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Rucaparib is a potent inhibitor of purified full-length human PARP-1 and shows higher inhibition of cellular PARP in LoVo and SW620 cells. Besides, Rucaparib binds detectably to eight other PARP domains, including PARP2, 3, 4, 10, 15, 16, TNKS1 and TNKS2. Rucaparib inhibits PARP-1 activity by 97.1% at a concentration of 1 μM in permeabilised D283Med cells.Rucaparib significantly potentiates the cytotoxicity of topotecan and temozolomide in NB-1691, SH-SY-5Y, and SKNBE (2c) cells. Rucaparib enhances the antitumor activity of temozolomide and indicates complete and sustained tumor regression in NB1691 and SHSY5Y xenografts.
Invest New Drugs. 2018 Jun 6.
The poly (ADP-ribose) polymerase inhibitor rucaparib suppresses proliferation and serves as an effective radiosensitizer in cervical cancer
Rucaparib purchased from AbMole
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Source | Invest New Drugs (2018). Figure 5. Rucaparib (AbMole BioScience) |
| Method | intraperitoneally | |
| Cell Lines | female BALB/c nude mice | |
| Concentrations | 8 mg/kg | |
| Incubation Time | 4 weeks | |
| Results | The tumor volume in the rucaparib treatment group was less than that in the control group (P<0.05), indicating that rucaparib inhibited tumor growth |
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Source | Invest New Drugs (2018). Figure 4. Rucaparib (AbMole BioScience) |
| Method | Immunofluorescence | |
| Cell Lines | Hela and Siha cells | |
| Concentrations | 10 μmol/L | |
| Incubation Time | 24 hours | |
| Results | Compared with the radiotherapy group, the overall expression of DNA damage markers decreased slowly in the combined group, implying that rucaparib can block IR-induced DNA DSB repair, and enhance the sensitivity to radiotherapy by cervical cancer cells. |
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Source | Invest New Drugs (2018). Figure 3. Rucaparib (AbMole BioScience) |
| Method | Clonogenic assay | |
| Cell Lines | Hela and Siha cells | |
| Concentrations | 0, 1, 5, or 10 μmol/L | |
| Incubation Time | 24 hours | |
| Results | The clonogenic assay showed that rucaparib combined with radiotherapy inhibited the ability of cervical cancer cells to form colonies, with the effect exacerbated with an increasing drug concentration |
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Source | Invest New Drugs (2018). Figure 2. Rucaparib (AbMole BioScience) |
| Method | Flow cytometry | |
| Cell Lines | Hela and Siha cells | |
| Concentrations | 0, 1, 5, 10, 20, 40, or 80 umol/L | |
| Incubation Time | 48 h | |
| Results | At rucaparib concentrations of 0 μM, 20 μM, and 40 μM, the proportions of Hela cells in the G2/M phase were 25.11%, 31.11%, and 35.78%, respectively; while the proportions of Siha cells in the G2/M phase were 16.09%, 26.71%, and 32.22%, respectively |
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Source | Invest New Drugs (2018). Figure 1. Rucaparib (AbMole BioScience) |
| Method | CCK-8 assay | |
| Cell Lines | Hela and Siha cells | |
| Concentrations | 20 μM, 40 μM | |
| Incubation Time | 72 h | |
| Results | CCK-8 results showed that the viability of cells decreased significantly as the concentration of rucaparib gradually increased |
| Molecular Weight | 323.36 |
| Formula | C19H18FN3O |
| CAS Number | 283173-50-2 |
| Solubility (25°C) | DMSO 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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AG-014699 (PF-01367338, Rucaparib) is a PARP inhibitor with a Ki of 1.4 nM. |
| AG14361
AG14361 is a novel poly (ADP-ribose) polymerase-1 inhibitor with a GI50 of 10.9 µM. |
| AZD2281 (Olaparib)
AZD 2281 (Olaparib, KU-0059436) is a potent PARP (poly ADP-ribose polymerase) inhibitorwith IC50 of 5 and 1 nM for PARP-1and PARP-2 respectively. Olaparib is an autophagy and mitophagy activator. |
| Talazoparib
Talazoparib (BMN-673) is a highly potent, orally active PARP1/2 inhibitor.Talazoparib inhibits PARP1 and PARP2 enzyme activity with Kis of 1.2 nM and 0.87 nM, respectively. Talazoparib has antitumor activity. |
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