Lapatinib Base CAS 231277-92-2 Purity ≥99.0% (HPLC)
Lebitso la Lik'hemik'hale | Motheo oa Lapatinib |
Litlhaloso tse tšoanang | 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 |
Nomoro ea CAS | 231277-92-2 |
Boemo ba Setoko | E teng thepeng e teng ka lebenkeleng |
Foromo ea limolek'hule | Setšoantšo sa C29H26ClFN4O4S |
Boima ba Molek'hule | 581.06 |
Melting Point | 141.0 ~ 149.0 ℃ |
Botenya | 1.381±0.06 g/cm3 |
COA & MSDS | E fumaneha |
Brand | Ruifu Chemical |
Ntho | Litlhaloso |
Ponahalo | Phofo e Batlileng e Le Bosoeu kapa Bosehla ba Crystalline |
Boitsebiso | IR;HPLC |
Mokhoa oa Bohloeki / Analysis | ≥99.0% (HPLC) |
Melting Point | 141.0 ~ 149.0 ℃ |
Tahlehelo ka ho Omisa | ≤0.50% |
Masalla a ho Ignition | ≤0.10% |
Heavy Metals (as Pb) | ≤20ppm |
Litšila tsa Organic Volatile | Kopana le Tlhokahalo |
Lintho Tse Amanang | |
Tšilafalo e le Mong | ≤0.30% |
Litšila ka Kakaretso | ≤1.00% |
Tekanyetso ea Teko | Maemo a Khoebo |
Shelf Life | Lilemo tse 2 ha li bolokiloe hantle |
Tšebeliso | API, Kalafo ea Molomo bakeng sa Kankere ea Matsoele |
Sephutheloana: Botlolo, Aluminium foil bag, 25kg/Cardboard Drum, kapa ho ea ka tlhokahalo ea moreki.
Boemo ba polokelo:Boloka ka lijaneng tse koetsoeng sebakeng se phodileng le se omileng;Sireletsa leseli le mongobo
API (CAS: 231277-92-2)ke phekolo e lebisitsoeng ea lithethefatsi tsa kankere ea matsoele, ke tyrosine kinase inhibitor, e ka thibelang ka katleho tšebetso ea epidermal growth factor receptor -1 (ErbB1) le human epidermal growth factor receptor (ErbB2) tyrosine kinase mosebetsi oa -2.E ikhetha ka hore e ka phetha karolo ka litsela tse sa tšoaneng, e le hore lisele tsa kankere ea matsoele li se ke tsa fumana pontšo e hlokahalang bakeng sa khōlo.Mokhoa oa ts'ebetso ke ho thibela libaka tsa ATP tsa intracellular EGFR (ErbB-1) le HER2 (ErbB-2) ho thibela phosphorylation le ts'ebetso ea lisele tsa tumor, le ho thibela ho theoha-taolo ea pontšo ka EGFR (ErbB-1) le HER2 (ErbB-1) likarolo tse peli tse homogeneous le tse fapaneng.Motsoako oa (CAS: 231277-92-2) le Capecitabine e sebelisetsoa ho phekola bakuli ba nang le kankere ea matsoele e tsoetseng pele kapa ea metastatic ka ho feteletsa ha motho epidermal receptor2, e seng e phekoloa ka anthracyclines, paclitaxel, le trastuzumab.Liteko tsa bongaka li bonts'itse hore e boetse e phekola bakuli ba mofets'e oa mofuta oa HER2 ka katleho ba nang le khanyetso ea Herceptin.
Lapatinib hammoho le Capecitabine e loketse bakeng sa phekolo ea bakuli ba kankere ea matsoele e tsoetseng pele kapa ea metastatic ka HER2 (ErbB-2 overexpression) le phekolo ea pele e kenyeletsang anthracyclines, paclitaxel le trastuzumab.
