Art. -Nr.: HY-10619

Niraparib

Name: Niraparib
Brand: MedChemExpress
SKU: HY-10619
Price: 70.00 USD
Availability: InStock
Rating: 5 (91 reviews)

(Synonyms: MK-4827)

91 Cited Publications

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Based on 91 publication(s) in Google Scholar

Niraparib (MK-4827) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC₅₀s of 3.8 and 2.1 nM, respectively. Niraparib leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.

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Reinheit : 99.96%
CAS. Nr.: 1038915-60-4
Formel: C₁₉H₂₀N₄O
Molecular Weight:320.39

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Niraparib Chemical Structure

CAS. Nr.: 1038915-60-4

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (91)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

PARP-2

2.1 nM (IC₅₀)

PARP-1

3.8 nM (IC₅₀)

V-PARP

330 nM (IC₅₀)

TANK-1

570 nM (IC₅₀)

PARP-3

1300 nM (IC₅₀)

Alle PARP Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	4 nM Compound: 8, MK-4827	Inhibition of PARP in human A2780 cells assessed as inhibition of hydrogen peroxide-induced PARylation by cell-based assay Inhibition of PARP in human A2780 cells assessed as inhibition of hydrogen peroxide-induced PARylation by cell-based assay	[PMID: 25761096]
A549	CC₅₀	11 nM Compound: 8, MK-4827	Cytotoxicity against human A549 cells transfected with BRCA2 shRNA assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay Cytotoxicity against human A549 cells transfected with BRCA2 shRNA assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay	[PMID: 25761096]
A549	CC₅₀	1760 nM Compound: 8, MK-4827	Cytotoxicity against wild type human A549 cells assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay Cytotoxicity against wild type human A549 cells assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay	[PMID: 25761096]
A549	IC₅₀	12.55 μM Compound: Niraparib	Antiproliferative activity against human A549 cells assessed as inhibition of cell viability incubated for 72 hrs by CCK8 assay Antiproliferative activity against human A549 cells assessed as inhibition of cell viability incubated for 72 hrs by CCK8 assay	[PMID: 37832229]
A549	IC₅₀	4.17 μM Compound: Niraparib	Antiproliferative activity against human A549 cells assessed as inhibition of cell viability incubated for 72 hrs in presence of IDM by CCK8 assay Antiproliferative activity against human A549 cells assessed as inhibition of cell viability incubated for 72 hrs in presence of IDM by CCK8 assay	[PMID: 37832229]
BT-20	CC₅₀	2200 nM Compound: 8, MK-4827	Cytotoxicity against human BT20 cells assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay Cytotoxicity against human BT20 cells assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay	[PMID: 25761096]
BT-549	IC₅₀	15.36 μM Compound: Nir	Synergistic cytotoxicity against human BT-549 cells incubated for 72 hrs in presence of Tazemetostat by MTT assay Synergistic cytotoxicity against human BT-549 cells incubated for 72 hrs in presence of Tazemetostat by MTT assay	[PMID: 38134746]
BT-549	IC₅₀	22.43 μM Compound: Nir	Cytotoxicity against human BT-549 cells incubated for 72 hrs by MTT assay Cytotoxicity against human BT-549 cells incubated for 72 hrs by MTT assay	[PMID: 38134746]
BT-549	IC₅₀	8.28 μM Compound: Nir	Synergistic cytotoxicity against human BT-549 cells incubated for 72 hrs in presence of GSK by MTT assay Synergistic cytotoxicity against human BT-549 cells incubated for 72 hrs in presence of GSK by MTT assay	[PMID: 38134746]
CAPAN-1	CC₅₀	90 nM Compound: 56, MK-4827	Antiproliferative activity against human Capan1 cells expressing BRCA2 6174delT mutation and loss of wild-type allele after 13 days by cell titer-blue assay Antiproliferative activity against human Capan1 cells expressing BRCA2 6174delT mutation and loss of wild-type allele after 13 days by cell titer-blue assay	[PMID: 19873981]
CAPAN-1	CC₅₀	90 nM Compound: 8, MK-4827	Cytotoxicity against BRCA2-deficient human Capan1 cells Cytotoxicity against BRCA2-deficient human Capan1 cells	[PMID: 25761096]
CAPAN-1	IC₅₀	3.5 nM Compound: 8, MK-4827	Inhibition of PARP in BRCA2-deficient human CAPAN-1 cells assessed as inhibition of hydrogen peroxide-induced PARylation by cell-based assay Inhibition of PARP in BRCA2-deficient human CAPAN-1 cells assessed as inhibition of hydrogen peroxide-induced PARylation by cell-based assay	[PMID: 25761096]
CAPAN-1	EC₅₀	650 nM Compound: 3; MK-4827	Cytotoxicity against BRCA2-deficient human Capan1 cells Cytotoxicity against BRCA2-deficient human Capan1 cells	[PMID: 26652717]
