Lapatinib Base CAS 231277-92-2 Tsaftace ≥99.0% (HPLC)
Sunan Sinadari | Lapatinib Base |
Makamantu | Lapatinib;N-[3-Chloro-4-[(3-fluorobenzyl) oxy] phenyl]-6-[5-[(2- (methylsulfonyl) ethyl]amino] methyl]furan-2-yl] quinazolin-4-amine ; N-[3-Chloro-4-[(3-fluorobenzyl) oxy] phenyl] -6-[5-[[2- (methylsulfonyl) ethyl] amino] methyl] -2-furyl] -4-quinazolinamine |
Lambar CAS | 231277-92-2 |
Matsayin Hannun jari | A Stock |
Tsarin kwayoyin halitta | Saukewa: C29H26ClFN4O4S |
Nauyin Kwayoyin Halitta | 581.06 |
Matsayin narkewa | 141.0 ~ 149.0 ℃ |
Yawan yawa | 1.381± 0.06 g/cm3 |
COA & MSDS | Akwai |
Alamar | Ruifu Chemical |
Abu | Ƙayyadaddun bayanai |
Bayyanar | Kusan Fari ko Haske Rawaya Crystalline Foda |
Ganewa | IR;HPLC |
Tsarkake / Hanyar Bincike | ≥99.0% (HPLC) |
Matsayin narkewa | 141.0 ~ 149.0 ℃ |
Asara akan bushewa | ≤0.50% |
Ragowa akan Ignition | ≤0.10% |
Karfe masu nauyi (kamar Pb) | ≤20ppm |
Najasa maras tabbas | Cika Bukatun |
Abubuwa masu alaƙa | |
Tsaftace Guda Daya | ≤0.30% |
Jimlar ƙazanta | ≤1.00% |
Matsayin Gwaji | Matsayin Kasuwanci |
Rayuwar Rayuwa | Shekaru 2 Lokacin Ajiye Daidai |
Amfani | API, Maganin Baki don Ciwon Kan Nono |
Kunshin: Bottle, Aluminum tsare jakar, 25kg / kwali Drum, ko bisa ga abokin ciniki ta bukata
Yanayin Ajiya:Ajiye a cikin kwantena da aka rufe a wuri mai sanyi da bushe;Kare daga haske da danshi
API (CAS: 231277-92-2)shine maganin da aka yi niyya na maganin ciwon daji na nono, shine mai hana tyrosine kinase, zai iya hana mai karɓar haɓakar haɓakar haɓakar ɗan adam -1 (ErbB1) da kuma mai karɓar haɓakar haɓakar haɓakar ɗan adam (ErbB2) aikin tyrosine kinase na -2.Yana da mahimmanci ta yadda zai iya taka rawa ta hanyoyi daban-daban, ta yadda kwayoyin cutar kansar nono ba za su iya samun siginar da ake bukata don girma ba.Hanyar aikin shine don hana EGFR intracellular (ErbB-1) da HER2 (ErbB-2) rukunin ATP don hana phosphorylation da kunna ƙwayoyin tumo, da kuma toshe ƙa'idodin sigina ta EGFR (ErbB-1) da kuma HER2 (ErbB-1) mai kama da nau'in tari biyu.Haɗuwa da (CAS: 231277-92-2) tare da Capecitabine ana amfani dashi don magance marasa lafiya da ciwon nono mai ci gaba ko metastatic tare da wuce gona da iri na mai karɓa na mutum na epidermal2, wanda aka riga aka bi da shi tare da anthracyclines, paclitaxel, da trastuzumab.Gwaje-gwaje na asibiti sun nuna cewa yana kuma magance masu cutar kansa irin na HER2 da kyau tare da juriya na Herceptin.
Lapatinib a hade tare da Capecitabine ya dace da maganin ciwon nono na ci gaba ko masu ciwon nono tare da HER2 (ErbB-2 overexpression) da magani na baya ciki har da anthracyclines, paclitaxel da trastuzumab.
