Reagents and instruments for immunology, cell biology and molecular biology.

Niraparib [1038915-60-4]

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Cat# HY-10619-10mg

Size : 10mg

Brand : MedChemExpress

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Description

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^[1]^[2]^[3].

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)

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]
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]
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	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]
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]
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	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	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]
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	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]
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]
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]
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-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-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]
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.

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.

Purity & Documentation

Purity: 99.96%

Data Sheet (279 KB) SDS (393 KB)

COA (248 KB) HNMR (0 KB) LCMS (237 KB)

Handling Instructions (2659 KB)

References

[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]

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