| Size | Price | Stock | Qty |
|---|---|---|---|
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| 1g |
|
||
| 2g |
|
||
| Other Sizes |
|
| 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 )
|
|---|---|
| ln Vitro |
Niraparib (MK-4827) tosylate hydrate inhibits PARP activity with EC50=4 nM and EC90=45 nM in a whole cell assay. In the 10-100 nM range, Niraparib tosylate hydrate inhibits the growth of cancer cells expressing mutant BRCA-1 and BRCA-2 with CC50. In a whole cell assay, niraparib tosylate hydrate exhibits good inhibition of PARP 1 and 2 (IC50=3.8 and 2.1 nM, respectively)[1].
Niraparib tosylate hydrate suppresses PARP within 15 minutes of treatment, with the A549 cells showing 85% inhibition at 1 hour and the H1299 cells showing about 55% inhibition at 1 hour[2]. |
| ln Vivo |
Niraparib (MK-4827) tosylate hydrate is well tolerated and effective when used alone in a xenograft model of BRCA-1 deficient cancer[1].
Niraparib (MK-4827) tosylate hydrate is effective as a single agent in a xenograft model of cancer lacking BRCA-1 and is well tolerated in vivo[1]. Niraparib (MK-4827) tosylate hydrate is defined by very high volume of distribution (Vdss=6.9 L/kg), long terminal half-life (t1/2=3.4 h), superb bioavailability (F=65%), and acceptable pharmacokinetics in rats with plasma clearance of 28 (mL/min)/kg[1]. Niraparib (MK-4827) tosylate hydrate increases the p53 mutant Calu-6 tumor's radiation response in both situations, with a single daily dosage of 50 mg/kg working better than two doses of 25 mg/kg[3]. |
| Cell Assay |
The assays for proliferation were carried out in 96-well black viewplates. 300 cells/well (250 cells/well for BRCA-1 wt) were plated in 190 μL/well of culture medium (DMEM containing 10% FCS, 0.1 mg/mL penicillin-streptomycin, and 2 mM L-glutamine), which was then incubated for four hours at 37°C in an atmosphere of 5% CO2. After that, inhibitors were added in 10-μL/well serial dilutions to achieve the target final compound concentration in 0.5% DMSO. Following a 7-day incubation period at 37°C with 5% CO2, the viability of the cells was evaluated. In summary, 100 μL/well of prediluted 1:10 CellTiter-Blue solution was added, and the cells were incubated for 45 minutes at 37°C with 5% CO2 and then for an additional 15 minutes at room temperature in the dark. By reading the plate at the fluorimeter, excitation at 550 nm, and emission at 590 nm, the number of living cells was ascertained. The percentage growth of the cells in comparison to the vehicle-treated cells was used to express cell growth. It was established what concentration (CC50) would stop cell growth 50% of the time.
|
| Animal Protocol |
Female nude mice
25 mg/kg twice daily or 50 mg/kg once daily oral administration |
| References |
|
| Molecular Formula |
C26H30N4O5S
|
|---|---|
| Molecular Weight |
510.6052
|
| Exact Mass |
510.19
|
| Elemental Analysis |
C, 61.16; H, 5.92; N, 10.97; O, 15.67; S, 6.28
|
| CAS # |
1613220-15-7
|
| Related CAS # |
1038915-64-8 (HCl); 1038915-73-9; 613220-15-7 (tosylate hydrate); 1038915-60-4; 1038915-58-0
|
| Appearance |
Solid powder
|
| 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.O
|
| InChi Key |
ACNPUCQQZDAPJH-FMOMHUKBSA-N
|
| InChi Code |
InChI=1S/C19H20N4O.C7H8O3S.H2O/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);1H2/t14-;;/m1../s1
|
| Chemical Name |
4-methylbenzenesulfonic acid;2-[4-[(3S)-piperidin-3-yl]phenyl]indazole-7-carboxamide;hydrate
|
| Synonyms |
MK-4827; MK-4827; MK4827; MK4827-tosylate; Niraparib tosylate
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO: ~64 mg/mL (~199.8 mM)
Ethanol: ~64 mg/mL |
|---|---|
| Solubility (In Vivo) |
5%DMSO+ 40%PEG300+ 5%Tween 80+ 50%ddH2O: 2.5mg/ml (7.80mM) (Please use freshly prepared in vivo formulations for optimal results.)
|
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9584 mL | 9.7922 mL | 19.5844 mL | |
| 5 mM | 0.3917 mL | 1.9584 mL | 3.9169 mL | |
| 10 mM | 0.1958 mL | 0.9792 mL | 1.9584 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 |
| NCT03601923 | Active Recruiting |
Drug: Niraparib | Pancreatic Cancer | Dana-Farber Cancer Institute | August 22, 2018 | Phase 2 |
| NCT04313504 | Active Recruiting |
Drug: Niraparib Drug: Dostarlimab |
Head and Neck Cancer | Trisha Wise-Draper | November 4, 2020 | Phase 2 |
| NCT03016338 | Active Recruiting |
Drug: Niraparib Drug: TSR-042 |
Endometrial Cancer | University Health Network, Toronto |
November 6, 2017 | Phase 2 |
| NCT03326193 | Active Recruiting |
Drug: Niraparib Biological: Bevacizumab |
Ovarian Neoplasms | Tesaro, Inc. | December 12, 2017 | Phase 2 |
| NCT03840967 | Active Recruiting |
Drug: Niraparib | Esophageal Cancer Adenocarcinoma Gastric Cancer |
Shadia Jalal, MD | July 9, 2019 | Phase 2 |
|
|
|
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
