Niraparib (MK-4827) tosylate

Catalog No.S7625 Synonyms: Niraparib tosylate, MK 4827 tosylate

Niraparib (MK-4827) tosylate Chemical Structure

Molecular Weight(MW): 492.59

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

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  • Berberine activates PARP1 in ovarian cancer cells. PAR synthesis is detected by immunofluorescence staining in A2780 and HO8910 treated with different concentration of berberine alone or in combination with niraparib (10 μM) for 48 h. Top: representative examples of immunofluorescence staining of PAR. Scale bar, 20 μm. Bottom: quantification of PAR level in A2780 and HO8910. Immunofluorescence intensities were quantified by ImageJ. *P<0.05, **P<0.01

    Cell Death & Disease, 2017, 8: e3070. Niraparib (MK-4827) tosylate purchased from Selleck.

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Biological Activity

Description Niraparib (MK-4827) tosylate is a selective inhibitor of PARP1/PARP2 with IC50 of 3.8 nM/2.1 nM.
Targets
PARP2 [3]
(Cell-free assay)		 PARP1 [3]
(Cell-free assay)
2.1 nM 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 H2O2 and converts H2O2-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].

Protocol

Cell Research:

[2]
+ Expand
  • Cell lines: V-C8 cells
  • Concentrations: 50 nM
  • Incubation Time: 24 h
  • Method:

    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)
Animal Research:

[1]
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  • Animal Models: Female nude mice (Ncr Nu/Nu)
  • Formulation: Suspended in 0.5% Methocel in deionized water
  • Dosages: 25 or 50 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 98 mg/mL (198.94 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 492.59
Formula

C19H20N4O.C7H8O3S
CAS No. 1038915-73-9
Storage powder
in solvent
Synonyms Niraparib tosylate, MK 4827 tosylate

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PARP Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID