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Niraparib

Catalog No. T3231 CAS 1038915-60-4

Synonyms: MK-4827

Niraparib (MK-4827) is a PARP inhibitor that selectively inhibits PARP1 and PARP2 (IC50=3.8/2.1 nM). Niraparib has antitumor activity, inhibits DNA damage repair, and induces apoptosis.

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Niraparib, CAS 1038915-60-4

Pack Size	Availability	Price/USD
5 mg	In stock	$ 55.00
10 mg	In stock	$ 80.00
25 mg	In stock	$ 119.00
50 mg	In stock	$ 147.00
100 mg	In stock	$ 228.00
200 mg	In stock	$ 338.00
500 mg	In stock	$ 573.00
1 g	In stock	$ 819.00
1 mL * 10 mM (in DMSO)	In stock	$ 61.00

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Purity: 99.91%

Purity: 99.85%

Purity: 99.48%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Niraparib (MK-4827) is a PARP inhibitor that selectively inhibits PARP1 and PARP2 (IC50=3.8/2.1 nM). Niraparib has antitumor activity, inhibits DNA damage repair, and induces apoptosis.
Targets&IC50	PARP2:2.1 nM, PARP1:3.8 nM
In vitro	METHODS: The PDAC cell lines MIA-PaCa-2, PANC-1, Capan-1 and the OvCa cell lines OVCAR8, PEO1 were treated with Niraparib (0.1-200 µM) for 48 h, and the cells were assayed for viability using the CellTiter-Glo Luminescent Cell Viability Assay. RESULTS: The IC50 of Niraparib on MIA-PaCa-2, PANC-1, Capan-1, OVCAR8, and PEO1 cells were 26 µm, 50 µm, 15 µM, 20 µM, and 28 µM, respectively.[1] [2]. METHODS: Ovarian cancer cells SKOV3 and UWB1.289 were treated with Niraparib (0.5-15 µM) for 48 h, and the expression levels of target proteins were detected by Western Blot. RESULTS: Niraparib upregulated the expression of PD-L1 in SKOV3 and UWB1.289 cells. [2]
In vivo	METHODS: To detect anti-tumor activity in vivo, Niraparib (25 mg/kg, administered orally four times per week) and PD-L1 (10 mg/kg, administered intraperitoneally twice per week) were administered to C57BL/6 mice bearing ovarian cancer tumor ID8 for eight weeks. RESULTS: Niraparib upregulated PD-L1 expression in ovarian tumors in vivo and synergized with PD-L1 blockade. [2] METHODS: To detect anti-tumor activity in vivo, Niraparib (50 mg/kg, 0.5% methylcellulose) was administered by gavage to C57BL/6 mice bearing intracranial human-derived TNBC cell lines SUM149, MDA-MB-231Br, or MDA-MB-436 once daily for two weeks. RESULTS: In the BRCA mutant MDA-MB-436 model, Niraparib increased median survival and decreased tumor load. However, it did not increase in the BRCA mutant SUM149 or BRCA wild-type MDA-MB-231Br models, despite high concentrations in intracranial tumors. [3]
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	Proliferation assays were conducted in 96-well black viewplates, and 300 cells/well (250 cell/well for BRCA-1 wt) in culture medium, 190 μL/well (DMEM containing 10% FCS, 0.1 mg/mL penicillin-streptomycin, and 2 mM L-glutamine), were plated and incubated for 4 h at 37℃ under 5% CO2 atmosphere. Inhibitors were then added with serial dilutions, 10 μL/well to obtain the desired final compound concentration in 0.5% DMSO. The cells were then incubated for 7 days at 37℃ in 5% CO2 after which time viability was assessed. Briefly, with CellTiter-Blue solution prediluted 1:10 in medium, 100 μL/well was added and the cells left for 45 min at 37℃ under 5% CO2 and then a further 15 min at room temperature in the dark. The number of living cells was determined by reading the plate at fluorimeter, excitation at 550 nm and emission at 590 nm. Cell growth was expressed as the percentage growth with respect to vehicle treated cells. The concentration required to inhibit cell growth by 50% (CC50) was determined.(Only for Reference)

Synonyms	MK-4827
Molecular Weight	320.39
Formula	C19H20N4O
CAS No.	1038915-60-4

Storage

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

Solubility Information

Ethanol: 60 mg/mL (187.3 mM)

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

DMSO: 60 mg/mL (187.3 mM)

References and Literature

1. Zhao Q, et al. Niraparib-induced STAT3 inhibition increases its antitumor effects. Front Oncol. 2022 Oct 17;12:966492. 2. Meng J, et al. Niraparib exhibits a synergistic anti-tumor effect with PD-L1 blockade by inducing an immune response in ovarian cancer. J Transl Med. 2021 Oct 7;19(1):415. 3. Sambade MJ, et al. Efficacy and pharmacodynamics of niraparib in BRCA-mutant and wild-type intracranial triple-negative breast cancer murine models. Neurooncol Adv. 2019 Jun 4;1(1):vdz005.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Approved Drug Library Anti-Cancer Active Compound Library Highly Selective Inhibitor Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Anti-Cancer Drug Library Inhibitor Library EMA Approved Drug Library Bioactive Compounds Library Max Anti-Breast Cancer Compound Library

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Keywords

Niraparib 1038915-60-4 Apoptosis Chromatin/Epigenetic DNA Damage/DNA Repair Others PARP breast DNA damage inhibit cancer anti-tumor poly ADP ribose polymerase bioavailable MK-4827 orally Inhibitor lung ovarian MK4827 MK 4827 inhibitor

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