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Purity: ≥98%
Niraparib Tosylate (also known as MK-4827; MK4827; Zejula), the tosylate salt of niraparib, is an orally bioavailable and selective inhibitor of PARP1/2 (IC50 = 3.8 nM and 2.1nM) that gained FDA approval in March 2017 for the treatment of recurrent epithelial ovarian, fallopian tube, or primary peritoneal cancer.
| Targets |
PARP-2 ( IC50 = 2.1 nM ); PARP-1 ( IC50 = 3.8 nM ); V-PARP ( IC50 = 330 nM ); TANK-1 ( IC50 = 570 nM ); PARP-3 ( IC50 = 1300 nM )
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| Enzyme Assay |
In a whole cell assay, MK-4827 inhibits PARP activity with EC(50) = 4 nM and prevents the growth of cancer cells expressing mutant BRCA-1 and BRCA-2 with CC(50) in the 10-100 nM range. It also exhibits excellent inhibition of PARP 1 and 2 with IC(50) = 3.8 and 2.1 nM, respectively.
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| Cell Assay |
A549 and H1299 cells are used to examine the inhibition of PARP using the HT Universal Chemiluminescent PARP Assay Kit. In summary, cells are trypsinized, treated for 15, 30, 60, or 120 minutes with DMSO or 1 μM Niraparib (MK-4827), and then moved to a tube that has been chilled beforehand. The cells are resuspended in cold PARP extraction buffer after being twice rinsed with ice-cold PBS. To break down the cell membrane, the cell suspensions are vortexed periodically while being incubated on ice for 30 minutes. After centrifuging the suspensions, the supernatant is moved to an ice-filled tube that has already been chilled. After being rehydrated with 1X PARP buffer, the histone-coated wells in the 96-well plate are incubated for 30 minutes at room temperature. Remove the PARP buffer, then add 1X PARP buffer, diluted PARP-HSA enzyme, and 20 μg of protein as measured by the Bio-Rad Protein Assay to each well. After 60 minutes of room temperature incubation, the strip wells are twice cleaned with PBS containing 0.1% Triton X-100 and then again with PBS. In the strip wells, diluted Strep-HRP is added, and they are then allowed to sit at room temperature for 60 minutes. Just like before, the wells are cleaned. Chemiluminescent readings are promptly obtained using a plate-reader after equal volumes of PeroxyGlow A and B are mixed and added to the wells.
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| References |
| Molecular Formula |
C26H28N4O4S
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| Molecular Weight |
492.59
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| Exact Mass |
492.18
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| Elemental Analysis |
C, 63.40; H, 5.73; N, 11.37; O, 12.99; S, 6.51
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| CAS # |
1038915-73-9
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| Related CAS # |
1038915-73-9;1613220-15-7 (tosylate hydrate); 1038915-60-4; 1038915-64-8 (HCl); 1476777-06-6 (Niraparib metabolite M1); 1038915-58-0 (Niraparib R-enantiomer)
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| Appearance |
Light yellow solid powder
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| SMILES |
CC1=CC=C(C=C1)S(=O)(=O)O.C1C[C@H](CNC1)C2=CC=C(C=C2)N3C=C4C=CC=C(C4=N3)C(=O)N
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| InChi Key |
LCPFHXWLJMNKNC-PFEQFJNWSA-N
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| InChi Code |
InChI=1S/C19H20N4O.C7H8O3S/c20-19(24)17-5-1-3-15-12-23(22-18(15)17)16-8-6-13(7-9-16)14-4-2-10-21-11-14;1-6-2-4-7(5-3-6)11(8,9)10/h1,3,5-9,12,14,21H,2,4,10-11H2,(H2,20,24);2-5H,1H3,(H,8,9,10)/t14-;/m1./s1
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| Chemical Name |
4-methylbenzenesulfonic acid;2-[4-[(3S)-piperidin-3-yl]phenyl]indazole-7-carboxamide;hydrate
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| Synonyms |
MK-4827 tosylate; MK 4827; MK4827 tosylate; MK 4827 tosylate; MK-4827; MK4827; Niraparib; Niraparib HCl; Niraparib hydrochloride; Zejula
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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: ≥ 2.5 mg/mL (5.08 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.08 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. 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. View More
Solubility in Formulation 3: ≥ 0.5 mg/mL (1.02 mM) (saturation unknown) in 1% DMSO 99% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0301 mL | 10.1504 mL | 20.3009 mL | |
| 5 mM | 0.4060 mL | 2.0301 mL | 4.0602 mL | |
| 10 mM | 0.2030 mL | 1.0150 mL | 2.0301 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 |
| NCT04221503 | Active Recruiting |
Drug: Niraparib Device: Optune |
Glioblastoma Recurrent Glioblastoma |
University of Pennsylvania | December 30, 2019 | Phase 2 |
| NCT04481113 | Active Recruiting |
Drug: Niraparib Tosylate Monohydrate Drug: Abemaciclib |
Invasive Breast Carcinoma Multifocal Breast Carcinoma |
OHSU Knight Cancer Institute | June 7, 2021 | Phase 1 |
| NCT04030559 | Recruiting | Drug: Niraparib Tosylate Monohydrate Drug: Niraparib |
ATM Gene Mutation BRCA1 Gene Mutation |
University of California, Davis | February 25, 2020 | Phase 2 |
| NCT05689021 | Recruiting | Procedure: Bone Scan Drug: Prednisone |
Stage IV Prostate Cancer AJCC v8 Metastatic Prostate Adenocarcinoma |
Mayo Clinic | July 7, 2023 | Phase 2 |
| NCT05455424 | Recruiting | Drug: Niraparib Oral Product Other: Active Symptom Control |
Mesothelioma, Malignant | University Hospital Southampton NHS Foundation Trust |
July 11, 2022 | Phase 2 |
Abstract Image J Med Chem.2009 Nov 26;52(22):7170-85.
Differential biochemical trapping of PARP1 by clinical PARP inhibitors.Cancer Res.2012 Nov 1;72(21):5588-99. |
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Three clinical PARP inhibitors differ in their potency to poison PARP1 and PARP2 irrespective of their potency to inhibit PARP catalytic activity.Cancer Res.2012 Nov 1;72(21):5588-99. |
Differential cellular trapping of PARP1 and PARP2 by clinical PARP inhibitors.Cancer Res.2012 Nov 1;72(21):5588-99. |
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