulu / Indlela yokuHlalutya | >98.0% (NMR) |
Ukufuma (KF) | <0.50% |
Intsalela kwi-Ignition | <0.20% |
Ukungacoceki Okukodwa | <0.50% |
Iintsimbi ezinzima (njenge Pb) | <20ppm |
I-Infrared Spectrum | Iyahambelana neSakhiwo |
I-1 H NMR Spectrum | Proton NMR Spectrum |
Umgangatho woVavanyo | Umgangatho woShishino |
Ukusetyenziswa | Umbindi weAfatinib, Afatinib Dimaleate |
Umqulu:Ibhotile, ingxowa yefoyile yeAluminiyam, 25kg/Igubu lekhadibhodi, okanye ngokwemfuno yomthengi.
Imeko yoGcino:Gcina kwizikhongozeli ezivaliweyo kwindawo epholileyo neyomileyo;Khusela ukukhanya kunye nokufuma.
Ukuhambisa ngenqanawe:Zisa kwihlabathi liphela ngomoya, ngeFedEx / DHL Express.Ukubonelela ngokukhawuleza nangokuthembekileyo.
Isixhobo: I-Agilent 1200 HPLC HPLC chromatograph, i-DAD detector.
Uluhlu: 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 esixubileyo se-mobile: thabatha isisombululo se-400ml B kunye ne-100ml ye-acetonitrile, xuba ngokucokisekileyo kwaye ulungelelanise, kwaye upompe ulwelo kwisigaba esinye.
Isantya sokuhamba: 0.5ml/min54bar
Ubushushu bekholamu: 25℃
Ubude bobude: 210nm
Isisombululo sesampuli: isigaba seselula sisetyenziswe njenge-solvent, isampuli eqinile: 0.0040g / 2ml, ubungakanani besampula 2.0μl.
I-trans-4-Dimethylaminocrotonic Acid Hydrochloride (CAS: 848133-35-7) i-reagent esetyenziselwa ukulungiswa kwe-tyrosine kinase inhibiting agents antitumor.I-trans-4-Dimethylaminocrotonic Acid Hydrochloride ingasetyenziselwa njenge-intermediate ye-Afatinib (CAS: 439081-18-2), i-Afatinib Dimaleate (CAS: 850140-73-7), i-Neratinib (CAS: 698387-09-6).I-Afatinib lichiza elivunyiweyo kunyango lwe-non-small cell lung carcinoma (NSCLC), ephuhliswe ngu-Boehringer Ingelheim.Isebenza njenge-angiokinase inhibitor.NjengeLapatinib kunye neNeratinib, i-Afatinib yi-tyrosine kinase inhibitor (TKI) ekwathintela ngokungenakuguquleka kwi-epidermal growth factor receptor 2 (Her2) kunye ne-epidermal growth factor receptor (EGFR) kinases.I-Afatinib ayisebenzi kuphela kwi-EGFRutshintsho olujoliswe kwisizukulwana sokuqala se-TKIs likeerlotinib okanye i-gefitinib, kodwa nakwabo bangenaluvelwano kolu nyango luqhelekileyo.Ngenxa yomsebenzi wayo owongezelelweyo ngokuchasene ne-Her2, iphandwa umhlaza wamabele kunye neminye imihlaza eqhutywa yi-EGFR kunye ne-Her2.I-Neratinib ephuhliswe yinkampani yase-US Wyeth yi-epidermal growth factor receptor (EGFR) inhibitor engaguqulekiyo.Iyindawo ekujoliswe kuyo emininzi ye-molecule encinci ye-tyrosine kinase inhibitors ukuya kwi-HER 2 kunye ne-HER1 emva kweLapatinib, kwaye i-ErbB engenakuguquleka ye-receptor tyrosine kinase inhibitor.I-Neratinib inokunqanda ngokukhethekileyo i-HER-1 kunye ne-HER-2 yentsapho ye-EGFR (IC50 yayingu-92 nmol / L kunye ne-59 nmol / L, ngokulandelanayo).Uphando lweklinikhi lubonise ukuba iNeratinib yenza isiphumo esibalulekileyo sonyango kumhlaza wemiphunga weseli ongengomncinci, umhlaza wekoloni, kunye nomhlaza wamabele.Ulingo lwe-phaseⅡclinical lubonise ukuba iNeratinib ibonise ukusebenza kakuhle kunye nokunyamezelana kwi-HER-2 izigulane ezinesifo somhlaza webele ophezulu oye wafunyanwa okanye akafumani unyango lweTrastuzumab.Isigaba Ⅲ solingo lwezonyango lomhlaza wamabele lwagqitywa ngoSeptemba wama-2014.