Matlapa a in vitro Lapatinib a ka thibela CYP3A4 le CYP2C8 maemong a kalafo, 'me a sebelisoa haholo ke CYP3A4.Lithethefatsi tse thibelang tšebetso ea enzyme ena li ka eketsa haholo khatello ea mali ea lithethefatsi ea Lapatinib.Ketoconazole, 0.2g nako le nako, makhetlo a 2 / d, e ka eketsa AUC ea Lapatinib ka makhetlo a 3-7 le ho lelefatsa halofo ea bophelo ka makhetlo a 1.7 kamora matsatsi a 7.Baithaopi ba phetseng hantle ba ile ba nka CYP3A4 inducer ka molomo, 100 mg nako le nako, habeli ka letsatsi, 'me ba fetoloa ho 200mg nako le nako ka mor'a matsatsi a 3, ba arolelana matsatsi a 17 habeli ka letsatsi.AUC ea Lapatinib e fokotsehile ka 72%.Lapatinib ke sebaka sa lipalangoang bakeng sa P-glycoprotein, 'me lithethefatsi tse thibelang glycoprotein li ka eketsa khatello ea mali ea moriana.
Lapatinib ke setlhare se secha bakeng sa kalafo e lebisitsoeng ea mofetše oa matsoele o ntlafalitsoeng ke GlaxoSmithKline, UK.Ke tyrosine kinase inhibitor e ka thibelang ka katleho ts'ebetso ea motho ea epidermal growth factor receptor -1 (ErbB1) le ts'ebetso ea epidermal growth factor receptor -2 (ErbB2) tyrosine kinase mosebetsi.E ikhetha ka hore e ka sebetsa ka litsela tse sa tšoaneng e le hore lisele tsa kankere ea matsoele li se ke tsa fumana matšoao a hlokahalang bakeng sa khōlo.Mokhoa oa ts'ebetso ke ho thibela libaka tsa ATP tsa EGFR (ErbB-1) le HER2 (ErbB-2) liseleng ho thibela phosphorylation le ts'ebetso ea lisele tsa tumor, le ho thibela matšoao a ho theola taolo ka li-dimers tse fapaneng le tse fapaneng tsa EGFR (ErbB). -1) le HER2 (ErbB-1).Phekolo e lebisitsoeng ho limolek'hule bakeng sa mofetše oa matsoele e bua ka kalafo ea li-oncogenes le lihlahisoa tse amanang le polelo tse amanang le ho hlaha le nts'etsopele ea mofetše oa matsoele.Lithethefatsi tse etselitsoeng limolek'hule li thibela kapa li bolaea lisele tsa hlahala ka ho thibela phetisetso ea lets'oao ho lisele tsa hlahala kapa lisele tse amanang le tsona ho laola liphetoho tsa polelo ea liphatsa tsa lefutso.ka March 14, 2007, tsamaiso ea lijo le lithethefatsi tsa US e amohetse motsoako oa lapatinib le xeloda (capecitabine) bakeng sa phekolo ea bakuli ba kankere ea matsoele e tsoetseng pele kapa ea metastatic e fetelelitsoeng ke motho epidermal factor receptor 2 (ErbB2) le ho phekoloa ka anthracyclines, paclitaxel le trastuzumab. .Liteko tsa tleliniki li bonts'a hore sehlahisoa sena se boetse se na le litlamorao tse ntle tsa kliniki ho bakuli ba mofetše oa matsoele oa HER2 ba seng ba hlaotse khanyetso ea lithethefatsi ho Roche's Herceptin (Herceptin).lapatinib ke sethethefatsi se secha se reretsoeng ho thibela mofetše.E ka sebetsa holima lipheo tsa Her-1 le Her-2 ka nako e le 'ngoe.Phello ea likokoana-hloko ea mokhoa ona oa ketso ho ata le ho hōla ha lisele tsa hlahala e kholo haholo ho feta ea sepheo se le seng feela.Seo ho thoeng ke litlhare tsa kalafo tse lebisitsoeng holima lithethefatsi tse sebelisang li-receptor tse itseng, liphatsa tsa lefutso kapa liprotheine tsa bohlokoa e le sepheo sa ho bolaea lisele tse amanang le hlahala ka mokhoa o lebisitsoeng.