AZD 3759 powder (1626387-80-1) - Mugadziri Wemuchina Wekutengesa
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AZD 3759

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AZD-3759 powder ndeyemuromo inhibitor yeese emusango-mhando uye mutant EGFR ine IC50 kukosha mune nanomolar renji. Mushonga uyu wakawanikwa neAstraZeneca yekurapa isiri-diki-sero kenza yemapapu neCNS metastases.

Product Description

Basic Hunhu

Product Name AZD 3759 upfu
CAS Number 1626387-80-1
Molecular Formula C22H23ClFN5O3
Formula Weight 459.90
Synonyms (2R)-2,4-dimethyl-1-piperazinecarboxylic acid, 4-[(3-chloro-2-fluorophenyl)amino]-7-methoxy-6-quinazolinyl ester;

1-Piperazinecarboxylic acid, 2,4-dimethyl-, 4 - [(3-chloro-2-fluorophenyl) amino] -7-methoxy-6-quinazolinyl ester, (2R) -AZD-3759 powder (Mahara Acid / Base) Parameter.

Kuonekwa crystalline upfu
Kuchengeta uye Kubata Chengetedza pasi pe20 ° C uye chengetedza kubva kumhepo uye mwenje, ≥ makore maviri

 

AZD 3759 Powder Tsananguro

AZD 3759 powder uropi hunopinda inhibitor yemusango-mhando uye inoshanda inoshanda mutant EGF receptors (EGFRs; IC50s = 0.3, 0.2, uye 0.2 nM yemusango-mhando, L858R-mutant, uye exon 19 kubviswa-iine EGFRs, zvichiteerana). Iyo inosarudzira EGFR pamusoro pe115 dzimwe kinases, ichiratidza <50% inhibition pakumisikidzwa kwe1 μm. azd 3579 inoderedza egfr phosphorylation uye kuwanda kwemaseru mu l858r-mutant exon 19 kubviswa-iine h3255 pc-9 masero (gi50s = 7.7 7.0 nm, zvichiteerana) asi haina mhedzisiro pa h838 inoratidza rudzi rwemusango (gi50 = 21,556 nm). 3759 powder inhibits bundu kukura ne 78% inokonzeresa kudzokorodza doses 7.5 15 mg / kg, po, zvichiteerana mbeva modhi isiri-diki sero kenza yemapapu kenza (nsclc) brain metastasis.

 

AZD 3759 Powder Mashandiro Ekuita

AZD-3759 poda inesimba epidermal yekukura factor receptor (EGFR) inhibitor, iine antineoplastic chiitiko. AZD-3759 powder inosunga uye inodzivirira zviitiko zveEGFR pamwe nemamwe mafomu ekuchinja eEGFR. Izvi zvinodzivirira EGFR-inoratidzirwa kusainira, uye zvinogona kutungamira kune ese ari maviri induction yesero kufa uye kudzivirirwa kwechunhu kukura muESG-overexpressing maseru.

 

AZD 3759 Powder Kunyorera

AZD-3759 powder ndeyemuromo inhibitor yeese emusango-mhando uye mutant EGFR ine IC50 kukosha mune nanomolar renji. Mushonga uyu wakawanikwa neAstraZeneca yekurapa isiri-diki-sero kenza yemapapu neCS metastases AZD-3759 poda inogona kupinda muropa-huropi chipingamupinyi uye yakasimbiswa kuve inoshanda mu vitro neNSCLC maseru maseru pamwe neiyo mbeva modhi yehuropi metastases. AZD-3759 powder pari zvino iri muChikamu 1 kliniki kuyedzwa.

 

Vit In vitro

MuH3255 (L858R) masero, AZD3759 inhibits EGFR phosphorylation neIC50 ye7.2 nM. AZD3759 inoratidza inhibitory mhedzisiro pane ese pEGFR nzira uye sero kuwanda kwema EGFR mutation-yakatorwa maseru PC-9 uye H3255 ine IC50 ye7.7 nM uye 7 nM, zvichiteerana, ichiratidza mo chiitiko pane sero kuwanda kwemaH838 masero.

 

♦ Mune vivo

AZD3759 inoratidza yakanaka yekuwanikwa bioavailability muimbwa, uye inopinda zvakanyanya muhuropi hwemonkey. Mune uropi metastasis PC-9 (Exon19Del) modhi, AZD3759 (15 mg / kg) inokonzeresa yakakosha yedhi-inomira antitumor kushanda.

 

AZD 3759 Powder Side Mhedzisiro & Yambiro

AZD 3759 poda rudzi rweEGFR inhibitors, Chemotherapy inoshandisa EGFR kana FGFR inhibitors inogona kukonzera corneal epithelial shanduko nekudzikira kwekuona acuity iyo inopora zvichitevera kumiswa kweavo vamiririri. Zvinosuruvarisa, vamwe vanachiremba vanoramba vasingazivi nezvemhedzisiro yakadaro, zvichisiya varwere vazhinji vasingatariswe. Naizvozvo, ophthalmologists anofanirwa kufanonyevera varwere vari kuronga chemotherapy nevamiriri vakadaro nezve mukana wekuchinja kwemakona kunotungamira mukuvhenekera kwechiono. Vanachiremba vanofanirwa zvakare kujekesa kuti maronda emakona anogona kugadzirisa mushure mekuguma kwekemotherapy.

 

Reference

[1] Zeng Q, et al. Kuwana uye Kuongorora kweKiriniki Yemubati AZD3759, ane Simba, Oral Inoshanda, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. J Med Chem. 2015 Gumiguru 22; 58 (20): 8200-15.

[2] Wang S, Zhou Y, Geng P, Zhang Q, Wen C. Pharmacokinetic yekudyidzana kudzidza pakati pe imatinib ne sorafenib mumakonzo. Lat Am J Pharm 2014; 33: 1723-7.

[3] Chen DX, Geng PW, Zhang LJ et al Pharmacokinetic kudzidza kweduloxetine mumakonzo nemvura chromatography yakawanda spectrometry. Lat Am J Pharm 2015; 34: 2078-83.

[4] Zhou Y, Wang S, Geng P, Zhang Q, Ma J. Pharmacokinetic kudyidzana pakati pe lapatinib uye sorafenib inotevera imwechete uye co- yemumuromo manejimendi mumakonzo. Lat Am J Pharm 2014; 33: 1718–22.

[5] Li X, Wang Y, Wang J et al Enhanced efficacy yeAZD3759 uye radiation pahuropi metastasis kubva kuEGFR mutant isiri-diki kenza yemapapu kenza. Int J Kenza 2018; 143: 212-24.

[6] Yang Z, Guo Q, Wang Y et al AZD3759, BBB-inopinza EGFR inhibitor yekurapa EGFR mutant NSCLC ine CNS metastases. Sci Dudzira Med 2016; 8: 368ra172.