DLD-1	IC₅₀	0.149 μM Compound: 3	Antiproliferative activity against human DLD-1 deficient in BRCA-2 cells measured after 7 days Antiproliferative activity against human DLD-1 deficient in BRCA-2 cells measured after 7 days	[PMID: 34570508]
DoTc2-4510	CC₅₀	23 nM Compound: 8, MK-4827	Cytotoxicity against human DoTc2-4510 cells carrying BRCA2 mutant assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay Cytotoxicity against human DoTc2-4510 cells carrying BRCA2 mutant assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay	[PMID: 25761096]
HCT-116	IC₅₀	0.83 μM Compound: Niraparib	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell viability incubated for 72 hrs in presence of IDM by CCK8 assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell viability incubated for 72 hrs in presence of IDM by CCK8 assay	[PMID: 37832229]
HCT-116	IC₅₀	1.81 μM Compound: Niraparib	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell viability incubated for 72 hrs by CCK8 assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell viability incubated for 72 hrs by CCK8 assay	[PMID: 37832229]
HeLa	CC₅₀	33 nM Compound: 56, MK-4827	Antiproliferative activity against BRCA1 deficient human HeLa cells after 7 days by cell titer-blue assay Antiproliferative activity against BRCA1 deficient human HeLa cells after 7 days by cell titer-blue assay	[PMID: 19873981]
HeLa	CC₅₀	860 nM Compound: 56, MK-4827	Antiproliferative activity against human HeLa cells expressing wild type BRCA1 after 7 days by cell titer-blue assay Antiproliferative activity against human HeLa cells expressing wild type BRCA1 after 7 days by cell titer-blue assay	[PMID: 19873981]
HeLa	EC₅₀	4 nM Compound: 56, MK-4827	Inhibition of PARP in hydrogen peroxide-induced human HeLa cells assessed as inhibition DNA-damage-induced PARylation Inhibition of PARP in hydrogen peroxide-induced human HeLa cells assessed as inhibition DNA-damage-induced PARylation	[PMID: 19873981]
HeLa	CC₅₀	34 nM Compound: 8, MK-4827	Cytotoxicity against human HeLa cells transfected with BRCA1 shRNA assessed as reduction of cell viability after 5 to 7 days by CellTiter-Blue assay Cytotoxicity against human HeLa cells transfected with BRCA1 shRNA assessed as reduction of cell viability after 5 to 7 days by CellTiter-Blue assay	[PMID: 25761096]
HeLa	CC₅₀	852 nM Compound: 8, MK-4827	Cytotoxicity against wild type human HeLa cells assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay Cytotoxicity against wild type human HeLa cells assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay	[PMID: 25761096]
HeLa	EC₅₀	4 nM Compound: 8, MK-4827	Inhibition of PARP in human HeLa cells assessed as inhibition of hydrogen peroxide-induced PARylation by cell-based assay Inhibition of PARP in human HeLa cells assessed as inhibition of hydrogen peroxide-induced PARylation by cell-based assay	[PMID: 25761096]
HMEC	CC₅₀	>5000 nM Compound: 56, MK-4827	Antiproliferative activity against HMEC after 6 to 7 days by cell titer-blue assay Antiproliferative activity against HMEC after 6 to 7 days by cell titer-blue assay	[PMID: 19873981]
HT-22	IC₅₀	35 μM Compound: 50	Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay	[PMID: 36876904]
Ishikawa	IC₅₀	0.024 μM Compound: Niraparib	Antiproliferative activity against human Ishikawa cells assessed as reduction in cell viability Antiproliferative activity against human Ishikawa cells assessed as reduction in cell viability	[PMID: 38911148]
Jurkat	EC₅₀	0.2 μM Compound: MK-4827	Inhibition of PARP1 in human Jurkat cells assessed as reduction of cell viability after 96 hrs by MTS assay in presence of 100 uM of temozolomide Inhibition of PARP1 in human Jurkat cells assessed as reduction of cell viability after 96 hrs by MTS assay in presence of 100 uM of temozolomide	[PMID: 23850199]
Jurkat	EC₅₀	31 μM Compound: MK-4827	Inhibition of PARP1 in human Jurkat cells assessed as reduction of cell viability after 96 hrs by MTS assay Inhibition of PARP1 in human Jurkat cells assessed as reduction of cell viability after 96 hrs by MTS assay	[PMID: 23850199]
MCF-10A	IC₅₀	>40 μM Compound: Nir	Cytotoxicity against human MCF-10A cells incubated for 72 hrs by MTT assay Cytotoxicity against human MCF-10A cells incubated for 72 hrs by MTT assay	[PMID: 38134746]
MCF-10A	IC₅₀	>40 μM Compound: Nir	Synergistic cytotoxicity against human MCF-10A cells incubated for 72 hrs in presence of GSK by MTT assay Synergistic cytotoxicity against human MCF-10A cells incubated for 72 hrs in presence of GSK by MTT assay	[PMID: 38134746]
