For research use only. Not for therapeutic Use.
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].
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].
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].
| Catalog Number | I043979 |
| CAS Number | 2756333-39-6 |
| Synonyms | 6-fluoro-5-[4-[(5-fluoro-2-methyl-3-oxo-4H-quinoxalin-6-yl)methyl]piperazin-1-yl]-N-methylpyridine-2-carboxamide |
| Molecular Formula | C21H22F2N6O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C21H22F2N6O2/c1-12-20(30)27-18-14(25-12)4-3-13(17(18)22)11-28-7-9-29(10-8-28)16-6-5-15(21(31)24-2)26-19(16)23/h3-6H,7-11H2,1-2H3,(H,24,31)(H,27,30) |
| InChIKey | WXRCLFFPZXJCLS-UHFFFAOYSA-N |
| SMILES | CC1=NC2=C(C(=C(C=C2)CN3CCN(CC3)C4=C(N=C(C=C4)C(=O)NC)F)F)NC1=O |
| 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. |
