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Purity: ≥98%
Niraparib HCl (MK-4827; MK4827; Zejula), the hydrochloride salt of Niraparib, is a PARP1/2 inhibitor that has been approved by for the maintenance 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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| ln Vitro |
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| Enzyme Assay |
In a buffer containing pH 8.0, 1 mM DTT, 1 mM spermine, 50 mM KCl, 0.01% Nonidet P-40, and 1 mM MgCl2, the enzyme assay is carried out. The components of the PARP reaction are as follows: 1.5 μM NAD+, 150 nM biotinylated NAD+, 1 μg/mL activated calf thymus, 0.1 μCi [3H]NAD+ (200 000 DPM), and 1.5 nM PARP-1. In white 96-well plates, 50 μL volumes are used for autoreactions that use SPA bead-based detection. Niraparib is one of the compounds that are prepared in 96-well plates using an 11-point serial dilution method, with 5 μL/well in 5% DMSO/H2O (10× concentrated). The reactions commence with the addition of 35 μL of PARP-1 enzyme in buffer, followed by a 5-minute room temperature incubation period and the addition of 10 μL of NAD+ and DNA substrate mixture. These reactions are stopped after three hours at room temperature by adding 50 μL of streptavidin-SPA beads (2.5 mg/mL in 200 mM EDTA, pH 8). They are counted using a TopCount microplate scintillation counter after five minutes. Inhibition curves at different substrate concentrations are used to calculate IC50 values[1].
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| Cell Assay |
The HT Universal Chemiluminescent PARP Assay Kit is used to examine the inhibition of PARP in A549 and H1299 cells. In brief, trypsinization and transfer of the cells to a pre-chilled tube follow a treatment of cells with DMSO or 1 μM niraparib for 15, 30, 60, or 120 minutes. After two cold PBS washes, the cells are resuspended in cold PARP extraction buffer. The cell suspensions undergo a 30-minute ice-soaking period punctuated by periodic vortexing to induce disruption of the cell membrane. When the suspensions are centrifuged, the supernatant is moved to an ice-filled tube that has already been chilled. The 96-well plate's histone-coated wells are rehydrated with 1X PARP buffer and left to incubate for half an hour 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[2].
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| References |
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| Molecular Formula |
C19H21CLN4O
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| Molecular Weight |
356.85
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| Exact Mass |
356.14
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| Elemental Analysis |
C, 63.95; H, 5.93; Cl, 9.93; N, 15.70; O, 4.48
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| CAS # |
1038915-64-8
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| Related CAS # |
1038915-64-8 (HCl); 1038915-73-9; 1613220-15-7 (tosylate hydrate);1038915-60-4; 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 |
C1C[C@H](CNC1)C2=CC=C(C=C2)N3C=C4C=CC=C(C4=N3)C(=O)N.Cl
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| InChi Key |
YXYDNYFWAFBCAN-PFEQFJNWSA-N
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| InChi Code |
InChI=1S/C19H20N4O.ClH/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;/h1,3,5-9,12,14,21H,2,4,10-11H2,(H2,20,24);1H/t14-;/m1./s1
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| Chemical Name |
2-[4-[(3S)-piperidin-3-yl]phenyl]indazole-7-carboxamide;hydrochloride
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| Synonyms |
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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. |
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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: ≥ 2.08 mg/mL (5.83 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 20.8 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: ≥ 2.08 mg/mL (5.83 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 20.8 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.83 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (280.23 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8023 mL | 14.0115 mL | 28.0230 mL | |
| 5 mM | 0.5605 mL | 2.8023 mL | 5.6046 mL | |
| 10 mM | 0.2802 mL | 1.4011 mL | 2.8023 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 |
| NCT05183984 | Recruiting | Drug: Niraparib Drug: Chemotherapy |
Ovarian Cancer | ARCAGY/ GINECO GROUP | February 1, 2022 | Phase 2 |
| NCT04861181 | Recruiting | Biological: Pharmacokinetics, Dosage of Niraparib |
Adult Patients With Platinum- sensitive, Relapsed, High Grade Serous Epithelial Ovarian Cancer |
Hospices Civils de Lyon | May 5, 2021 | Phase 4 |
| NCT05694715 | Recruiting | Drug: Niraparib Drug: Irinotecan |
BRCA1 Mutation BRCA2 Mutation |
University of California, San Francisco |
May 23, 2023 | Phase 1 |
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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