Lapatinib Base CAS 231277-92-2 Mama ≥99.0% (HPLC)
Igoa Vailaau | Lapatinib Base |
Synonyms | 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 |
Numera CAS | 231277-92-2 |
Tulaga Fa'asoa | E tele |
Fuafua mole | C29H26ClFN4O4S |
Molecular Weight | 581.06 |
Lisi Lisi | 141.0~149.0 ℃ |
Malosi | 1.381±0.06 g/cm3 |
COA & MSDS | Avanoa |
Fa'ailoga | Ruifu Chemical |
Aitema | Fa'amatalaga |
Fa'aaliga | Toeitiiti Pa'epa'e po'o Malamalama Samasama Crystalline Pa'u |
Fa'ailoaga | IR;HPLC |
Mama / Suʻesuʻega Metotia | ≥99.0% (HPLC) |
Lisi Lisi | 141.0~149.0 ℃ |
Ma'imau ile Fa'amago | ≤0.50% |
Toega i luga o le mumu | ≤0.10% |
Metala mamafa (pei o le Pb) | ≤20ppm |
Organic Volatile Oma | Faʻafeiloaʻi le Manaoga |
Mea Fa'atatau | |
Le mama nofofua | ≤0.30% |
Aofa'i Fa'aleaga | ≤1.00% |
Tulaga Su'ega | Pisinisi Tulaga |
Ola Fa'asa | 2 Tausaga Pe a Teu Lelei |
Fa'aoga | API, Ose Togafitiga Tauga mo le Kanesa o le Susu |
afifi: Fagu, ato pepa alumini, 25kg/Kati Pusa, pe tusa ai ma manaoga o tagata faatau
Tulaga teuina:Teu i totonu o pusa faʻamaufaʻailoga i se nofoaga malulu ma mago;Puipui mai le malamalama ma le susu
API (CAS: 231277-92-2)o se togafitiga faʻatatau o le kanesa o le susu, o se inhibitor tyrosine kinase, e mafai ona taofia lelei le tagata epidermal growth factor receptor -1 (ErbB1) ma le tagata epidermal growth factor receptor (ErbB2) tyrosine kinase activity of -2.E tulaga ese ona e mafai ona faia se sao i auala eseese, ina ia le mafai e sela o le kanesa o le susu ona maua le faailo e manaʻomia mo le tuputupu aʻe.O le faiga o le gaioiga o le taofia lea o le intracellular EGFR (ErbB-1) ma le HER2 (ErbB-2) ATP nofoaga e puipuia ai le phosphorylation ma le faʻagaoioia o sela tumo, ma poloka le faʻatonutonuina o faʻailoga e le EGFR (ErbB-1) ma HER2 (ErbB-1) fa'atasi ma fa'atasi e lua fa'atasi.O le tuufaatasiga o (CAS: 231277-92-2) faʻatasi ma Capecitabine e faʻaaogaina e togafitia ai tagata mamaʻi e maua i le kanesa o le susu maualuga poʻo metastatic ma le faʻaalia o le epidermal receptor2 tagata, ua uma ona togafitia i anthracyclines, paclitaxel, ma trastuzumab.O su'esu'ega fa'afoma'i ua fa'aalia ai e togafitia lelei fo'i ma'i o le kanesa ituaiga HER2 ma le Herceptin resistance.
Lapatinib faʻatasi ma Capecitabine e talafeagai mo le togafitiga o tagata gasegase o le susu maualuga poʻo metastatic ma le HER2 (ErbB-2 overexpression) ma togafitiga muamua e aofia ai anthracyclines, paclitaxel ma trastuzumab.
In vitro Lapatinib tablets e mafai ona faʻalavelaveina le CYP3A4 ma le CYP2C8 i faʻamaʻi togafitiga, ma e masani lava ona faʻaogaina e CYP3A4.O vailaʻau e faʻalavelaveina ai le gaioiga o le enzyme e mafai ona faʻateleina le faʻaogaina o le toto o le Lapatinib.Ketoconazole, 0.2g taimi taʻitasi, 2 taimi / d, e mafai ona faʻateleina le AUC o Lapatinib i le 3 ~ 7 taimi ma faʻaumi le afa-ola i le 1.7 taimi pe a uma le 7 aso.O tagata volenitia soifua maloloina na ave le CYP3A4 inducer i le tautala, 100 mg i taimi taʻitasi, faalua i le aso, ma suia i le 200mg i taimi taʻitasi pe a uma le 3 aso, faʻasoa 17 aso faalua i le aso.AUC o Lapatinib na faʻaititia i le 72%.Lapatinib ose nofoaga felauaiga mo le P-glycoprotein, ma o vailaʻau e taofia ai le glycoprotein e mafai ona faʻateleina ai le toto o le vailaʻau.
Lapatinib o se vailaʻau fou mo togafitiga faʻapitoa o le kanesa o le susu na atiaʻe e GlaxoSmithKline, UK.O se iniseti tyrosine kinase e mafai ona taofia lelei tagata epidermal growth factor receptor -1(ErbB1) ma tagata epidermal growth factor receptor -2(ErbB2) tyrosine kinase activity.E tulaga ese ona e mafai ona galue i auala eseese ina ia le mafai e sela o le kanesa o le susu ona maua faailo e manaʻomia mo le tuputupu aʻe.O le faiga o le gaioiga o le taofia lea o nofoaga ATP o le EGFR (ErbB-1) ma le HER2 (ErbB-2) i sela e puipuia ai le phosphorylation ma le faʻagaoioia o sela tumo, ma poloka faʻamaufaʻailoga tulafono faatonutonu e ala i dimers homogenous ma heterogeneous o EGFR (ErbB). -1) ma le HER2(ErbB-1).O togafitiga fa'atatau mole mole mo le kanesa o le susu e faasino ile togafitiga ole oncogenes ma fa'amatalaga fa'atusa e feso'ota'i ma le tupu ma le atina'eina ole kanesa o le susu.O vaila'au fa'atatau mole mole e taofia pe tape ai sela tumo e ala i le polokaina o le fa'aliliuina o fa'ailo i sela tumo po'o sela fa'afeso'ota'i e pulea ai suiga i le fa'aaliga o ga'o.i le aso 14 o Mati, 2007, na faʻamaonia ai e le US Food and Drug Administration le tuʻufaʻatasia o le lapatinib ma le xeloda (capecitabine) mo le togafitia o tagata gasegase o le kanesa o le susu maualuga poʻo metastatic o loʻo faʻaalia e le tagata epidermal factor receptor 2 (ErbB2) ma togafitia i anthracyclines, paclitaxel ma trastuzumab .O fa'ata'ita'iga fa'afoma'i ua fa'aalia ai o lenei oloa e iai fo'i a'afiaga lelei mo le kanesa o le susu o le HER2 o lo'o atia'e le tetee atu i vaila'au i le Roche's Herceptin (Herceptin).lapatinib o se vailaʻau faʻamaʻi faʻamaʻi fou.E mafai ona galue i Her-1 ma Her-2 sini i le taimi e tasi.O a'afiaga fa'aola o lenei faiga i le fa'ateleina ma le tuputupu a'e o sela tumo e sili mamao atu nai lo le na'o le tasi le fa'amoemoe.O vailaʻau faʻapitoa e faʻatatau i vailaʻau o loʻo faʻaogaina ai nisi o tali, kene poʻo polotini autu e fai ma sini e faʻaumatia ai sela tumo i se auala faʻatatau.