Niraparib (MK-4827)

Catalog No.S2741

Niraparib (MK-4827) Chemical Structure

Molecular Weight(MW): 320.39

Niraparib (MK-4827) is a selective inhibitor of PARP1/2 with IC50 of 3.8 nM/2.1 nM, with great activity in cancer cells with mutant BRCA-1 and BRCA-2. It is >330-fold selective against PARP3, V-PARP and Tank1. Phase 3.

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1 Customer Review

  • PARP1 silencing rescues PARP1/2 inhibitor sensitivity in the ERCC1-deficient population. Effect of PARP1 knockdown by siRNA on sensitivity of ERCC1-isogenic cell lines to niraparib. Cells were reverse-transfected with PARP1 siRNA and drug was added 48 h after transfection. Cells were exposed to the drug for 5 days. Error bars represent the s.d. from the mean of three independent experiments.

    Oncogene 2013 32(47):5377-87. Niraparib (MK-4827) purchased from Selleck.

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Biological Activity

Description Niraparib (MK-4827) is a selective inhibitor of PARP1/2 with IC50 of 3.8 nM/2.1 nM, with great activity in cancer cells with mutant BRCA-1 and BRCA-2. It is >330-fold selective against PARP3, V-PARP and Tank1. Phase 3.
PARP2 [1]
(Cell-free assay)
PARP1 [1]
(Cell-free assay)
2.1 nM 3.8 nM
In vitro

