Isiseko seLapatinib CAS 231277-92-2 Ubunyulu ≥99.0% (HPLC)
Igama leMchiza | Isiseko seLapatinib |
Izithethantonye | iLapatinib;N-[3-Chloro-4-[(3-fluorobenzyl)oxy]phenyl]-6-[5-[[(2-(methylsulfonyl)ethyl]amino]methyl]furan-2-yl]quinazolin-4-amine ; |
Inombolo yeCAS | 231277-92-2 |
Ubume beStokhwe | Ikhona evenkileni |
Ifomula yeemolekyuli | I-C29H26ClFN4O4S |
Ubunzima beMolekyuli | 581.06 |
Indawo yokunyibilika | 141.0 ~ 149.0℃ |
Ukuxinana | 1.381±0.06 g/cm3 |
I-COA kunye ne-MSDS | Iyafumaneka |
Uphawu | Ruifu Chemical |
Into | Iinkcukacha |
Imbonakalo | Phantse uMhlophe oMhlophe okanye oKhaphukhaphu wePowder oyikristale |
Ukuchongwa | I-IR;HPLC |
Ubunyulu / Indlela yokuHlalutya | ≥99.0% (HPLC) |
Indawo yokunyibilika | 141.0 ~ 149.0℃ |
Ilahleko ekomisweni | ≤0.50% |
Intsalela kwi-Ignition | ≤0.10% |
Iintsimbi ezinzima (njenge Pb) | ≤20ppm |
Ukungcola okuguquguqukayo kwe-Organic | Yifezekise iMfuneko |
Izinto ezinxulumeneyo | |
Ukungacoceki Okukodwa | ≤0.30% |
Ukungcola ngokupheleleyo | ≤1.00% |
Umgangatho woVavanyo | Umgangatho woShishino |
Beka ubomi kwishelufa | Iminyaka emi-2 xa igcinwe ngokufanelekileyo |
Ukusetyenziswa | I-API, Unyango lomlomo loMhlaza wamabele |
Iphakheji: Ibhotile, ingxowa yefoyile yeAluminiyam, 25kg/Igubu lekhadibhodi, okanye ngokwemfuno yomthengi
Imeko yoGcino:Gcina kwizikhongozeli ezivaliweyo kwindawo epholileyo neyomileyo;Khusela ukukhanya kunye nokufuma
API (CAS: 231277-92-2)lunyango olujoliswe kuyo lweyeza lomhlaza webele, i-tyrosine kinase inhibitor, inokuthintela ngokufanelekileyo i-epidermal growth factor receptor -1 (ErbB1) kunye ne-epidermal growth factor receptor (ErbB2) i-tyrosine kinase umsebenzi we-2.Iyingqayizivele kuba inokudlala indima ngeendlela ezahlukeneyo, ukwenzela ukuba iiseli zomhlaza webele zingakwazi ukufumana umqondiso ofunekayo ekukhuleni.Indlela yesenzo kukuthintela i-intracellular EGFR (ErbB-1) kunye ne-HER2 (ErbB-2) iisayithi ze-ATP ukukhusela i-phosphorylation kunye nokusebenza kweeseli ze-tumor, kunye nokuthintela ukulawulwa kweempawu ze-EGFR (ErbB-1) kunye I-HER2 (ErbB-1) i-homogeneous kunye ne-heterogeneous aggregates ezimbini.Ukudibanisa (i-CAS: i-231277-92-2) kunye ne-Capecitabine isetyenziselwa ukunyanga izigulane ezinomdlavuza webele ophezulu okanye we-metastatic ngokugqithiswa kwe-receptor2 ye-epidermal yabantu, esele iphathwe nge-anthracyclines, i-paclitaxel, kunye ne-trastuzumab.Ulingo lwezonyango lubonise ukuba ikwanyanga ngokukuko izigulane zomhlaza zohlobo lwe-HER2 ezinokumelana neHerceptin.
I-Lapatinib idibene ne-Capecitabine ifanelekile kunyango lwezigulane zomhlaza zebele eziphambili okanye ze-metastatic nge-HER2 (ErbB-2 overexpression) kunye nonyango lwangaphambili olubandakanya i-anthracyclines, i-paclitaxel kunye ne-trastuzumab.
