AZD 3759 efuefu (1626387-80-1) - Gaosi oloa Tuuina atu
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FA-3759

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AZD-3759 efuefu o se tautala taofia o le vao-ituaiga ma mutant EGFR ma IC50 taua i nanomolar tulaga. O le vailaʻau na mauaina e AstraZeneca mo le togafitia o le kanesa laiti e le o se sela laʻititi ma le CNS metastases.

Faamatalaga oloa

Tulaga Autu

Igoa oloa AZD 3759 pauta
Numera CAS 1626387-80-1
Faiga Faʻavae Molecular C22H23ClFN5O3
Fua Faatatau o le Umi 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 efuefu, Fuafua Acid / Base) Tapulaʻa

Faʻaaliga efuefu tioata
Teuina ma Taulimaina Faleoloa i lalo ole 20 ° C ma puipuia mai le ea ma le malamalama, ≥ 2 tausaga

 

AZD 3759 Faʻamatalaga o le efuefu

AZD 3759 efuefu o le faiʻai penisina taofiofia o le vao-ituaiga ma faʻatinoina gaioiga mutant EGF taliaina (EGFRs; IC50s = 0.3, 0.2, ma le 0.2 nM mo vao-ituaiga, L858R-mutant, ma exon 19 faʻamamaina-aofia ai EGFRs, faasologa). E filifilia mo EGFR sili atu 115 isi kinase, faʻaalia <50% taofi i le faʻatauaina o le 1 μm. azd 3579 faʻaititia egfr phosphorylation ma faʻateleina sela i l858r-mutant exon 19 aveese-aofia h3255 pc-9 sela (gi50s = 7.7 7.0 nm, faʻatulagaina) ae leai se aoga i le h838 e faʻaalia ituaiga vao (gi50 = 21,556 nm). 3759 efuefu taofiofia tuputupu tuputupu ae i le 78% mafua ai regression inumaga 7.5 15 mg / kg, po, faasologa isumu faataitaiga le-laiti sela sela kanesa (nsclc) faiai metastasis.

 

AZD 3759 Powder Faʻavae o Gaioiga

AZD-3759 efuefu o se malosiaga epidermal tuputupu ae vaega receptor (EGFR) taofia, ma ono antineoplastic gaioiga. O le paʻu AZD-3759 e fusifusia ma faʻagata le gaioiga a le EGFR faʻapea foʻi ma nisi ituaiga mutant o le EGFR. Ole mea e taofia ai le faʻatonutonu ole EGFR, ma e ono taitai atu ai i le faʻaulufaleina ole oti ile sela ma le taofiofia ole tuputupu aʻe o le EGFR-overexpressing cells.

 

AZD 3759 Paula Talosaga

AZD-3759 efuefu o se tautala taofia o le vao-ituaiga ma mutant EGFR ma IC50 taua i nanomolar tulaga. O le vailaʻau na mauaina e AstraZeneca mo le togafitia o le kanesa laiti e le o se sela laʻititi ma le CNS metastases. AZD-3759 efuefu mafai ona ofi i le toto-faiai papupuni ma faʻamaoniaina e aoga i vitro ma NSCLC sela laina faʻapea foi ma isumu faʻataʻitaʻi o metastases faiai. AZD-3759 pauta o loʻo i ai nei i le Vaega 1 faʻataʻitaʻi faʻataʻitaʻi.

 

♦ I vitro

I sela HC3255 (L858R), AZD3759 taofia le EGFR phosphorylation ma IC50 o le 7.2 nM. AZD3759 o loʻo faʻaalia ai le faʻatamaia o aʻafiaga i luga ole auala pEGFR ma le faʻateleina o sela ole EGFR suiga o sela PC-9 ma le H3255 ma le IC50 o le 7.7 nM ma le 7 nM, faʻasolosolo ona faʻaalia ai lou gaioiga i sela faʻaolaola o sela H838.

 

♦ I le ola

AZD3759 faʻaalia le lelei tautala bioavailability i maile, ma ati tele i totonu o manuki faiʻai. I le faiai metastasis PC-9 (Exon19Del) faʻataʻitaʻiga, AZD3759 (15 mg / kg) mafua ai taua tele-faʻalagolago antitumor aoga.

 

AZD 3759 Efuefu Itu Aafiaga & Lapataiga

AZD 3759 pauta o se ituaiga o EGFR mea faʻapipiʻi, Chemotherapy faʻaaogaina EGFR poʻo FGFR taofi e mafai ona mafua ai suiga o le epithelial corneal ma le faʻaititia o vaʻaiga vaʻaia e toe maua mai le maeʻaina o sooupu. Ae paga lea, o nisi fomaʻi tumau pea le nofouta i ia itu aʻafiaga, ma tuua ai le tele o tagata gasegase le pulea. O le mea lea, ophthalmologists tatau ona muaʻi lapatai tagata mamaʻi o loʻo fuafuaina chemotherapy ma ia sooupu e uiga i le ono mafai ona suia suiga e mafua ai le puaoa o le vaʻai. Fomaʻi tatau foi ona faʻamalamalamaina o le faʻaputuga o loʻo ono ono fofo pe a maeʻa le chemotherapy.

 

Tusitaiala

[1] Zeng Q, et al. Mauaina ma Suʻesuʻega o le Sui Tauva Aʻoaʻo AZD3759, o se Malosiaga, Tautalaga Gutu, Tutotonu Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. J Med Chem. 2015 Oketopa 22; 58 (20): 8200-15.

[2] Wang S, Zhou Y, Geng P, Zhang Q, Wen C. Pharmacokinetic fesoʻotaʻiga suʻesuʻega i le va imatinib ma sorafenib i isumu. Lat Am J Pharm 2014; 33: 1723–7.

[3] Chen DX, Geng PW, Zhang LJ et al Pharmacokinetic suʻesuʻega o duloxetine i isumu e suavai chromatography tele spectrometry. Lat Am J Pharm 2015; 34: 2078–83.

[4] Zhou Y, Wang S, Geng P, Zhang Q, Ma J. Pharmacokinetic fegalegaleaiga i le va o lapatinib ma sorafenib mulimuli i le nofofua ma tuʻufaʻatasia pulega i isumu. Lat Am J Pharm 2014; 33: 1718–22.

[5] Li X, Wang Y, Wang J et al Faʻamalosia le aoga o le AZD3759 ma le paʻu o le faiʻai metastasis mai le EGFR mutant non ‐ cell cell lung cancer. Int J Kanesa 2018; 143: 212–24.

[6] Yang Z, Guo Q, Wang Y et al AZD3759, o le BBB-ulufale i totonu o le EGFR taofi mo le togafitia o le EGFR mutant NSCLC ma CNS metastases. Sci faaliliu Med 2016; 8: 368ra172.