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Purity: ≥98%
Olaparib (formerly also known as AZD-2281; KU-59436; KU0059436; trade name Lynparza) is a potent, novel and orally bioavailable small molecule inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase (PARP) with potential anticancer activity. It has an IC50 of 1 nM for PARP2 and 5 nM for PARP1 that inhibits PARP. It might have antitumor, radiosensitizing, and chemosensitizing effects. Olaparib binds to PARP selectively and inhibits it, preventing PARP from repairing single-strand DNA breaks. By inhibiting PARP, agents that damage DNA may be more cytotoxic and may reverse the radioresistance and chemoresistance of tumor cells. In 2014, the FDA approved olaparib for the treatment of advanced ovarian cancer.
| Targets |
PARP-2 ( IC50 = 1 nM ); PARP-1 ( IC50 = 5 nM ); tankyrase-1 ( IC50 = 1.5 μM ); Autophagy; Mitophagy
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
The assay assessed Olaparib's capacity to suppress PARP-1 enzyme activity. An alternative method of measuring PARP-2 activity inhibition involves binding down the recombinant PARP-2 protein in a 96-well plate with white walls using an antibody specific to PARP-2. Measurements of PARP-2 activity are made after 3H-NAD+ DNA additions. Scintillant is added after washing in order to quantify 3H-incorporated ribosylations. An AlphaScreen assay for tankyrase-1 is created, involving the incubation of HIS-tagged recombinant TANK-1 protein in a 384-well ProxiPlate assay with biotinylated NAD+. A proximity signal is produced by adding alpha beads to bind the HIS and biotin tags; the loss of this signal is directly correlated with TANK-1 activity inhibition. At least three replications of each experiment are conducted.
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| Cell Assay |
The potentiation factor, or PF50 value, is determined by dividing the IC50 of the alkylating agent methylmethane sulfonate (MMS) used in the control growth by the IC50 of the MMS plus PARP inhibitor. Olaparib is tested for MMS screening at a fixed 200 nM concentration using HeLa B cells. The concentrations of olaparib that are tested on the colorectal cell line SW620 are 1, 3, 10, 100, and 300 nM. Sulforhodamine B (SRB) assay is used to measure cell growth.
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| Animal Protocol |
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| References |
| Molecular Formula |
C24H23FN4O3
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| Molecular Weight |
434.46
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| Exact Mass |
434.175
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| Elemental Analysis |
C, 66.35; H, 5.34; F, 4.37; N, 12.90; O, 11.05
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| CAS # |
763113-22-0
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| Related CAS # |
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| Appearance |
White solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.702
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| LogP |
1.9
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| SMILES |
FC1C([H])=C([H])C(C([H])([H])C2C3=C([H])C([H])=C([H])C([H])=C3C(N([H])N=2)=O)=C([H])C=1C(N1C([H])([H])C([H])([H])N(C([H])([H])C1([H])[H])C(C1([H])C([H])([H])C1([H])[H])=O)=O
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| InChi Key |
FDLYAMZZIXQODN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H23FN4O3/c25-20-8-5-15(14-21-17-3-1-2-4-18(17)22(30)27-26-21)13-19(20)24(32)29-11-9-28(10-12-29)23(31)16-6-7-16/h1-5,8,13,16H,6-7,9-12,14H2,(H,27,30)
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| Chemical Name |
4-[[3-[4-(cyclopropanecarbonyl)piperazine-1-carbonyl]-4-fluorophenyl]methyl]-2H-phthalazin-1-one
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| Synonyms |
AZD2281; Ku-0059436; AZD2281; AZD-2281; AZD 2281; KU59436; KU-59436; KU 59436; KU0059436; KU-0059436; KU 0059436; Olaparib; trade name Lynparza
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 10 mg/mL (23.02 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 100.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 5 mg/mL (11.51 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 5 mg/mL (11.51 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.5 mg/mL (5.75 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 5: ≥ 2.5 mg/mL (5.75 mM) (saturation unknown) in 10% DMF 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 6: ≥ 2.5 mg/mL (5.75 mM) (saturation unknown) in 10% DMF 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 7: ≥ 2.5 mg/mL (5.75 mM) (saturation unknown) in 10% DMF 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 8: ≥ 2.08 mg/mL (4.79 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 9: ≥ 0.5 mg/mL (1.15 mM) (saturation unknown) in 1% DMSO 99% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 10: 20 mg/mL (46.03 mM) in 0.5% CMC-Na/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3017 mL | 11.5085 mL | 23.0171 mL | |
| 5 mM | 0.4603 mL | 2.3017 mL | 4.6034 mL | |
| 10 mM | 0.2302 mL | 1.1509 mL | 2.3017 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02446704 | Active Recruiting |
Drug: Olaparib Drug: Temozolomide |
Small Cell Lung Cancer | Zofia Piotrowska | October 13, 2015 | Phase 1 Phase 2 |
| NCT03641755 | Active Recruiting |
Drug: Olaparib Drug: Sapacitabine |
Breast Cancer | Dana-Farber Cancer Institute | October 1, 2018 | Phase 1 |
| NCT03047135 | Active Recruiting |
Drug: Olaparib | Prostate | Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins |
March 1, 2017 | Phase 2 |
| NCT04123366 | Active Recruiting |
Biological: Pembrolizumab Drug: Olaparib |
Solid Tumors | Merck Sharp & Dohme LLC | November 18, 2019 | Phase 2 |
| NCT04076579 | Active Recruiting |
Drug: Olaparib Drug: Trabectedin |
Sarcoma Sarcoma Metastatic |
University of Michigan Rogel Cancer Center |
March 17, 2020 | Phase 2 |
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