| Identification | Back Directory | [Name]
AZD-5305 | [CAS]
2589531-76-8 | [Synonyms]
AZD-5305
5-[4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]-1-piperazinyl]-N-methylpicolinamide
2-Pyridinecarboxamide, 5-[4-[(7-ethyl-5,6-dihydro-6-oxo-1,5-naphthyridin-3-yl)methyl]-1-piperazinyl]-N-methyl- | [Molecular Formula]
C22H26N6O2 | [MDL Number]
MFCD34471686 | [MOL File]
2589531-76-8.mol | [Molecular Weight]
406.48 |
| Chemical Properties | Back Directory | [Boiling point ]
702.6±60.0 °C(Predicted) | [density ]
1.246±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 41.67 mg/mL (102.51 mM; Need ultrasonic) | [form ]
Solid | [pka]
11.26±0.40(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
Saruparib (AZD5305) is a potent, orally active and selective PARP inhibitor and trapper with IC50 values of 3 nM and 1400 nM for PARP1 and PARP2, respectively. Saruparib has anti-proliferative activity and inhibits growth in cells with deficiencies in DNA repair[1][2]. | [in vivo]
Saruparib (AZD5305) (0.01-0.3 mg/kg; p.o.; daily, for 35 d; female Han Wistar rats) demonstrates sustained antitumor activity in BRCAm xenograft and PDX models in vivo[1].
| Animal Model: | Female Han Wistar rats with BRCAm xenograft and PDX models (12-13 weeks of age)[1] | | Dosage: | 0.01, 0.03, 0.1, and 0.3 mg/kg | | Administration: | Oral administration; daily, for 35 days | | Result: | Had antitumor efficacy in a dose-dependent manner. |
| [IC 50]
PARP1: 3 nM (IC50); PARP2: 1400 nM (IC50) | [References]
[1] Illuzzi G, et, al. Preclinical Characterization of AZD5305, A Next-Generation, Highly Selective PARP1 Inhibitor and Trapper. Clin Cancer Res. 2022 Nov 1;28(21):4724-4736. DOI:10.1158/1078-0432.CCR-22-0301
[2] Johannes JW, et, al. Discovery of 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}-N-methylpyridine-2-carboxamide (AZD5305): A PARP1-DNA Trapper with High Selectivity for PARP1 over PARP2 and Other PARPs. J Med Chem. 2021 Oct 14;64(19):14498-14512. DOI:10.1021/acs.jmedchem.1c01012 |
|
|