AZD-9574

AZD-9574 is a potent and brain penetrant PARP1 inhibitor and shows >8000-fold selectivity for PARP1 compared to PARP2/3/5a/6. AZD-9574 acts by selectively inhibiting and trapping PARP1 at the sites of SSBs. AZD-9574 is an anti-cancer agent and can be used for HRD + breast cancer and advanced solid malignancies research In Vitro AZD-9574 inhibits PARP1 enzymatic activity with IC 50 s range between 0.3-2 nM in all tested cell lines irrespective of the homologous recombination repair (HRR) status. In isogenic cell lines pairs confirms higher potency and selectivity towards HRR-deficient (HRD + ) models (DLD1 BRCA2 -/- ; SKOV-3 BRCA2 -/- and SKOV-3 PALB2 -/- ). The IC 50 in BRCA2 -/- DLD1 cells is 1.38 nM compared to IC 50 >40 µM BRCA2 wt cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo AZD-9574 (3 mg/kg) shows sustained tumour growth suppression resulting in a significantly extended survival of tumour-bearing mice, in intracranial xenograft model of breast cancer brain metastases . MCE has not independently confirmed the accuracy of these methods. They are for reference only. IC50& Target:PPAR

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