Niraparib hydrochloride

SKU: orb1304290

Description

Niraparib hydrochloride

Research Area

Cell Biology, Epigenetics & Chromatin, Molecular Biology

Key Properties

• CAS Number: 1038915-64-8
• MW: 356.85
• Purity: 99.26%
• Formula: C₁₉H₂₁ClN₄O
• SMILES: C(N)(=O)C=1C=2C(=CN(N2)C3=CC=C(C=C3)[C@@H]4CCCNC4)C=CC1.Cl
• Target: PARP,Apoptosis
• Solubility: DMSO:50 mg/mL (140.11 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.6 mM);H2O:180 mg/mL (504.41 mM)

Bioactivity

• Target IC50:
  PARP3:1300 nM|PARP2:2.1 nM|PARP1:3.8nM|PARP4:330 nM|tankyrase 1:570 nM
• In Vivo:
  In cell assays, MK-4827 exhibits inhibitory effects on PARP activity (EC50: 4 nM) and suppresses the proliferation of cancer cells carrying BRCA-1/2 mutations (IC50: 10-100 nM). It effectively inhibits PARP-1/2 (IC50: 3.8/2.1 nM) but shows significantly lower selectivity (over 100-fold) against PARP-3, V-PARP, and tankyrase-1 (IC50: 1300/330/570 nM). In MDA-MB-436 human breast adenocarcinoma cells with a BRCA-1 mutation, MK-4827 has a CC50 of 18 nM; in CAPAN-1 human pancreatic cancer cells with a BRCA-2 deficiency, the CC50 is 90 nM. Normal human prostatic and breast epithelial cells exhibit resistance to MK-4827. This indicates that PARP inhibitors like MK-4827 have selective cytotoxicity in cancer cells with BRCA-1/2 mutations, minimizing the impact on surrounding tissue.
• In Vitro:
  MK-4827 significantly enhances the effectiveness of radiation on human tumor xenografts (whether p53 wild-type or p53 mutant), demonstrating good tolerability in vivo. When used alone, it also exhibits efficacy against BRCA-1 deficient xenograft models.

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, anti-tumor, Apoptosis, cancer, bioavailable, lung, PARP2, PARP3, PARP1, PARP, MK 4827, MK 4827 Hydrochloride, MK4827, MK-4827, MK-4827 (hydrochloride), MK4827 Hydrochloride, MK-4827 hydrochloride, MK-4827 Hydrochloride, Niraparib hydrochloride, Niraparib Hydrochloride, Niraparib, orally, ovarian, inhibit, Inhibitor, V-PARP, TANK-1, poly ADP ribose polymerase

Compound Identifiers

PubChem CID

44550597