MCF-10A	IC₅₀	>40 μM Compound: Nir	Synergistic cytotoxicity against human MCF-10A cells incubated for 72 hrs in presence of Tazemetostat by MTT assay Synergistic cytotoxicity against human MCF-10A cells incubated for 72 hrs in presence of Tazemetostat by MTT assay	[PMID: 38134746]
MCF7	IC₅₀	1.41 μM Compound: Niraparib	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability incubated for 72 hrs in presence of IDM by CCK8 assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability incubated for 72 hrs in presence of IDM by CCK8 assay	[PMID: 37832229]
MCF7	IC₅₀	11.77 μM Compound: Niraparib	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability incubated for 72 hrs by CCK8 assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability incubated for 72 hrs by CCK8 assay	[PMID: 37832229]
MDA-MB-231	IC₅₀	33.22 μM Compound: Niraparib	Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 24 hrs by CCK-8 assay Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 24 hrs by CCK-8 assay	[PMID: 36512711]
MDA-MB-231	IC₅₀	60.91 μM Compound: Niraparib	Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 24 hrs in presence of nutlin-3 by CCK-8 assay Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 24 hrs in presence of nutlin-3 by CCK-8 assay	[PMID: 36512711]
MDA-MB-231	IC₅₀	11.07 μM Compound: Nir	Synergistic cytotoxicity against human MDA-MB-231 cells incubated for 72 hrs in presence of Tazemetostat by MTT assay Synergistic cytotoxicity against human MDA-MB-231 cells incubated for 72 hrs in presence of Tazemetostat by MTT assay	[PMID: 38134746]
MDA-MB-231	IC₅₀	13.35 μM Compound: Nir	Cytotoxicity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay	[PMID: 38134746]
MDA-MB-231	IC₅₀	6.32 μM Compound: Nir	Synergistic cytotoxicity against human MDA-MB-231 cells incubated for 72 hrs in presence of GSK by MTT assay Synergistic cytotoxicity against human MDA-MB-231 cells incubated for 72 hrs in presence of GSK by MTT assay	[PMID: 38134746]
MDA-MB-436	CC₅₀	18 nM Compound: 56, MK-4827	Antiproliferative activity against human MDA-MB-436 cells expressing BRCA1 5396 + 1G>A mutant after 6 days by cell titer-blue assay Antiproliferative activity against human MDA-MB-436 cells expressing BRCA1 5396 + 1G>A mutant after 6 days by cell titer-blue assay	[PMID: 19873981]
MDA-MB-436	CC₅₀	18 nM Compound: 8, MK-4827	Cytotoxicity against human MDA-MB-436 cells carrying BRCA1 mutant assessed as inhibition of cell proliferation Cytotoxicity against human MDA-MB-436 cells carrying BRCA1 mutant assessed as inhibition of cell proliferation	[PMID: 25761096]
MDA-MB-468	IC₅₀	7.6 μM Compound: Niraparib	Cytotoxicity against human MDA-MB-468 cells measured after 72 hrs by Celltiter-Glo assay Cytotoxicity against human MDA-MB-468 cells measured after 72 hrs by Celltiter-Glo assay	[PMID: 33200929]
MV4-11	IC₅₀	1.69 μM Compound: Niraparib	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell viability incubated for 72 hrs in presence of IDM by CCK8 assay Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell viability incubated for 72 hrs in presence of IDM by CCK8 assay	[PMID: 37832229]
MV4-11	IC₅₀	3.82 μM Compound: Niraparib	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell viability incubated for 72 hrs by CCK8 assay Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell viability incubated for 72 hrs by CCK8 assay	[PMID: 37832229]
NCM460	IC₅₀	21.13 μM Compound: Niraparib	Antiproliferative activity against human NCM460 cells assessed as inhibition of cell viability incubated for 72 hrs in presence of IDM by CCK8 assay Antiproliferative activity against human NCM460 cells assessed as inhibition of cell viability incubated for 72 hrs in presence of IDM by CCK8 assay	[PMID: 37832229]
NCM460	IC₅₀	53.71 μM Compound: Niraparib	Antiproliferative activity against human NCM460 cells assessed as inhibition of cell viability incubated for 72 hrs by CCK8 assay Antiproliferative activity against human NCM460 cells assessed as inhibition of cell viability incubated for 72 hrs by CCK8 assay	[PMID: 37832229]
PrEC	CC₅₀	>5000 nM Compound: 56, MK-4827	Antiproliferative activity against human PrEC cells after 6 to 7 days by cell titer-blue assay Antiproliferative activity against human PrEC cells after 6 to 7 days by cell titer-blue assay	[PMID: 19873981]
SUM149PT	CC₅₀	24 nM Compound: 8, MK-4827	Cytotoxicity against human SUM149PT cells carrying BRCA1 mutant assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay Cytotoxicity against human SUM149PT cells carrying BRCA1 mutant assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay	[PMID: 25761096]

