AZD-9574(CAS No.:2756333-39-6) yog ib tug muaj zog thiab lub hlwb penetrant PARP1 inhibitor

AZD-9574 yog lub zog, ntshav-hlwb barrier (BBB) ​​penetrant thiab PARP1 selective inhibitor. AZD9574 tuaj yeem siv rau kev tshawb fawb thawj zaug thiab theem nrab ntawm lub hlwb malignancies. AstraZeneca tau soj ntsuam qhov ua tau zoo ntawm AZD9574 nrog rau tus qauv intracranial xenotransplantation ntawm mob qog noj ntshav lub hlwb metastasis. Cov txiaj ntsig ua ntej tau pom tias 3 mg / kg AZ9574 tau pom cov qog loj hlob tseem ceeb ntawm tus tsiaj qauv ntawm cov kab mob intracranial, ua rau lub sijhawm muaj sia nyob ntawm cov qog nqaij nas, thiab xav tias yuav muab cov txheej txheem kho tshiab rau cov neeg mob HRD + mob qog noj ntshav hauv lub hlwb. metastasis.Thawj tiam PARP inhibitor tsis tuaj yeem nkag mus rau hauv lub hlwb, yog li nws tsis tuaj yeem kho cov neeg mob hlwb metastases. Tus tsim AZD9574 muaj ntau dua 8000 npaug ntawm kev xaiv rau PARP1 dua li lwm yam subtypes, thiab muaj txiaj ntsig zoo hauv kev nkag mus rau hauv lub hlwb, muab kev ua si rau kev ua tau zoo, ntxiv txo cov koob tshuaj kho mob, thiab txhim kho kev kho mob index.

AZD-9574 is a potent and brain penetrant PARP1 inhibitor and shows >8000-fold selectivity rau PARP1 piv rau PARP2/3/5a/6. AZD-9574 ua los ntawm kev xaiv inhibiting thiab ntxiab PARP1 ntawm qhov chaw ntawm SSBs. AZD-9574 yog ib qho tshuaj tiv thaiv kab mob qog noj ntshav thiab tuaj yeem siv rau HRD + mob qog noj ntshav mis thiab kev tshawb fawb txog kev mob qog noj ntshav.