Lapatinib Base CAS 231277-92-2 Kuchena ≥99.0% (HPLC)
Chemical Name | Lapatinib Base |
Mashoko anoreva zvakafanana | 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 |
Nhamba yeCAS | 231277-92-2 |
Stock Status | Mudura |
Molecular Formula | C29H26ClFN4O4S |
Molecular Weight | 581.06 |
Melting Point | 141.0~149.0℃ |
Density | 1.381±0.06 g/cm3 |
COA & MSDS | Available |
Brand | Ruifu Chemical |
Item | Zvinotsanangurwa |
Chitarisiko | Inenge Ichena kana Yero Yellow Crystalline Powder |
Identification | IR;HPLC |
Kuchena / Analysis Method | ≥99.0% (HPLC) |
Melting Point | 141.0~149.0℃ |
Kurasika paKuomesa | ≤0.50% |
Residue paIgnition | ≤0.10% |
Heavy Metals (as Pb) | ≤20ppm |
Organic Volatile Impurities | Ita Zvinodiwa |
Related Substances | |
Kusachena Kumwechete | ≤0.30% |
Zvose Zvisina Kuchena | ≤1.00% |
Test Standard | Enterprise Standard |
Sherufu Hupenyu | 2 Makore Paakachengetedzwa Zvakanaka |
Usage | API, Kurapwa Kwemuromo kweGomarara reMazamu |
Package: Bhodhoro, Aluminium foil bag, 25kg/Cardboard Drum, kana zvinoenderana nezvinodiwa nemutengi.
Storage Condition:Chengetedza mumidziyo yakavharwa panzvimbo inotonhorera uye yakaoma;Dzivirira kubva kuchiedza uye unyoro
API (CAS: 231277-92-2)inotarirwa kurapwa kwechirwere chegomarara rezamu, inonzi tyrosine kinase inhibitor, inogona kunyatso kuvharidzira munhu epidermal growth factor receptor -1 (ErbB1) uye epidermal kukura factor receptor (ErbB2) tyrosine kinase basa re -2.Iyo yakasiyana-siyana pakuti inogona kuita basa nenzira dzakasiyana-siyana, kuitira kuti masero emukenza wezamu arege kugamuchira chiratidzo chinodiwa pakukura.Iyo nzira yekuita ndeye inhibit iyo intracellular EGFR (ErbB-1) uye HER2 (ErbB-2) ATP nzvimbo kudzivirira phosphorylation uye activation ye tumor cell, uye kuvhara pasi-mutemo wekuisa chiratidzo neEGFR (ErbB-1) uye HER2 (ErbB-1) homogeneous uye heterogeneous maviri aggregates.Iko kusanganiswa kwe (CAS: 231277-92-2) neCapecitabine inoshandiswa kurapa varwere vane kenza yepamusoro kana metastatic yemazamu ine overexpression yemunhu epidermal receptor2, yakatorapwa neanthracyclines, paclitaxel, uye trastuzumab.Miedzo yemakiriniki yakaratidza kuti inobata zvakare HER2-mhando yekenza varwere vane Herceptin kuramba.
Lapatinib yakabatana neCapecitabine inokodzera kurapwa kwevarwere vekenza yemazamu yepamusoro kana metastatic vane HER2 (ErbB-2 overexpression) uye kurapwa kwekare kunosanganisira anthracyclines, paclitaxel uye trastuzumab.
In vitro Lapatinib mapiritsi anogona kudzivisa CYP3A4 uye CYP2C8 pamagariro ekurapa, uye anonyanya kushandiswa neCYP3A4.mishonga inodzivisa iyi enzyme basa inogona kuwedzera zvakanyanya kuwedzerwa kweropa remishonga yeLapatinib.Ketoconazole, 0.2g nguva imwe neimwe, 2 nguva / d, inogona kuwedzera AUC yeLapatinib ne3 ~ 7 nguva uye kuwedzera hafu yehupenyu ne 1.7 nguva mushure memazuva manomwe.Vazvipiri vane hutano vakatora CYP3A4 inducer nemuromo, 100 mg nguva imwe neimwe, kaviri pazuva, uye vakashandura kusvika ku200mg nguva imwe neimwe mushure memazuva matatu, vachigovana mazuva 17 kaviri pazuva.AUC yeLapatinib yakaderera ne72%.Lapatinib inzvimbo yekutakura yeP-glycoprotein, uye zvinodhaka zvinodzivisa glycoprotein zvinogona kuwedzera kuwedzera kweropa remushonga.
Lapatinib mushonga mutsva wekunangwa kurapa cancer yemazamu yakagadziriswa neGlaxoSmithKline, UK.Iyo inonzi tyrosine kinase inhibitor inogona kuvharidzira zvinobudirira epidermal kukura factor receptor -1 (ErbB1) uye epidermal kukura factor receptor -2 (ErbB2) tyrosine kinase basa.Iyo yakasiyana-siyana pakuti inogona kushanda nenzira dzakasiyana-siyana kuitira kuti masero emukenza wezamu asakwanise kugamuchira zviratidzo zvinodiwa pakukura.Iyo nzira yekuita ndeyekuvharira nzvimbo dzeATP dzeEGFR (ErbB-1) uye HER2 (ErbB-2) mumasero kudzivirira phosphorylation uye activation ye tumor cell, uye kuvhara pasi-mutemo masaini kuburikidza nehomogenous uye heterogeneous dimers yeEGFR (ErbB). -1) uye HER2 (ErbB-1).Molecular yakanangwa kurapwa kwegomarara rezamu inoreva kurapwa kweoncogenes uye zvine chekuita nekutaura zvigadzirwa zvine chekuita nekuitika uye kukura kwegomarara rezamu.Molecular yakanangwa zvinodhaka inhibisa kana kuuraya bundu maseru nekuvharira kutapurirana chiratidzo mumamota maseru kana maseru ane hukama kudzora shanduko musero gene kutaura.musi waKurume 14, 2007, chikafu cheUS uye manejimendi manejimendi akabvumidza kusanganiswa kwelapatinib uye xeloda (capecitabine) yekurapa kwepamusoro kana metastatic kenza yemazamu varwere vakawedzeredzwa nemunhu epidermal factor receptor 2 (ErbB2) uye kurapwa neanthracyclines, paclitaxel uye trastuzumab. .Miedzo yemakiriniki inoratidza kuti chigadzirwa ichi chine zvakare yakanaka kiriniki mhedzisiro yeHER2 varwere vegomarara rezamu vakagadzira kuramba kwemishonga kuRoche's Herceptin (Herceptin).lapatinib mushonga mutsva wakanangana necancer.Inogona kuita paHer-1 uye Her-2 zvinangwa panguva imwe chete.The biological effect yeiyi modhi yechiito pakuwanda nekukura kwemabundu masero yakakura kwazvo kupfuura yechinangwa chimwe chete.Iyo inonzi inonangwa yekurapa mishonga inoreva mishonga inoshandisa mamwe ma receptors, majini kana mapuroteni akakosha sezvinangwa zvekuuraya ane hukama nebundu maseru nenzira yakanangwa.