AZD 3759 phofo (1626387-80-1) - Mofani oa Sefektheri sa Moetsi
AASraw e hlahisa phofo ea Cannabidiol (CBD) le oli ea bohlokoa ea Hemp ka bongata!

EA-3759-AZ

Rating: Category:

AZD-3759 phofo ke inhibitor ea molomo ea mofuta o hlaha le o fetohileng oa EGFR o nang le boleng ba IC50 ka bongata ba nanomolar. Lithethefatsi li fumanoe ke AstraZeneca bakeng sa kalafo ea mofets'e o seng o monyane oa lisele tsa matšoafo le metastase ea CNS.

Tlhaloso ea Sehlahisoa

Litšobotsi tsa Motheo

Name Product AZD 3759 phofo
Nomoro ea CAS 1626387-80-1
Molecular Formula EA-KO22-C23
Boima ba 'mele 459.90
Li-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 phofo (Free Acid / Base) Mekhahlelo.

Ponahalo phofo ea kristale
Ho Boloka le ho Sebetsana Boloka tlasa 20 ° C le ho sireletsa moeeng le leseling, years lilemo tse 2

 

Tlhaloso ea phofo ea AZD 3759

Phofo ea AZD 3759 ke boko bo kenellang ka hare ho mofuta oa mofuta o hlaha le li-receptor tsa EGF tse sebetsang ka mafolofolo (EGFRs; IC50s = 0.3, 0.2, le 0.2 nM bakeng sa mofuta o hlaha, L858R-mutant, le exon 19 e nang le li-EGFR, ka ho latellana). E khetha EGFR ho feta li-kinase tse ling tse 115, e bonts'a thibelo ea 50% mokokotlong oa 1 μm. azd 3579 e fokotsa egfr phosphorylation le keketseho ea lisele ho l858r-mutant exon 19 deletion e nang le h3255 pc-9 lisele (gi50s = 7.7 7.0 nm, ka ho latellana) empa ha e na tšusumetso ho h838 e hlalosang mofuta o hlaha (gi50 = 21,556 nm). 3759 phofo e thibela kholo ea hlahala ka 78% e hlohlelletsa litekanyo tsa khatello ea maikutlo 7.5 15 mg / kg, po, ka ho latellana ea mofuta oa toeba e seng e nyane ea mofets'e oa kankere ea matšoafo (nsclc) metastasis ea boko.

 

Mokhoa oa Ts'ebetso oa Powder oa AZD 3759

AZD-3759 phofo ke inhibitor e matla ea kholo ea li-epidermal factor (EGFR) inhibitor, e nang le tšebetso e ka bang teng ho thibela tšoaetso. Phofo ea AZD-3759 e tlama le ho thibela ts'ebetso ea EGFR hammoho le mefuta e meng ea phetoho ea EGFR. Sena se thibela lets'oao le lumellanang la EGFR, mme se ka lebisa ho kenngoe ha lefu la sele le ho thibela kholo ea hlahala liseleng tsa EGFR-overexpressing.

 

Kopo ea AZD 3759 Powder

AZD-3759 phofo ke inhibitor ea molomo ea mofuta o hlaha le o fetohileng oa EGFR o nang le boleng ba IC50 ka bongata ba nanomolar. Lithethefatsi li fumanoe ke AstraZeneca bakeng sa kalafo ea mofets'e o seng o monyane oa lisele tsa matšoafo le metastase ea CNS. Phofo ea AZD-3759 e ka phunyeletsa tšitiso ea mali le boko mme ea netefatsoa hore e sebetsa ka har'a vitro e nang le methapo ea sele ea NSCLC le mohlala oa toeba oa metastases ea boko. AZD-3759 phofo hajoale e le tekong ea bongaka ea Phase 1.

 

♦ In vitro

Liseleng tsa H3255 (L858R), AZD3759 e thibela phosphorylation ea EGFR le IC50 ea 7.2 nM. AZD3759 e bonts'a litlamorao tse thibelang tsela ea pEGFR le ho ata ha sele ea lisele tse tsoang ho EGFR tse tsoang phetohong ea PC-9 le H3255 le IC50 ea 7.7 nM le 7 nM, ka ho latellana, e bonts'a ts'ebetso ea ts'ebeliso ea lisele tsa lisele tsa H838.

 

♦ Ka vivo

AZD3759 e bonts'a ho fumaneha habonolo ha lintja ka molomo, 'me e kenella haholo bokong ba tšoene. Ka har'a metastasis ea PC-9 (Exon19Del) ea methapo ea boko, AZD3759 (15 mg / kg) e baka tšebetso e matla ea ts'oaetso ea antitumor.

 

Litla-morao le litemoso tsa AZD 3759

Phofo ea AZD 3759 ke mofuta oa li-inhibitors tsa EGFR, Chemotherapy e sebelisang EGFR kapa FGFR inhibitors e ka baka liphetoho tsa epithelial ea corneal ka phokotso ea pono e folang kamora ho emisoa ha mahlahana. Ka bomalimabe, lingaka tse ling li lula li sa tsebe litla-morao tse joalo, li siea bakuli ba bangata ba sa laoloe. Ka hona, lingaka tsa mahlo li lokela ho lemosa bakuli ba rerang chemotherapy le baemeli ba joalo ka monyetla oa ho fetoha ha li-corneal tse lebisang lefifing la pono. Lingaka li boetse li lokela ho hlakisa hore liso tsa corneal li kanna tsa raroloha kamora ho fela ha chemotherapy.

 

Reference

[1] Zeng Q, le al. Tlhatlhobo le Tlhatlhobo ea Mokhethoa oa Tleliniking AZD3759, ea Matla, ea Sebetsang ka Molomo, Sistimi e Kholo ea Nervous-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. J Med Chem. 2015 Mphalane 22; 58 (20): 8200-15.

[2] Wang S, Zhou Y, Geng P, Zhang Q, Wen C. Boithuto ba tšebelisano ea Pharmacokinetic lipakeng tsa imatinib le sorafenib ka likhoto. Lat Am J Pharm 2014; 33: 1723-7.

[3] Chen DX, Geng PW, Zhang LJ le al Pharmacokinetic ho ithuta ka duloxetine ka rat ka mokelikeli oa chromatography boima ba spectrometry. Lat Am J Pharm 2015; 34: 2078-83.

[4] Zhou Y, Wang S, Geng P, Zhang Q, Ma J. Pharmacokinetic tšebelisano lipakeng tsa lapatinib le sorafenib ho latela taolo e le 'ngoe le e kopanetsoeng ea molomo ka likhoto. Lat Am J Pharm 2014; 33: 1718–22.

[5] Li X, Wang Y, Wang J et al Ntlafatso ea ts'ebetso ea AZD3759 le radiation maqhubu a bokong a tsoang ho EGFR mutant non-small cancer cancer cancer. Kankere ea Int J 2018; 143: 212–24.

[6] Yang Z, Guo Q, Wang Y et al AZD3759, BBB e kenang ka hare ho EGFR inhibitor bakeng sa kalafo ea EGFR mutant NSCLC ka metastase ea CNS. Sci Transl Med 2016; 8: 368ra172.