Lapatinib Base CAS 231277-92-2 Purity ≥99.0% (HPLC)
Dzina la Chemical | Lapatinib Base |
Mawu ofanana ndi mawu | 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 |
Nambala ya CAS | 231277-92-2 |
Stock Status | Zilipo |
Molecular Formula | Chithunzi cha C29H26ClFN4O4S |
Kulemera kwa Maselo | 581.06 |
Melting Point | 141.0 ~ 149.0 ℃ |
Kuchulukana | 1.381±0.06 g/cm3 |
COA & MSDS | Likupezeka |
Mtundu | Ruifu Chemical |
Kanthu | Zofotokozera |
Maonekedwe | Pafupifupi Ufa Woyera Kapena Wachikasu Wamakristalo |
Chizindikiritso | IR;Mtengo wa HPLC |
Kuyera / Kusanthula Njira | ≥99.0% (HPLC) |
Melting Point | 141.0 ~ 149.0 ℃ |
Kutaya pa Kuyanika | ≤0.50% |
Zotsalira pa Ignition | ≤0.10% |
Zitsulo Zolemera (monga Pb) | ≤20ppm |
Organic Volatile Zonyansa | Gwirani Chofunikira |
Zogwirizana nazo | |
Chidetso Chimodzi | ≤0.30% |
Zonse Zonyansa | ≤1.00% |
Test Standard | Enterprise Standard |
Shelf Life | Zaka 2 Zosungidwa Moyenera |
Kugwiritsa ntchito | API, Chithandizo cha Mkamwa cha Khansa ya M'mawere |
Phukusi: Botolo, Aluminiyamu zojambulazo thumba, 25kg/Cardboard Drum, kapena malinga ndi lamulo la kasitomala
Mkhalidwe Wosungira:Sungani muzitsulo zosindikizidwa pamalo ozizira ndi owuma;Tetezani ku kuwala ndi chinyezi
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API (CAS: 231277-92-2)ndi mankhwala ochizira khansa ya m'mawere, ndi tyrosine kinase inhibitor, amatha kulepheretsa munthu epidermal growth factor receptor -1 (ErbB1) ndi human epidermal growth factor receptor (ErbB2) tyrosine kinase ntchito ya -2.Ndi yapadera chifukwa imatha kugwira ntchito m'njira zosiyanasiyana, kotero kuti maselo a khansa ya m'mawere sangalandire chizindikiro chofunikira kuti chikule.Limagwirira ntchito ndi ziletsa intracellular EGFR (ErbB-1) ndi HER2 (ErbB-2) ATP malo kupewa phosphorylation ndi kutsegula kwa chotupa maselo, ndi kuletsa pansi-malamulo a siginecha ndi EGFR (ErbB-1) ndi HER2 (ErbB-1) yofanana komanso yosakanikirana ndi magulu awiri.Kuphatikizika kwa (CAS: 231277-92-2) ndi Capecitabine kumagwiritsidwa ntchito pochiza odwala omwe ali ndi khansa ya m'mawere yapamwamba kapena ya metastatic ndi overexpression ya human epidermal receptor2, yothandizidwa kale ndi anthracyclines, paclitaxel, ndi trastuzumab.Mayesero azachipatala awonetsa kuti imathandiziranso bwino odwala khansa yamtundu wa HER2 omwe ali ndi vuto la Herceptin.
Lapatinib pamodzi ndi Capecitabine ndi yoyenera kuchiza odwala khansa ya m'mawere yapamwamba kapena ya metastatic ndi HER2 (ErbB-2 overexpression) ndi chithandizo cham'mbuyo kuphatikizapo anthracyclines, paclitaxel ndi trastuzumab.
In vitro Lapatinib mapiritsi akhoza ziletsa CYP3A4 ndi CYP2C8 pa achire ndende, ndipo makamaka zimapukusidwa ndi CYP3A4.mankhwala ziletsa izi puloteni ntchito akhoza kwambiri kuonjezera magazi mankhwala ndende ya Lapatinib.Ketoconazole, 0.2g nthawi iliyonse, 2 nthawi/d, imatha kukulitsa AUC ya Lapatinib ndi nthawi 3-7 ndikutalikitsa theka la moyo ndi nthawi 1.7 patatha masiku 7.Odzipereka athanzi adatenga CYP3A4 inducer pamlomo, 100 mg nthawi iliyonse, kawiri pa tsiku, ndikusintha kukhala 200mg nthawi iliyonse patatha masiku atatu, akugawana masiku 17 kawiri pa tsiku.AUC ya Lapatinib idatsika ndi 72%.Lapatinib ndi malo oyendetsera P-glycoprotein, ndipo mankhwala omwe amaletsa glycoprotein amatha kuwonjezera kuchuluka kwa mankhwalawa.
Lapatinib ndi mankhwala atsopano ochizira khansa ya m'mawere opangidwa ndi GlaxoSmithKline, UK.Ndi tyrosine kinase inhibitor yomwe imatha kuletsa bwino epidermal growth factor receptor -1 (ErbB1) ndi epidermal growth factor receptor -2 (ErbB2) tyrosine kinase ntchito.Ndi yapadera chifukwa imatha kugwira ntchito m'njira zosiyanasiyana kuti maselo a khansa ya m'mawere asalandire zizindikiro zofunika kuti akule.Njira yochitirapo kanthu ndikulepheretsa malo a ATP a EGFR (ErbB-1) ndi HER2 (ErbB-2) m'maselo kuti ateteze phosphorylation ndi kutsegula kwa maselo a chotupa, ndikuletsa ma sign apansi-regulation kudzera ma homogenous and heterogeneous dimers a EGFR (ErbB). -1) ndi HER2 (ErbB-1).Thandizo la mamolekyulu la khansa ya m'mawere limatanthawuza kuchiza ma oncogene ndi zinthu zina zokhudzana ndi zomwe zimachitika komanso kukula kwa khansa ya m'mawere.Mankhwala omwe amapangidwa ndi mamolekyulu amaletsa kapena kupha ma cell chotupa poletsa kutulutsa kwa ma cell m'ma cell chotupa kapena ma cell ofananira nawo kuti athe kuwongolera kusintha kwa jini.pa March 14, 2007, bungwe la US Food and Drug Administration linavomereza kuphatikizika kwa lapatinib ndi xeloda (capecitabine) pofuna kuchiza odwala khansa ya m'mawere yapamwamba kapena ya metastatic yomwe imakhudzidwa kwambiri ndi epidermal factor receptor 2 (ErbB2) ndikuchiritsidwa ndi anthracyclines, paclitaxel ndi trastuzumab. .Mayesero azachipatala akuwonetsa kuti mankhwalawa alinso ndi zotsatira zabwino zachipatala kwa odwala khansa ya m'mawere a HER2 omwe ayamba kukana mankhwala ku Roche's Herceptin (Herceptin).lapatinib ndi mankhwala atsopano oletsa khansa.Ikhoza kuchitapo kanthu pa zolinga za Her-1 ndi Her-2 nthawi imodzi.Mphamvu yachilengedwe yamachitidwe awa pakukula ndi kukula kwa maselo otupa ndi akulu kuposa chandamale imodzi yokha.Mankhwala ochizira omwe amatchedwa kuti achire amatanthawuza mankhwala omwe amagwiritsa ntchito zolandilira, majini kapena mapuloteni ofunikira ngati chandamale chopha maselo okhudzana ndi chotupa m'njira yolunjika.
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