In Vitro

Niraparib (MK-4827) inhibits PARP activity with EC₅₀=4 nM and EC₉₀=45 nM in a whole cell assay. MK-4827 inhibits proliferation of cancer cells with mutant BRCA-1 and BRCA-2 with CC₅₀ in the 10-100 nM range. MK-4827 displays excellent PARP 1 and 2 inhibition with IC₅₀=3.8 and 2.1 nM, respectively, and in a whole cell assay^[1]. To validate that Niraparib (MK-4827) inhibits PARP in these cell lines, A549 and H1299 cells are treated with 1 μM MK-4827 for various times and measured PARP enzymatic activity using a chemiluminescent assay. The results show that Niraparib (MK-4827) inhibits PARP within 15 minutes of treatment reaching about 85% inhibition in the A549 cells at 1 h and about 55% inhibition at 1 h for the H1299 cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Niraparib (MK-4827) is well tolerated and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer. Niraparib (MK-4827) is well tolerated in vivo and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer. Niraparib (MK-4827) is characterized by acceptable pharmacokinetics in rats with plasma clearance of 28 (mL/min)/kg, very high volume of distribution (Vd_ss=6.9 L/kg), long terminal half-life (t_1/2=3.4 h), and excellent bioavailability, F=65%^[1]. Niraparib (MK-4827) enhances radiation response of p53 mutant Calu-6 tumor in both cases, with the single daily dose of 50 mg/kg being more effective than 25 mg/kg given twice daily^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Female nude mice (Ncr Nu/Nu) with solitary tumor xenografts^[3]
Dosage:

25 mg/kg or 50 mg/kg
Administration:

Gavage, 25 mg/kg twice a day with 6 h between doses or 50 mg/kg once daily for 21 consecutive days
Result:

Enhanced radiation response.

Related Protocols :

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991			2011-05	PHASE1

Chemical Information

CAS. Nr. 1038915-60-4
Appearance Solid
Molecular Weight 320.39
Formel C₁₉H₂₀N₄O
Color White to light yellow
SMILES

NC(C1=CC=CC2=CN(C3=CC=C([C@H]4CNCCC4)C=C3)N=C21)=O
Synonyms

MK-4827
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (91)

All In Vivo Efficacy StudyCell Proliferation/Viability AssayIn Vivo ImagingWB

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Journal Impact Factor

Cancer Cell

Elevated CXorf67 Expression in PFA Ependymomas Suppresses DNA Repair and Sensitizes to PARP Inhibitors. [Abstract]

2020 Dec 14;38(6):844-856.e7. PMID: 33186520

Niraparib purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2020 Dec 14;38(6):844-856.e7. [Abstract]

Re-expression of CXorf67 in C67-KO Daoy cells increases sensitivity to PARPi and IR combination. Cell viability was assessed by the CellTiter-Glo assay. Data are presented as mean ± SD. Western blot showing expression levels of CXorf67.

Niraparib purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2020 Dec 14;38(6):844-856.e7. [Abstract]

The mice were randomized into four treatment groups (n = 5 per group) after 7 days from the implantation: vehicle (0.5% methylcellulose in PBS), niraparib (50 mg/kg in 0.5% methylcellulose, orally once daily for 5 days per week), 8 Gy fractionated radiotherapy (2 Gy daily for 4 days), and niraparib combined with 8 Gy fractionated radiotherapy. The bioluminescence imaging levels were acquired every 10 days using an IVIS SpectrumCT imaging system.
Cancer Discov

Secondary Somatic Mutations Restoring RAD51C and RAD51D Associated with Acquired Resistance to the PARP Inhibitor Rucaparib in High-Grade Ovarian Carcinoma. [Abstract]

