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A-966492 is a highly potent and efficacious poly (ADP-ribose) polymerase (PARP) inhibitor with a Ki and EC50 of 1 nM. In addition, it is orally bioavailable across multiple species, crosses the blood-brain barrier, and appears to distribute into tumor tissue. It also demonstrated good in vivo efficacy in a B16F10 subcutaneous murine melanoma model in combination with temozolomide and in an MX-1 breast cancer xenograft model both as a single agent and in combination with carboplatin.
| Cell Experiment | |
|---|---|
| Cell lines | C41 cell |
| Preparation method | Treating C41 cells with A-966492 for 30 minutes in a 96-well plate . Activating PARP by damaging DNA with 1 mM H2O2 for 10 minutes. Washing cells with ice-cold phosphate-buffered saline (PBS) once and fixing with prechilled methanol/acetone (7:3) at -20 °C for 10 minutes. When they are air-dried, rehydrating plates with PBS and blocked using 5% nonfat dry milk in PBS-Tween(0.05%) (blocking solution) for 30 minutes at room temperature. Incubating cell with anti-PAR antibody 10H (1:50) in blocking solution at room temperature for 60 minutes followed by washing with PBS-Tween20 five times, and incubation with goat antimouse fluorescein 5(6)-isothiocyanate (FITC)-coupled antibody (1:50) and 1 μg/mL 40,6-diamidino-2-phenylindole (DAPI) in blocking solution at room temperature for 60 minutes. After washing with PBS-Tween20 5 times, using an fmax Fluorescence Microplate Reader set at the excitation and emission wavelength for FITC or the excitation and emission wavelength for DAPI to perform analysis. Normalizing PARP activity (FITC signal) with cell numbers (DAPI). |
| Concentrations | ~10 nM |
| Incubation time | 30 minutes |
| Animal Experiment | |
|---|---|
| Animal models | A 0.2 cc amount of a 1:10 dilution of tumor brei in 45% Matrigel and 45% Spinner MEM is injected subcutaneously into the flank of female SCID mice. |
| Formulation | |
| Dosages | 12.5, 25, and 50 mg/kg/day, for 14 days |
| Administration | Orally administrated |
| Molecular Weight | 324.35 |
| Formula | C18H17FN4O |
| CAS Number | 934162-61-5 |
| Solubility (25°C) | DMSO 60 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 |
|---|
| ABT-888
ABT-888 (Veliparib) is a potent inhibitor of PARP-1 and PARP-2 with Ki values of 5.2nM and 2.9nM respectively. |
| AG-014699 phosphate
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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