| Bioactivity | 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[1]. | ||||||||||||
| Invitro | AZD-9574 inhibits PARP1 enzymatic activity with IC50s range between 0.3-2 nM in all tested cell lines irrespective of the homologous recombination repair (HRR) status[1].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 IC50 in BRCA2-/- DLD1 cells is 1.38 nM compared to IC50 >40 µM BRCA2wt cells[1]. | ||||||||||||
| 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[1]. | ||||||||||||
| Name | AZD-9574 | ||||||||||||
| CAS | 2756333-39-6 | ||||||||||||
| Formula | C21H22F2N6O2 | ||||||||||||
| Molar Mass | 428.44 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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| Reference | [1]. Hybrid meeting divulges structures of drug candidates [2]. 1.Kunzah Jamal, et al. Abstract 2609: AZD9574 is a novel, brain penetrant PARP-1 selective inhibitor with activity in an orthotopic, intracranial xenograft model with aberrant DNA repair. Cancer Res (2022) 82 (12_Supplement): 2609. |
AZD-9574
CAS: 2756333-39-6 F: C21H22F2N6O2 W: 428.44
AZD-9574 is a potent and brain penetrant PARP1 inhibitor and shows >8000-fold selectivity for PARP1 compared to PARP2/3/
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