Niraparib tosylate

Catalog No.S7625 Batch:S762508

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Technical Data

Formula

C19H20N4O.C7H8O3S
Molecular Weight 492.59 CAS No. 1038915-73-9
Solubility (25°C)* In vitro DMSO 99 mg/mL (200.97 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
4.95mg/ml Taking the 1 mL working solution as an example, add 50 μL of 99 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Niraparib tosylate is a selective inhibitor of PARP1/PARP2 with IC50 of 3.8 nM/2.1 nM. Niraparib increases formation of PARP-DNA complexes resulting in DNA damage, apoptosis, and cell death.
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 (from reference)

Cell Assay:

[2]
  • 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.
Animal Study:

[1]
  • Animal Models

    Female nude mice (Ncr Nu/Nu)

  • Dosages

    25 or 50 mg/kg

  • Administration

    p.o.

Customer Product Validation

Data from [Data independently produced by , , Cell Death & Disease, 2017, 8: e3070]

Selleck's Niraparib tosylate has been cited by 39 publications

Detection of senescence using machine learning algorithms based on nuclear features [ Nat Commun, 2024, 15(1):1041] PubMed: 38310113
BRCA2 Germline Mutations Identify Gastric Cancers Responsive to PARP Inhibitors [ Cancer Res, 2023, 83(10):1699-1710] PubMed: 37129948
Temozolomide Sensitizes ARID1A-Mutated Cancers to PARP Inhibitors [ Cancer Res, 2023, 83(16):2750-2762] PubMed: 37306706
OGG1 Inhibition Triggers Synthetic Lethality and Enhances The Effect of PARP Inhibitor Olaparib in BRCA1-Deficient TNBC Cells [ Front Oncol, 2022, 12:888810] PubMed: 35619904
Novel Paired Normal Prostate and Prostate Cancer Model Cell Systems Derived from African American Patients [ Cancer Res Commun, 2022, 2(12):1617-1625] PubMed: 36970725
Translational evidence for RRM2 as a prognostic biomarker and therapeutic target in Ewing sarcoma [ Mol Cancer, 2021, 20(1):97] PubMed: 34315482
Targeting immunosuppressive macrophages overcomes PARP inhibitor resistance in BRCA1-associated triple-negative breast cancer [ Nat Cancer, 2021, 2(1):66-82] PubMed: 33738458
Targeting immunosuppressive macrophages overcomes PARP inhibitor resistance in BRCA1-associated triple-negative breast cancer [ Nat Cancer, 2021, 2(1):66-82] PubMed: 33738458
A subset of PARP inhibitors induces lethal telomere fusion in ALT-dependent tumor cells [ Sci Transl Med, 2021, 13(592)eabc7211] PubMed: 33952676
Histone Parylation factor 1 contributes to the inhibition of PARP1 by cancer drugs [ Nat Commun, 2021, 12(1):736] PubMed: 33531508

RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.