2017 Sep;7(9):984-998. PMID: 28588062
Nat Biomed Eng

Functional annotation of variants of the BRCA2 gene via locally haploid human pluripotent stem cells. [Abstract]

2024 Feb;8(2):165-176. PMID: 37488236
Cancer Res

Oncohistone Mutations Occur at Functional Sites of Regulatory ADP-Ribosylation. [Abstract]

2022 Jul 5;82(13):2361-2377. PMID: 35472077

Niraparib purchased from MedChemExpress. Usage Cited in: Cancer Res. 2022 Jul 5;82(13):2361-2377. [Abstract]

Growth of xenograft tumors formed from MDA-MB-231 cells engineered for ectopic expression of FLAG-tagged WT or D51A mutant H2B in NOD scid gamma (NSG) mice, treated with vehicle or 25 mg/kg Niraparib intraperitoneally (i.p.) 5 days a week over 4 weeks.
Drug Resist Updat

ZBP1 antagonizes MRE11-mediated DNA end resection and confers synthetic lethality to PARP inhibition in ovarian cancer. [Abstract]

2026 Jan:84:101319. PMID: 41192279
Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Nat Commun

DNA mechanical flexibility controls DNA potential to activate cGAS-mediated immune surveillance. [Abstract]

2022 Nov 19;13(1):7107. PMID: 36402783
Theranostics

Molecular signatures of BRCAness analysis identifies PARP inhibitor Niraparib as a novel targeted therapeutic strategy for soft tissue Sarcomas. [Abstract]

2020 Jul 25;10(21):9477-9494. PMID: 32863940
Acta Pharm Sin B

The cytoskeletal protein smoothelin maintains homologous recombination repair by stabilizing RAD51 in an HUWE1-dependent manner in colorectal cancer. [Abstract]

2025 Dec;15(12):6444-6460. PMID: 41477349
J Clin Invest

Targeting Wnt/β-Catenin and circadian regulator restores PRC2/EZH2 controlled chromatin bivalency and suppresses cell state diversity. [Abstract]

2026 Mar 17:e200260. PMID: 41842971
J Exp Clin Cancer Res

PARP-1 as a novel target in endocrine-resistant breast cancer. [Abstract]

2025 Jun 16;44(1):175. PMID: 40518539
J Clin Invest

PARP inhibition enhances tumor cell-intrinsic immunity in ERCC1-deficient non-small cell lung cancer. [Abstract]

2019 Mar 1;129(3):1211-1228. PMID: 30589644
Adv Sci (Weinh)

2026 Jul 13:e76141. PMID: 42439473
Adv Sci (Weinh)

Disruption of ARID1B Recruitment to the Nuclear Pore Complex as a New Anticancer Therapeutic Strategy. [Abstract]

2025 Jul 16:e15585. PMID: 40671262
Adv Sci (Weinh)

Vanguard is a Glucose Deprivation-Responsive Long Non-Coding RNA Essential for Chromatin Remodeling-Reliant DNA Repair. [Abstract]

2022 Oct;9(30):e2201210. PMID: 36047643
Sci Adv

Acute BRCAness induction and AR pathway blockage through CDK12/7/9 degradation enhances PARP inhibitor sensitivity in prostate cancer. [Abstract]

Sci Adv. 2025 Apr 25;11(17):eadu0847. PMID: 40267193
Mol Biomed

2026 Aug 26;7(1):151. PMID: 42645640
Cell Death Dis

Targeting EZH2-driven cholesterol metabolic vulnerability through Napabucasin suppresses ovarian cancer metastasis. [Abstract]

2026 Jun 27;17(1):603. PMID: 42373608
Cell Death Dis

Cdk1-phosphorylated Nur77 accumulates at the centrosome during mitosis to regulate the Cep192-PLK1 signaling axis. [Abstract]

2026 Jun 3. PMID: 42236697
Cell Death Dis

Pan-cancer analysis reveals synergistic effects of CDK4/6i and PARPi combination treatment in RB-proficient and RB-deficient breast cancer cells. [Abstract]

2020 Apr 6;11(4):219. PMID: 32249776
Cancer Lett

Inhibiting Src-mediated PARP1 tyrosine phosphorylation confers synthetic lethality to PARP1 inhibition in HCC. [Abstract]

2022 Feb 1:526:180-192. PMID: 34762994
Int J Biol Sci

Quantitative determination of niraparib and olaparib tumor distribution by mass spectrometry imaging. [Abstract]