Iipilisi ze-in vitro Lapatinib zinokunqanda i-CYP3A4 kunye ne-CYP2C8 kwiimpawu zonyango, kwaye i-metabolized ikakhulu yi-CYP3A4.iziyobisi ezithintela lo msebenzi we-enzyme zinokunyusa kakhulu ukuxinwa kweziyobisi zegazi zeLapatinib.I-Ketoconazole, i-0.2g ngexesha ngalinye, amaxesha angama-2 / d, inokunyusa i-AUC yeLapatinib ngamaxesha angama-3 ~ 7 kwaye yandise isiqingatha sobomi ngamaxesha angama-1.7 emva kweentsuku ezi-7.Amavolontiya anempilo athatha i-CYP3A4 inducer ngomlomo, i-100 mg ngexesha ngalinye, kabini ngosuku, kwaye yatshintshela kwi-200mg rhoqo emva kweentsuku ze-3, ukwabelana ngeentsuku ze-17 kabini ngosuku.I-AUC yeLapatinib yehle nge-72%.I-Lapatinib yindawo yokuthutha ye-P-glycoprotein, kwaye iziyobisi ezivimbela i-glycoprotein zinokunyusa ukuxinwa kwegazi kweyeza.
I-Lapatinib lichiza elitsha lonyango ekujoliswe kulo lomhlaza wamabele ophuhliswe yi-GlaxoSmithKline, e-UK.I-tyrosine kinase inhibitor enokuthintela ngokufanelekileyo i-epidermal growth factor receptor -1 (ErbB1) kunye ne-epidermal growth factor receptor -2 (ErbB2) umsebenzi we-tyrosine kinase.Ikhethekile kuba inokusebenza ngeendlela ezahlukeneyo ukuze iiseli zomhlaza wamabele zingakwazi ukufumana imiqondiso efunekayo ekukhuleni.Indlela yesenzo kukuthintela iisayithi ze-ATP ze-EGFR (ErbB-1) kunye ne-HER2 (ErbB-2) kwiiseli ukuthintela i-phosphorylation kunye nokusebenza kweeseli ze-tumor, kunye nokuthintela imiqondiso yokulawula phantsi ngokusebenzisa i-homogenous kunye ne-heterogeneous dimers ye-EGFR (ErbB). -1) kunye ne-HER2 (ErbB-1).Unyango olujoliswe kwimolekyuli yomhlaza wamabele lubhekisa kunyango lwe-oncogenes kunye neemveliso ezihambelanayo zokubonisa ezinxulumene nokwenzeka kunye nophuhliso lomhlaza wamabele.Amachiza ajoliswe kwimolekyuli anqanda okanye abulale iiseli zethumba ngokuthintela ukudluliselwa komqondiso kwiiseli zethumba okanye iiseli ezinxulumene nokulawula utshintsho kwintetho yemfuza yeseli.ngo-Matshi 14, i-2007, ukutya kwe-US kunye nokulawulwa kweziyobisi kuvume ukuhlanganiswa kwe-lapatinib kunye ne-xeloda (capecitabine) kunyango lwezigulane zomhlaza webele ophezulu okanye we-metastatic ogqithiswe ngokugqithiseleyo yi-human epidermal factor receptor 2 (ErbB2) kwaye iphathwe nge-anthracyclines, i-paclitaxel kunye ne-trastuzumab. .Ulingo lwezonyango lubonisa ukuba le mveliso ikwaneziphumo ezilungileyo zonyango kwi-HER2 izigulane ezinomhlaza wamabele eziphuhlise ukuxhathisa kumachiza kwi-Roche's Herceptin (Herceptin).i-lapatinib lichiza elitsha ekujoliswe kulo lokulwa nomhlaza.Inokuthi isebenze kwiithagethi ze-Her-1 kunye ne-Her-2 ngaxeshanye.Isiphumo sebhayoloji yale ndlela yesenzo ekwandeni nasekukhuleni kweeseli zethumba likhulu kakhulu kunolo lwethagethi enye kuphela.Okubizwa ngokuba ngamachiza okujoliswe kuwo abhekisela kumachiza asebenzisa i-receptors ezithile, izakhi zofuzo okanye iiprotheni eziphambili njengeenjongo zokubulala iiseli ze-tumor ezihambelanayo ngendlela ekujoliswe kuyo.