Niraparib tosylate

SKU: orb1300371

Description

Niraparib tosylate is a potent and selective inhibitor of PARP1 and PARP2 enzymes, exhibiting IC50 values of 3.8 nM and 2.1 nM, respectively. It is widely used in cancer research, particularly for studying synthetic lethality in BRCA-deficient models, and has demonstrated efficacy in both in vitro cellular assays and in vivo tumor xenograft studies.

Research Area

Cell Biology, Epigenetics & Chromatin, Molecular Biology

Key Properties

• CAS Number: 1038915-73-9
• MW: 492.59
• Purity: 99.87% (May vary between batches)
• Formula: C₁₉H₂₀N₄O·C₇H₈O₃S
• SMILES: Cc1ccc(cc1)S(O)(=O)=O.NC(=O)c1cccc2cn(nc12)-c1ccc(cc1)[C@@H]1CCCNC1
• Target: PARP,Apoptosis
• Solubility: Ethanol:< 1 mg/mL (insoluble or slightly soluble);DMSO:91 mg/mL (184.74 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  PARP1:3.8 nM|PARP2:2.1 nM|PARP3:1300 nM|tankyrase 1:570 nM|PARP4:330 nM
• In Vivo:
  Niraparib tosylate strongly enhances the effect of radiation on a variety of human tumor xenografts, both p53 wild type and p53 mutant. Niraparib tosylate reduces PAR levels in tumors by 1 h after administration which persisted for up to 24 h. In vivo treatment with Niraparib tosylate and radiation prolonged survival (p<0.01) compared to single modalities. In vivo superiority of Niraparib tosylate 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.
• 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.
• 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)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

damage, DNA, breast, Apoptosis, anti-tumor, bioavailable, cancer, Inhibitor, inhibit, lung, poly ADP ribose polymerase, ovarian, Niraparib tosylate, Niraparib Tosylate, Niraparib, Niraparib (MK-4827) tosylate, Niraparib (MK-4827) Tosylate, orally, PARP, PARP1, PARP2, MK 4827, MK 4827 tosylate, MK 4827 Tosylate, MK4827, MK-4827, MK-4827 (tosylate), MK4827 Tosylate, MK-4827 Tosylate

Compound Identifiers

PubChem CID

78357761