2020 Feb 21;16(8):1363-1375. PMID: 32210725
Phytomedicine

2026 Jun 11.
EBioMedicine

Molecular correlates of sensitivity to PARP inhibition beyond homologous recombination deficiency in pre-clinical models of colorectal cancer point to wild-type TP53 activity. [Abstract]

2020 Sep:59:102923. PMID: 32799124
Mater Today Bio

Low dose novel PARP-PI3K inhibition via nanoformulation improves colorectal cancer immunoradiotherapy. [Abstract]

2020 Oct 22:8:100082. PMID: 33294836
Clin Cancer Res

The pharmacological profile of ART6043, a first-in-class clinical DNA polymerase theta polymerase domain inhibitor potentiating PARP inhibitor efficacy. [Abstract]

2026 Jul 13. PMID: 42440368
Clin Cancer Res

Drug-Driven Synthetic Lethality: Bypassing Tumor Cell Genetics with a Combination of AsiDNA and PARP Inhibitors. [Abstract]

2017 Feb 15;23(4):1001-1011. PMID: 27559053
NPJ Precis Oncol

Ex vivo 3D micro-tumour testing platform for predicting clinical response to platinum-based therapy in patients with high-grade serous ovarian cancer. [Abstract]

2025 Aug 30;9(1):306. PMID: 40885787
NPJ Precis Oncol

PARP inhibitors promote stromal fibroblast activation by enhancing CCL5 autocrine signaling in ovarian cancer. [Abstract]

2021 Jun 9;5(1):49. PMID: 34108603
J Transl Med

Ivabradine induces RAD51 degradation, potentiating PARP inhibitor efficacy in non-germline BRCA pathogenic variant triple-negative breast cancer. [Abstract]

2025 Aug 5;23(1):860. PMID: 40764992
Oncogene

A genome-wide CRISPR-Cas9 knockout screen identifies novel PARP inhibitor resistance genes in prostate cancer. [Abstract]

2022 Sep;41(37):4271-4281. PMID: 35933519
Int J Biol Macromol

Injectable bio-multifunctional hyaluronic acid-based hydrogels loaded with poly ADP-ribose polymerase inhibitors for ovarian cancer therapy. [Abstract]

2024 Jun;270(Pt 1):132275. PMID: 38734345
Cell Rep

Targeting ZDHHC12-mediated PARP1 palmitoylation potentiates PARP inhibitor cytotoxicity. [Abstract]

2026 Jan 24;45(2):116910. PMID: 41581148
J Med Chem

Discovery of the Potent and Selective ATR Inhibitor Camonsertib (RP-3500). [Abstract]

2024 Feb 22;67(4):2349-2368. PMID: 38299539
J Med Chem

Comparative Efficacy and Selectivity of Pharmacological Inhibitors of DYRK and CLK Protein Kinases. [Abstract]

2023 Mar 23;66(6):4106-4130. PMID: 36876904
Mol Cancer Ther

Bepotastine sensitizes ovarian cancer to PARP inhibitors through suppressing NF-κB-triggered SASP in cancer-associated fibroblasts. [Abstract]

2023 Apr 3;22(4):447-458. PMID: 36780236
Mol Cancer Ther

RP-3500: A Novel, Potent, and Selective ATR Inhibitor that is Effective in Preclinical Models as a Monotherapy and in Combination with PARP Inhibitors. [Abstract]

2022 Feb;21(2):245-256. PMID: 34911817
JCI Insight

Mutant RB1 enhances therapeutic efficacy of PARPis in lung adenocarcinoma by triggering the cGAS/STING pathway. [Abstract]

2023 Nov 8;8(21):e165268. PMID: 37937640
Biochem Pharmacol

Discovery of Bi-magnolignan as a novel BRD4 inhibitor inducing apoptosis and DNA damage for cancer therapy. [Abstract]

2025 May:235:116843. PMID: 40024351
Pharmaceuticals (Basel)

2026 Sep 28;19(10):1538.
Int Immunopharmacol

Fluzoparib disrupts Golgi apparatus to inhibit O-GlcNAcylation and nuclear translocation of β-catenin to attenuate ovarian cancer invasion and metastasis. [Abstract]

2025 Sep 23:162:115158. PMID: 40602265
Int J Mol Sci

Trabectedin Induces Synthetic Lethality via the p53-Dependent Apoptotic Pathway in Ovarian Cancer Cells Without BRCA Mutations When Used in Combination with Niraparib. [Abstract]

2025 Mar 24;26(7):2921. PMID: 40243501
J Mol Med (Berl)

Combination of PARP inhibitor and temozolomide to suppress chordoma progression. [Abstract]

