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ABT-888 (Veliparib) is a potent inhibitor of PARP-1 and PARP-2 with Ki values of 5.2nM and 2.9nM respectively. ABT-888 (Veliparib) inhibits PARPs, thereby inhibiting DNA repair and potentiating the cytotoxicity of DNA-damaging agents. ABT-888 (Veliparib) has good oral bioavailability, can cross the blood-brain barrier, and potentiates temozolomide, platinums, cyclophosphamide, and radiation in syngeneic and xenograft tumor models. This broad spectrum of chemopotentiation and radiopotentiation makes this compound an attractive candidate for clinical evaluation. Phase I study of PARP inhibitor ABT-888 in combination with topotecan in adults reveal that PARP inhibition can modulate the capacity to repair topoisomerase I-mediated DNA damage in the clinic.
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Source | Invest New Drugs (2013). Figure 4. ABT-888 |
| Method | Annexin V apoptosis assay | |
| Cell Lines | HCT-116 cells | |
| Concentrations | 0.5 μM | |
| Incubation Time | 4 h, 24 h or 48 h | |
| Results | Although little apoptosis was detected at the 24 h time point, a significant increase in apoptosis was observed at 48 h in the presence of SN38 or SN38 plus ABT-888 for both cell lines indicating that γH2AX preceded drug-inducedapoptosis. |
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Source | Invest New Drugs (2013). Figure 1. ABT-888 |
| Method | PARP inhibition assay | |
| Cell Lines | HCT-116 cells | |
| Concentrations | 0.5 μM | |
| Incubation Time | 24 h | |
| Results | To demonstrate that this change in activity was not due to altered protein expression, western blot analysis was performed on samples treated for 1 h or 24 h with 0.5 μM ABT-888, 10 nM SN38 or combinations of these two |
| Cell Experiment | |
|---|---|
| Cell lines | C41 cells |
| Preparation method | Cellular PARP Assay. C41 cells were treated with test compound for 30 min in a 96-well plate. PARP was activated by damaging DNA with 1 mM H2O2 for 10 min. Cells were washed with ice-cold PBS once and fixed with prechilled methanol/acetone (7:3) at -20 °C for 10 min. After air-drying, plates were rehydrated with PBS and blocked using 5% nonfat dry milk in PBS-tween (0.05%) (blocking solution) for 30 min at room temperature. Cells were incubated with anti-PAR antibody 10H (1:50) in blocking solution at room temperature for 60 min followed by washing with PBS-Tween20 5 times and incubation with goat antimouse fluorescein 5(6)-isothiocyanate (FITC)-coupled antibody (1:50) and 1 µg/mL 4′,6-diamidino-2-phenylindole (DAPI) in blocking solution at room temperature for 60 min. After washing with PBS-Tween20 5 times, analysis was performed using an fmax Fluorescence Microplate Reader set at the excitation and emission wavelength for FITC or the excitation and emission wavelength for DAPI. PARP activity (FITC signal) was normalized with cell numbers (DAPI). |
| Concentrations | 0~1uM |
| Incubation time | 30 min |
| Animal Experiment | |
|---|---|
| Animal models | MX-1 Tumor Model |
| Formulation | 2.5% EtOH, 1 drop TW-80, 25% PEG400, PBS |
| Dosages | 12.5mg/kg, BID, P6-11 |
| Administration | orally |
| Molecular Weight | 244.29 |
| Formula | C13H16N4O |
| CAS Number | 912444-00-9 |
| Solubility (25°C) | DMSO ≥45 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 |
|---|
| 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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