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AZD 2281 (Olaparib, KU-0059436) is a novel, potent orally active PARP (poly ADP-ribose polymerase) inhibitorwith IC50 of 5 and 1 nM for PARP-1and PARP-2 respectively. AZD 2281 (Olaparib, KU-0059436) acts as an inhibitor of the enzyme Poly ADP ribose polymerase (PARP) and is one of the first PARP inhibitors.It induces cancer specific synthetic lethality in homologous recombination repair defective cells, including BRCA-deficient tumors. Olaparib is an autophagy and mitophagy activator.
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Application | Transmission electron microscopy |
| Results | The growth inhibition effect of AZD2281 was significantly higher in the BRCA wild-type cell lines with BRCA1 allelic loss than in the BRCA wild-type cell line without BRCA1 allelic loss. |
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Application | apoptosis assay |
| Results | Inhibition of autophagy by knocking down ATG5 also partially inhibited AZD2281-induced apoptosis, suggesting that autophagy contributes to AZD2281-induced cell death in BRCA mutated breast cancer cells. |
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Application | IP |
| Results | In mice co-treated with olaparib and MK-2206, tumor volume was only increased ~1.8-fold at this same time, indicating that these agents exerted a additive effect on tumor growth. |
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Application | IP |
| Results | The overall RTVs (treated vs. non-treated tumors) for mice bearing Brca1-mutant tumor allografts were 60.8% and 62.6% for mice treated with MK-2206 and olaparib, respectively. |
| Cell Experiment | |
|---|---|
| Cell lines | SW620 colorectal cell line |
| Preparation method | Potentiation of MMS Cytotoxicity by 47 Determined by the Use of Sulforhodamine B Cell Growth Assays. SW620 cells were seeded in 96-well plates and were left to attach overnight. Cells were preincubated with vehicle control (DMSO) or with a single concentration of KU-0059436 (1, 3, 10, 30, 100 or 300 nM) for 1 h before the addition of increasing concentrations of MMS. Cells were incubated in the presence of each drug combination for 4 days before cell growth was quantified by the use of an SRB assay.44 Data were calculated from triplicate wells as the mean percentage of cell growth relative to KU-0059436-only wells, and (SE and IC50 were calculated by the use of XL-FIT 4 software. SW620 cells showed <24% growth inhibition (>76% cell growth) when only KU-0059436 was used at concentrations below 300 nM (data not shown). |
| Concentrations | 1, 3, 10, 100 and 300 nM |
| Incubation time | 4 days |
| Animal Experiment | |
|---|---|
| Animal models | mouse bearing SW620 xenografted tumors |
| Formulation | methylcellulose/PBS |
| Dosages | 10 mg/kg once daily for 5 consecutive days |
| Administration | orally |
| Molecular Weight | 434.46 |
| Formula | C24H23FN4O3 |
| CAS Number | 763113-22-0 |
| Solubility (25°C) | DMSO 90 mg/mL DMF 45 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Marchetti et al. Expert Opin Investig Drugs. Olaparib , PARP1 inhibitor in ovarian cancer.
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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. |
| 3-Aminobenzamide
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MK-4827 (Niraparib) is a selective PARP1/2 inhibitor with an IC50 value of 3.8 nM/2.1 nM that increases the formation of PARP-DNA complexes through inhibition of PARPase activity, leading to DNA damage, apoptosis, PARP-1-dependent cell death (parthanatos) and cell death. Strong effector activity when acting on cancer cells harboring mutant BRCA-1 and BRCA-2. It is more than 330-fold more selective than PARP3, V-PARP and Tank1. |
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NVP-TNKS656 is a highly potent, selective, and orally active TNKS2 inhibitor with IC50 of 6 nM; > 300 fold selectivity against PARP1 and PARP2. |
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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. |
| LT-628
LT-628 is the racemate of BMN 673 and LT-674. |
| LT-674
LT-674 inhibits PARP-1 with an IC50 of 144 nM. |
| Iniparib
Iniparib is an irreversible, noncompetitive inhibitor of PARP1 that disrupts binding between PARP1 and DNA by interacting with the DNA binding domain. |
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