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Saruparib (AZD5305) is a potent and oral active, second-generation PARP (highly selective PARP1) inhibitor with IC50 values of 3 nM and 1400 nM for PARP1 and PARP2, respectively. Saruparib (AZD5305) has anti-proliferative activity and inhibits growth in cells with deficiencies in DNA repair. AZD5305 showed highly effective and sustained anti-tumor activity in selected BRCAm xenograft and PDX in vivo models. At the same time, AZD5305 also showed benefits when used in combination with chemotherapy.
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Source | AZD5305 |
| Method | orally | |
| Cell Lines | BRCAm xenograft and PDX models | |
| Concentrations | 0.01~1mg/kg | |
| Incubation Time | - | |
| Results | AZD5305 shows benefit in combination with chemotherapy. |
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Source | AZD5305 |
| Method | orally (PO) | |
| Cell Lines | BRCAm xenograft and PDX models | |
| Concentrations | 0.01~10mg/kg | |
| Incubation Time | 20, 31, 35 days | |
| Results | AZD5305 demonstrates high and sustained anti-tumour activity in a selection of BRCAm xenograft and PDX models in vivo. |
| Molecular Weight | 406.48 |
| Formula | C22H26N6O2 |
| CAS Number | 2589531-76-8 |
| Solubility (25°C) | DMSO 12 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PARP Products |
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| 2-Methylquinazolin-4-ol
2-Methylquinazolin-4-ol is a potent competitive poly(ADP-ribose) synthetase inhibitor, with a Ki of 1.1 μM. 2-Methylquinazolin-4-ol mammalian aspartate transcarbamylase (ATCase) inhibitor, with IC50 of 0.20 mM. |
| DPQ
DPQ is a potent PARP-1 inhibitor. |
| OUL232
OUL232 is a potent inhibitor of mono-ARTs PARP7, PARP10, PARP11, PARP12, PARP14, and PARP15. |
| AZ3391
AZ3391 is a potent inhibitor of PARP. |
| PARP1-IN-5
PARP1-IN-5 is a low toxicity, orally active, potent and selective PARP-1 inhibitor (IC50 =14.7 nM). |
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