2019 Aug;97(8):1183-1193. PMID: 31201471
Am J Pathol

Low-Dose Radiotherapy Attenuates Pulmonary Granulomas Involving Ataxia-Telangiectasia Mutated-Dependent Modulation of the Interferon-β Response: A Host-Directed Therapeutic Strategy for Tuberculosis. [Abstract]

2026 Jun 10:S0002-9440(26)00163-X. PMID: 42270072
Int J Cancer

Combined inhibition of RAD51 and CHK1 causes synergistic toxicity in cisplatin resistant cancer cells by triggering replication fork collapse. [Abstract]

2025 Jan 15;156(2):389-402. PMID: 39239809
Am J Pathol

Medulloblastomas Initiated by Homologous Recombination Defects in Mice. [Abstract]

2024 Nov;194(11):2007-2022. PMID: 39168365
Mol Pharm

P-Glycoprotein (ABCB1/MDR1) Controls Brain Penetration and Intestinal Disposition of the PARP1/2 Inhibitor Niraparib. [Abstract]

2021 Dec 6;18(12):4371-4384. PMID: 34730366
Sci Rep

Integrated genomics point to immune vulnerabilities in pleural mesothelioma. [Abstract]

2021 Sep 27;11(1):19138. PMID: 34580349
Cancers (Basel)

Dual Targeting of CX3CR1 and PARP in Models of High-Grade Serous Ovarian Carcinoma. [Abstract]

2024 Nov 5;16(22):3728. PMID: 39594684
Cancers (Basel)

[89Zr]-Atezolizumab-PET Imaging Reveals Longitudinal Alterations in PDL1 during Therapy in TNBC Preclinical Models. [Abstract]

2023 May 11;15(10):2708. PMID: 37345044
Appl Microbiol Biotechnol

Autophagy suppression enhances DNA damage and cell death upon treatment with PARP inhibitor Niraparib in laryngeal squamous cell carcinoma. [Abstract]

2019 Dec;103(23-24):9557-9568. PMID: 31686145

Niraparib purchased from MedChemExpress. Usage Cited in: Appl Microbiol Biotechnol. 2019 Dec;103(23-24):9557-9568. [Abstract]

Cyclin D is evaluated via western blot analysis in different cell lines with the treatment of Niraparib in different concentrations and times.

Niraparib purchased from MedChemExpress. Usage Cited in: Appl Microbiol Biotechnol. 2019 Dec;103(23-24):9557-9568. [Abstract]

CDK4 is evaluated via western blot analysis in different cell lines with the treatment of Niraparib in different concentrations and times.
Neurooncol Adv

Ion channel modulator DPI-201-106 significantly enhances antitumor activity of DNA damage response inhibitors in glioblastoma. [Abstract]

2024 Nov 19;6(1):vdae187. PMID: 39659830
Bioengineering (Basel)

Precision Oncology for High-Grade Gliomas: A Tumor Organoid Model for Adjuvant Treatment Selection. [Abstract]

2025 Oct 19;12(10):1121. PMID: 41155119
BMC Cancer

Regorafenib induces DNA damage and enhances PARP inhibitor efficacy in pancreatic ductal carcinoma. [Abstract]

2024 Dec 20;24(1):1562. PMID: 39707244
BMC Cancer

PARP inhibitors chemopotentiate and synergize with cisplatin to inhibit bladder cancer cell survival and tumor growth. [Abstract]

2022 Mar 23;22(1):312. PMID: 35321693
Cancer Res Commun

Nucleolar Localization of the RNA Helicase DDX21 Predicts Survival Outcomes in Gynecological Cancers. [Abstract]

2024 Jun 13;4(6):1495-1504. PMID: 38767454
Carcinogenesis

Targeting PARP and autophagy evoked synergistic lethality in hepatocellular carcinoma. [Abstract]

2020 May 14;41(3):345-357. PMID: 31175354
Front Oncol

The Emerging Role of Poly (ADP-Ribose) Polymerase Inhibitors as Effective Therapeutic Agents in Renal Cell Carcinoma. [Abstract]

2021 Jul 9:11:681441. PMID: 34307148
DNA Repair

Loss of the p12 subunit of DNA polymerase delta leads to a defect in HR and sensitization to PARP inhibitors. [Abstract]

2019 Jan:73:64-70. PMID: 30470508
Am J Cancer Res

Novel dual action PARP and microtubule polymerization inhibitor AMXI-5001 powerfully inhibits growth of esophageal carcinoma both alone and in combination with radiotherapy. [Abstract]

2024 Jan 15;14(1):378-389. PMID: 38323288
Life Sci Alliance

Suppression of isoprenylcysteine carboxylmethyltransferase compromises DNA damage repair. [Abstract]

