Home Tools
Log in
Cart

Niraparib tosylate

Catalog No. T6892   CAS 1038915-73-9
Synonyms: MK-4827 (tosylate), MK 4827 tosylate, Niraparib (MK-4827) tosylate

Niraparib tosylate (MK-4827 (tosylate))(with IC50 of 3.8 nM/2.1 nM) is a selective PARP1/PARP2 inhibitor.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Niraparib tosylate Chemical Structure
Niraparib tosylate, CAS 1038915-73-9
Pack Size Availability Price/USD Quantity
2 mg In stock $ 38.00
5 mg In stock $ 61.00
10 mg In stock $ 85.00
25 mg In stock $ 119.00
50 mg In stock $ 150.00
100 mg In stock $ 243.00
500 mg In stock $ 593.00
1 mL * 10 mM (in DMSO) In stock $ 66.00
Bulk Inquiry
Get quote
Select Batch  
Contact us for more batch information
Biological Description
Chemical Properties
Storage & Solubility Information
Description Niraparib tosylate (MK-4827 (tosylate))(with IC50 of 3.8 nM/2.1 nM) is a selective PARP1/PARP2 inhibitor.
Targets&IC50 PARP2:2.1 nM, PARP1:3.8 nM
In vitro Micromolar concentrations of niraparib radiosensitizes tumor cell lines derived from lung, breast, and prostate cancers independently of their p53 status but not cell lines derived from normal tissues. Niraparib also sensitizes tumor cells to Water2 and converts Water2-induced single strand breaks (SSBs) into DSBs during DNA replication[5].
In vivo MK-4827 strongly enhances the effect of radiation on a variety of human tumor xenografts, both p53 wild type and p53 mutant. MK-4827 reduces PAR levels in tumors by 1 h after administration which persisted for up to 24 h[1]. In vivo treatment with MK-4827 and radiation prolonged survival (p<0.01) compared to single modalities. In vivo superiority of MK-4827 plus radiation is further documented by significant elevations of cleaved caspase-3 and γ-H2AX in tumors from the combination group compared to single modality cohorts[4].
Kinase Assay Enzyme assay is conducted in buffer containing 25 mM Tris, pH 8.0, 1 mM DTT, 1 mM spermine, 50 mM KCl, 0.01% Nonidet P-40, and 1 mM MgCl2. PARP reaction contains 0.1 μCi [3H]NAD+ (200 000 DPM), 1.5 μM NAD+, 150 nM biotinylated NAD+, 1 μg/mL activated calf thymus, and 1?5 nM PARP-1. Autoreactions utilizing SPA bead-based detection are carried out in 50 μL volumes in white 96-well plates. Compounds (e.g., MK-4827) are prepared in 11-point serial dilution in 96-well plate, 5 μL/well in 5% DMSO/Water (10× concentrated). Reactions are initiated by adding first 35 μL of PARP-1 enzyme in buffer and incubating for 5 min at room temperature and then 10 μL of NAD+ and DNA substrate mixture. After 3 h at room temperature, these reactions are terminated by the addition of 50 μL of streptavidin-SPA beads (2.5 mg/mL in 200 mM EDTA, pH 8). After 5 min, they are counted using a TopCount microplate scintillation counter. IC50 data is determined from inhibition curves at various substrate concentrations[1].
Cell Research V-C8 (BRCA2-negative) Chinese hamster cells are treated with the PARP inhibitor MK-4827 for 24 h, washed and incubated in drug-free medium for 5-7 days until colonies formed. (Only for Reference)
Synonyms MK-4827 (tosylate), MK 4827 tosylate, Niraparib (MK-4827) tosylate
Molecular Weight 492.59
Formula C19H20N4O·C7H8O3S
CAS No. 1038915-73-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 91 mg/mL (184.7 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Wang L, et al. Invest New Drugs. 2012, 30(6):2113-20. 2. Patel AG, et al. J Biol Chem. 2012, 287(6):4198-210. 3. Jones P, et al. J Med Chem. 2009, 52(22):7170-85. 4. Mueller S, et al. Anticancer Res. 2013, 33(3):755-62. 5. Bridges KA, et al. oncotarget. 2014, 5(13):5076-86.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Anti-Cancer Drug Library Anti-Cancer Approved Drug Library Bioactive Compound Library Anti-Pancreatic Cancer Compound Library DNA Damage & Repair Compound Library Anti-Cancer Compound Library Drug Repurposing Compound Library Apoptosis Compound Library

Related Products

Related compounds with same targets
Oxcarbazepine Stachyose tetrahydrate Palomid 529 Angiotensin II human WHI-P154 Oxibendazole DEL-22379 AES-350

TargetMolDose Conversion

You can also refer to dose conversion for different animals. More

TargetMol In vivo Formulation Calculator (Clear solution)

Step One: Enter information below
Dosage
mg/kg
Average weight of animals
g
Dosing volume per animal
ul
Number of animals
Step Two: Enter the in vivo formulation
% DMSO
%
% Tween 80
% ddH2O
Calculate Reset

TargetMolCalculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculation
Molecular Weight Calculator
=
X
X

Molarity Calculator allows you to calculate the

  • Mass of a compound required to prepare a solution of known volume and concentration
  • Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Concentration of a solution resulting from a known mass of compound in a specific volume
See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

X
=
X

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

=
/

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Niraparib tosylate 1038915-73-9 Apoptosis Chromatin/Epigenetic DNA Damage/DNA Repair PARP MK-4827 (tosylate) MK 4827 tosylate inhibit MK-4827 Tosylate MK4827 Niraparib Tosylate bioavailable cancer damage poly ADP ribose polymerase breast MK 4827 Tosylate Inhibitor MK-4827 anti-tumor orally ovarian Niraparib (MK-4827) tosylate MK4827 Tosylate MK 4827 lung Niraparib DNA Niraparib (MK-4827) Tosylate inhibitor

 

TargetMol