In vitro Lapatinib Allunan na iya hana CYP3A4 da CYP2C8 a adadin warkewa, kuma galibi ana daidaita su ta hanyar CYP3A4.magungunan da ke hana wannan aikin enzyme na iya ƙara haɓaka ƙwayar ƙwayar ƙwayar cuta ta Lapatinib.Ketoconazole, 0.2g kowane lokaci, 2 sau / d, na iya ƙara AUC na Lapatinib sau 3 ~ 7 kuma ya tsawaita rabin rayuwar ta sau 1.7 bayan kwanaki 7.Masu sa kai masu lafiya sun ɗauki CYP3A4 inducer da baki, 100 MG kowane lokaci, sau biyu a rana, kuma sun canza zuwa 200mg kowane lokaci bayan kwanaki 3, raba kwanaki 17 sau biyu a rana.AUC na Lapatinib ya ragu da 72%.Lapatinib wuri ne na sufuri na P-glycoprotein, kuma magungunan da ke hana glycoprotein na iya ƙara yawan ƙwayar jini na miyagun ƙwayoyi.
Lapatinib sabon magani ne don maganin cutar kansar nono wanda GlaxoSmithKline, UK ya kirkira.Yana da mai hanawa na tyrosine kinase wanda zai iya hana haɓakar haɓakar haɓakar haɓakar ɗan adam -1 (ErbB1) da haɓakar haɓakar haɓakar ɗan adam -2 (ErbB2) ayyukan tyrosine kinase.Yana da mahimmanci a cikin cewa yana iya aiki ta hanyoyi daban-daban ta yadda kwayoyin cutar kansar nono ba za su iya karɓar siginar da ake bukata don girma ba.Tsarin aikin shine don hana wuraren ATP na EGFR (ErbB-1) da HER2 (ErbB-2) a cikin sel don hana phosphorylation da kunna ƙwayoyin ƙari, da toshe siginar ƙa'ida ta hanyar kamanni da dimers iri-iri na EGFR (ErbB) -1) da HER2 (ErbB-1).Magungunan da aka yi niyya na kwayoyin halitta don ciwon nono yana nufin maganin oncogenes da samfuran maganganun da ke da alaƙa da abin da ya faru da haɓakar ciwon nono.Kwayoyin da aka yi niyya na ƙwayoyin cuta suna hana ko kashe ƙwayoyin ƙari ta hanyar toshe siginar sigina a cikin ƙwayoyin ƙari ko ƙwayoyin da ke da alaƙa don sarrafa canje-canje a cikin maganganun kwayoyin halitta.A ranar 14 ga Maris, 2007, Hukumar Abinci da Magunguna ta Amurka ta amince da haɗakar lapatinib da xeloda (capecitabine) don kula da ci gaba ko masu cutar kansar nono da aka yi amfani da su ta hanyar mai karɓar ƙwayar cuta ta ɗan adam 2 (ErbB2) kuma ana bi da su tare da anthracyclines, paclitaxel da trastuzumab. .Gwaje-gwaje na asibiti sun nuna cewa wannan samfurin kuma yana da kyakkyawan sakamako na asibiti ga masu cutar kansar nono na HER2 waɗanda suka haɓaka jurewar magani ga Roche's Herceptin (Herceptin).Lapatinib sabon maganin ciwon daji ne da aka yi niyya.Yana iya yin aiki a kan Her-1 da Her-2 hari a lokaci guda.Tasirin ilimin halitta na wannan yanayin aiki akan haɓakawa da haɓakar ƙwayoyin ƙari ya fi na manufa ɗaya kawai.Abin da ake kira magungunan warkewa da aka yi niyya suna nufin magungunan da ke amfani da wasu masu karɓa, kwayoyin halitta ko sunadarai masu mahimmanci a matsayin maƙasudi don kashe ƙwayoyin tumo masu alaƙa ta hanyar da aka yi niyya.