2021 Oct 5;4(12):e202101144. PMID: 34610973
Nucl Med Biol

Iodinated benzimidazole PARP radiotracer for evaluating PARP1/2 expression in vitro and in vivo. [Abstract]

2016 Dec;43(12):752-758. PMID: 27689533
PeerJ

Niraparib restrains prostate cancer cell proliferation and metastasis and tumor growth in mice by regulating the lncRNA MEG3/miR-181-5p/GATA6 pathway. [Abstract]

2023 Nov 29:11:e16314. PMID: 38047026
Urol Oncol

PTTG1-mediated reprogramming of asparagine metabolism enhances DNA damage repair and leads to compromised antitumor immunity in prostate cancer. [Abstract]

2025 Sep 30:S1078-1439(25)00359-X. PMID: 41033896
Cancer Chemother Pharmacol

Synthetic lethality in malignant pleural mesothelioma with PARP1 inhibition. [Abstract]

2017 Oct;80(4):861-867. PMID: 28756516
Res Connect

2026 May 28.
bioRxiv

2026 Mar 13.
Biomed Pharmacother

Synergistic suppression of cholangiocarcinoma cells via DNA damage response and cell cycle arrest by dual targeting PARP and ATM in DNA damage repair pathway. [Abstract]

2025 Aug:189:118273. PMID: 40527032
bioRxiv

2025 July 08.
bioRxiv

2025 April 26.
bioRxiv

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Acute BRCAness Induction and AR Signaling Blockage through CDK12/7/9 Degradation Enhances PARP Inhibitor Sensitivity in Prostate Cancer. [Abstract]

2024 Jul 10:2024.07.09.602803. PMID: 39026842
J Oncol

The PARP1 Inhibitor Niraparib Represses DNA Damage Repair and Synergizes with Temozolomide for Antimyeloma Effects. [Abstract]

2022 Apr 5;2022:2800488. PMID: 35422863
Elife

Development and characterization of new tools for detecting poly(ADP-ribose) in vitro and in vivo. [Abstract]

2022 Apr 27;11:e72464. PMID: 35476036
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2022 Feb.
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Exosome component 1 cleaves single-stranded DNA and sensitizes human kidney renal clear cell carcinoma cells to poly(ADP-ribose) polymerase inhibitor. [Abstract]

2021 Jun 23:10:e69454. PMID: 34159897
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Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 31.25 mg/mL (97.54 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.1212 mL

15.6060 mL

31.2120 mL

5 mM

0.6242 mL

3.1212 mL

6.2424 mL

10 mM

0.3121 mL

1.5606 mL

3.1212 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (6.49 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (6.49 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (6.49 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 2.5 mg/mL (7.80 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Jones P, et al. Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors. J Med Chem. 2009 Nov 26;52(22):7170-85. [Content Brief]

[2]. Bridges KA, et al. Niraparib (MK-4827), a novel poly(ADP-Ribose) polymerase inhibitor, radiosensitizes human lung and breast cancer cells. Oncotarget. 2014 Jul 15;5(13):5076-86. [Content Brief]

[3]. Wang L, et al. MK-4827, a PARP-1/-2 inhibitor, strongly enhances response of human lung and breast cancer xenografts to radiation. Invest New Drugs. 2012 Dec;30(6):2113-20. [Content Brief]

[4]. Mirza MR, et al. Niraparib Maintenance Therapy in Platinum-Sensitive, Recurrent Ovarian Cancer. N Engl J Med. 2016 Dec 1;375(22):2154-2164. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.1212 mL	15.6060 mL	31.2120 mL	78.0299 mL
	5 mM	0.6242 mL	3.1212 mL	6.2424 mL	15.6060 mL
	10 mM	0.3121 mL	1.5606 mL	3.1212 mL	7.8030 mL
	15 mM	0.2081 mL	1.0404 mL	2.0808 mL	5.2020 mL
	20 mM	0.1561 mL	0.7803 mL	1.5606 mL	3.9015 mL
	25 mM	0.1248 mL	0.6242 mL	1.2485 mL	3.1212 mL
	30 mM	0.1040 mL	0.5202 mL	1.0404 mL	2.6010 mL
	40 mM	0.0780 mL	0.3901 mL	0.7803 mL	1.9507 mL
	50 mM	0.0624 mL	0.3121 mL	0.6242 mL	1.5606 mL
	60 mM	0.0520 mL	0.2601 mL	0.5202 mL	1.3005 mL
	80 mM	0.0390 mL	0.1951 mL	0.3901 mL	0.9754 mL

Bioz

Keywords

Niraparib

91 Cited Publications

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Niraparib

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