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AZD-2461 is a potent PARP inhibitor, with IC50s of 5 nM, 2 nM and 200 nM for PARP1, PARP2 and PARP3, respectively.
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Source | Cancer Res (2016). Figure 4. AZD2461 |
| Method | immunofluorescence | |
| Cell Lines | A549 cells | |
| Concentrations | 500 nmol/L | |
| Incubation Time | 1 hour | |
| Results | Unlike olaparib, which results in persistence of gH2AX following IR to the same degree as APLF knockdown, AZD2461 had no effect on gH2AX dynamics. |
| Molecular Weight | 395.43 |
| Formula | C22H22FN3O3 |
| CAS Number | 1174043-16-3 |
| Solubility (25°C) | DMSO 79 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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