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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related PARP Products |
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| DSB-1522
DSB-1522 is a PARP1 inhibitor that can be used in tumor-related studies. |
| DM-5167
DM-5167 is a PARP1 inhibitor that can be used in studies related to triple negative breast cancer. |
| NMS-03305293
NMS-03305293 is a PARP inhibitor with high selectivity for PARP1 isoforms and low DNA capture effect, which specifically kills BRCA mutated tumor cells. In addition, NMS-03305293 can penetrate the blood-brain barrier and can be used in studies related to CNS tumors and brain metastatic tumors. |
| SNV1521
SNV1521 is a potential best-in-class (BIC), highly selective and CNS-permeable PARP1 inhibitor. |
| Basroparib
Basroparib is an orally active selective inhibitor of end-anchor polymerase (TNKS) and an inhibitor of ribose polymerase (PARP) with antitumor activity. |
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