In a whole cell assay, MK-4827 inhibited PARP activity with EC50 = 4 nM and inhibited proliferation of cancer cells with mutant BRCA-1 and BRCA-2 with CC50 in the 10-100 nM range. It was demonstrated to be a potent and selective PARP-1 and PARP-2 inhibitor with IC50=3.8 and 2.1 nM, respectively. Furthermore, it displayed at least a 100-fold selectivity over PARP-3, V-PARP, and tankyrase-1, with IC50 = 1300, 330, and 570 nM, respectively. As well as inhibiting the growth of HeLa cell lacking BRCA-1 because of silencing by RNA interference, MK-4827 is able to inhibit the proliferation of cancer cell lines carrying natural BRCA-1 or BRCA-2 mutations. In MDA-MB-436 human mammary gland adenocarcinoma cells carrying BRCA-1 mutations, MK-4827 displayed CC50 = 18 nM, while in CAPAN-1 human pancreatic adenocarcinoma cells, which are BRCA-2 mutant, MK-4827 displayed CC50 = 90 nM. In contrast, normal human prostate and mammary epithelial cells are resistant to MK-4827, displaying antiproliferative effects in the micromolar range, thereby demonstrating the very high selective cytotoxicity from these PARP inhibitors in BRCA-1 and -2 mutant cancer cells compared to surrounding tissue[2].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HeLa cells MUfGeY5kfGmxbjDhd5NigQ>? M2TDTGlvcGmkaYTpc44hd2ZiUFHSVEBqdiCqeXTyc4dmdiCyZYLvfIll\S2rbnT1Z4VlKGi3bXHuJGhmVGFiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDEUmEu\GGvYXflMYlv\HWlZXSgVGFTgWyjdHnvckwhTUN3ME2wMlAxPCEQvF2= MnXjNVk5PzN7OEG=
A549 cells MmnJR5l1d3SxeHnjbZR6KGG|c3H5 NIrTe2o2NTdiZHH5dy=> NYrVdIpyS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTV2OTDj[YxteyC2cnHud4Zm[3SnZDD3bZRpKEKUQ1GyJJNpWk6DIHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiY3XscEBxem:uaX\ldoF1cW:wIHHmeIVzKDVidH:gO{Bl[Xm|IHL5JGNmdGyWaYTldk1DdHWnIHHzd4F6NCCFQ{WwQVAvODFzIN88US=> NFzpWIYzPTd4MUC5Oi=>
MDA-MB-436 cells MXLQdo9tcW[ncnH0bY9vKGG|c3H5 NV;hUJhiPiCmYYnz MWPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2GQT3NRk01OzZiY3XscJMh\XiycnXzd4lv\yCEUlPBNUA2Ozl4IDugNWc,SSCvdYThcpQh[W[2ZYKgOkBl[Xm|IHL5JINmdGxidHn0[ZIu[my3ZTDhd5NigSxiQ1O1NF0yQCCwTR?= NHm2b2wyQTh5M{m4NS=>
SUM1315MO2 cells Mn;MR5l1d3SxeHnjbZR6KGG|c3H5 MW[xNkBl[Xm| NEP5UWhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUXU1zM{G1UW8zKGOnbHzzJINienK7aX7nJGJTS0FzIH31eIFvfCCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdiCjZoTldkAyOiCmYYnzJIJ6KEOnbHzUbZRmei2EbIXlJIF{e2G7LDDDR|UxRTBwMEKg{txO NVjVTJZHOjV5NkGwPVY>
DoTc2-4510 cells M3HNVmN6fG:2b4jpZ4l1gSCjc4PhfS=> Mn;qOU04KGSjeYO= Mm\DR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gSI9V[zJvNEWxNEBk\WyuczDjZZJzgWmwZzDCVmNCOiCvdYThcpQh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBk\WyuIIDyc4xq\mW{YYTpc44h[W[2ZYKgOUB1dyB5IHThfZMh[nliQ3XscHRqfGW{LVLseYUh[XO|YYmsJGNEPTB;MD6wNlMh|ryP M1fEVFI2PzZzMEm2
SUM149PT cells M3n2ZmN6fG:2b4jpZ4l1gSCjc4PhfS=> M4judlUuPyCmYYnz MU\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTWW0yPDmSVDDj[YxteyClYYLyfYlv\yCEUlPBNUBufXSjboSgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36gZYZ1\XJiNTD0c{A4KGSjeYOgZpkhS2WubGTpeIVzNUKudXWgZZN{[XluIFPDOVA:OC5yMkSg{txO NInkWIYzPTd4MUC5Oi=>
UWB1.289 cells MYfDfZRwfG:6aXPpeJkh[XO|YYm= MXO1MVch\GG7cx?= Mo\SR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gWXdDOS5{OEmgZ4VtdHNiY3HydplqdmdiQmLDRVEhdXW2YX70JIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gZ4VtdCCycn;sbYZmemG2aX;uJIFnfGW{IEWgeI8hPyCmYYnzJIJ6KEOnbHzUbZRmei2EbIXlJIF{e2G7LDDDR|UxRTBwMEW2JO69VQ>? NHzCVI8zPTd4MUC5Oi=>
Capan1 cells MYnDfZRwfG:6aXPpeJkh[XO|YYm= M3jqTWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KEKUQ1GyMYRm\mmlaXXueEBpfW2jbjDDZZBidjFiY3XscJMtKEOFNUC9NE4xQSEQvF2= M16xVFI2PzZzMEm2
Jurkat cells M1yxTGZ2dmO2aX;uJIF{e2G7 Ml60TY5pcWKrdHnvckBw\iCSQWLQNUBqdiCqdX3hckBLfXKtYYSgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJI9nKGOnbHygeoli[mmuaYT5JIFnfGW{IEm2JIhzeyCkeTDNWHMh[XO|YYmgbY4heHKnc3XuZ4Uhd2ZiMUCwJJVOKG:oIITlcY97d2yxbXnk[UwhTUN3ME2wMlIh|ryP M1\5[lI{QDVyMUm5
BT20 cells NXzDeo86S3m2b4TvfIlkcXS7IHHzd4F6 NEPjRY02NTdiZHH5dy=> MkHZR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRnQzOCClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJINmdGxicILvcIln\XKjdHnvckBi\nSncjC1JJRwKDdiZHH5d{BjgSCFZXzsWIl1\XJvQnz1[UBie3OjeTygR2M2OD1{LkKg{txO MmfNNlU4PjFyOU[=
A2780 cells M4KxSGZ2dmO2aX;uJIF{e2G7 MkHMTY5pcWKrdHnvckBw\iCSQWLQJIlvKGi3bXHuJGEzPzhyIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhcHmmcn;n[Y4heGW{b4jp[IUucW6mdXPl[EBRSVK7bHH0bY9vKGK7IHPlcIwu[mG|ZXSgZZN{[Xl? MYWyOVc3OTB7Nh?=

... Click to View More Cell Line Experimental Data

In vivo MK-4827, a novel, orally bioavailable, PARP-1 and PARP-2 inhibitor, strongly enhanced the effect of radiation on a variety of human tumor xenografts, both p53 wild type and p53 mutant[1]. It was well tolerated in vivo and demonstrated efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer[2].


Cell Research:[2]
+ Expand
  • Cell lines: HeLa BRCA1-silenced cells
  • Concentrations: serial dilutions
  • Incubation Time: 7 days
  • Method: 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)
Animal Research:[1]
+ Expand
  • Animal Models: Female nude mice
  • Formulation: 0.5% Methocel in deionized water
  • Dosages: 25 mg/kg twice daily or 50 mg/kg once daily
  • Administration: oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 64 mg/mL (199.75 mM)
Ethanol 64 mg/mL (199.75 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 320.39


CAS No. 1038915-60-4
Storage powder
in solvent

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID