trans-4-Dimethylaminocrotonic Acid Hydrochloride CAS 848133-35-7 Tsarkake>98.0% (HPLC) Afatinib Dimaleate Intermediate

trans-4-Dimethylaminocrotonic Acid Hydrochloride (CAS: 848133-35-7) wani reagent ne da aka yi amfani dashi a cikin shirye-shiryen tyrosine kinase yana hana jami'an antitumor.trans-4-Dimethylaminocrotonic Acid Hydrochloride za a iya amfani dashi azaman matsakaici na Afatinib (CAS: 439081-18-2), Afatinib Dimaleate (CAS: 850140-73-7), Neratinib (CAS: 698387-09-6).Afatinib magani ne da aka amince da shi don maganin cutar sankarau mara kanana (NSCLC), wanda Boehringer Ingelheim ya haɓaka.Yana aiki azaman mai hana angiokinase.Kamar Lapatinib da Neratinib, Afatinib shine mai hanawa na tyrosine kinase (TKI) wanda kuma ba zai iya jurewa ba yana hana mai karɓar haɓakar haɓakar haɓakar ɗan adam 2 (Her2) da kuma mai karɓar haɓakar haɓakar haɓakar epidermal (EGFR) kinases.Afatinib ba kawai yana aiki akan EGFR bamaye gurbi da aka yi niyya ta ƙarni na farko TKIs likeerlotinib ko gefitinib, amma kuma a kan waɗanda ba su kula da waɗannan daidaitattun hanyoyin kwantar da hankali ba.Saboda ƙarin ayyukansa akan Her2, ana bincikar cutar kansar nono da sauran cututtukan daji na EGFR da Her2.Neratinib wanda kamfanin US Wyeth ya haɓaka shine mai hana haɓakar haɓakar haɓakar epidermal (EGFR) wanda ba zai iya jurewa ba.Yana da maƙasudin manufa da yawa na ƙananan ƙwayoyin tyrosine kinase inhibitors zuwa HER 2 da HER1 bayan Lapatinib, kuma mai hanawa na ErbB tyrosine kinase mai hanawa.Neratinib na iya zaɓin hana HER-1 da HER-2 na dangin EGFR (IC50 shine 92 nmol/L da 59 nmol/L, bi da bi).Bincike na asibiti ya nuna cewa Neratinib yana yin tasiri mai mahimmanci akan ciwon daji na huhu, ciwon daji na hanji, da ciwon nono.Gwajin gwaji na lokaciⅡ na asibiti ya nuna cewa Neratinib ya nuna inganci mai kyau da haƙuri ga HER-2 marasa lafiya masu inganci tare da ci gaba da ciwon nono waɗanda aka karɓi ko a'a maganin Trastuzumab.An kammala gwajin asibiti na kashi Ⅲ ciwon nono a cikin Satumba 2014.