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.
Targets
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 MVnGeY5kfGmxbjDhd5NigQ>? NFrkdXlKdmirYnn0bY9vKG:oIGDBVnAhcW5iaInkdo9o\W5icHXyc5hq\GVvaX7keYNm\CCqdX3hckBJ\UyjIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gSG5CNWSjbXHn[U1qdmS3Y3XkJHBCWnmuYYTpc44tKEWFNUC9NE4xODRizszN M3;aSVE6QDd|OUix
A549 cells NW\melgyS3m2b4TvfIlkcXS7IHHzd4F6 NIK0TVg2NTdiZHH5dy=> MWDDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJJRz[W6|ZnXjeIVlKHerdHigRnJESTJic3jSUmEh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBk\WyuIIDyc4xq\mW{YYTpc44h[W[2ZYKgOUB1dyB5IHThfZMh[nliQ3XscHRqfGW{LVLseYUh[XO|YYmsJGNEPTB;MD6wNVEh|ryP NV[3c4xpOjV5NkGwPVY>
MDA-MB-436 cells MnzPVJJwdGmoZYLheIlwdiCjc4PhfS=> MmDnOkBl[Xm| MnL5RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuPDN4IHPlcIx{KGW6cILld5NqdmdiQmLDRVEhPTN7NjCrJFFIRkFibYX0ZY51KGGodHXyJFYh\GG7czDifUBk\WyuIITpeIVzNWKudXWgZZN{[XluIFPDOVA:OThibl2= MnfENVk5PzN7OEG=
SUM1315MO2 cells M33Q[WN6fG:2b4jpZ4l1gSCjc4PhfS=> Ml7sNVIh\GG7cx?= MXrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTWW0yOzF3TV:yJINmdGy|IHPhdpJ6cW6pIFLSR2EyKG23dHHueEBie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJINmdGxicILvcIln\XKjdHnvckBi\nSncjCxNkBl[Xm|IHL5JGNmdGyWaYTldk1DdHWnIHHzd4F6NCCFQ{WwQVAvODJizszN NVvXcpVxOjV5NkGwPVY>
DoTc2-4510 cells MojIR5l1d3SxeHnjbZR6KGG|c3H5 M3\tPVUuPyCmYYnz MWnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDEc3RkOi12NUGwJINmdGy|IHPhdpJ6cW6pIFLSR2EzKG23dHHueEBie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJINmdGxicILvcIln\XKjdHnvckBi\nSncjC1JJRwKDdiZHH5d{BjgSCFZXzsWIl1\XJvQnz1[UBie3OjeTygR2M2OD1yLkCyN{DPxE1? Ml7sNlU4PjFyOU[=
SUM149PT cells M1fMUmN6fG:2b4jpZ4l1gSCjc4PhfS=> MUG1MVch\GG7cx?= NGHRSJNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUXU1zNEnQWEBk\WyuczDjZZJzgWmwZzDCVmNCOSCvdYThcpQh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBk\WyuIIDyc4xq\mW{YYTpc44h[W[2ZYKgOUB1dyB5IHThfZMh[nliQ3XscHRqfGW{LVLseYUh[XO|YYmsJGNEPTB;MD6wNlQh|ryP NH\pOJczPTd4MUC5Oi=>
UWB1.289 cells M2PzWGN6fG:2b4jpZ4l1gSCjc4PhfS=> MXq1MVch\GG7cx?= MYjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDVW2IyNjJ6OTDj[YxteyClYYLyfYlv\yCEUlPBNUBufXSjboSgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36gZYZ1\XJiNTD0c{A4KGSjeYOgZpkhS2WubGTpeIVzNUKudXWgZZN{[XluIFPDOVA:OC5yNU[g{txO MXiyOVc3OTB7Nh?=
Capan1 cells NEPob5BEgXSxdH;4bYNqfHliYYPzZZk> MXfDfZRwfG:6aXPpeJkh[WejaX7zeEBDWkODMj3k[YZq[2mnboSgbJVu[W5iQ3HwZY4yKGOnbHzzMEBESzVyPUCuNFkh|ryP MVSyOVc3OTB7Nh?=
Jurkat cells M4X6fmZ2dmO2aX;uJIF{e2G7 NXPtbpF6UW6qaXLpeIlwdiCxZjDQRXJROSCrbjDoeY1idiCMdYLrZZQh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKG:oIHPlcIwhfmmjYnnsbZR6KGGodHXyJFk3KGi{czDifUBOXFNiYYPzZZkhcW5icILld4Vv[2Vib3[gNVAxKHWPIH;mJJRmdW:8b3zvcYll\SxiRVO1NF0xNjJizszN NXHQT3BDOjN6NUCxPVk>
BT20 cells MkLRR5l1d3SxeHnjbZR6KGG|c3H5 M2jIflUuPyCmYYnz MWnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDCWFIxKGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gZ4VtdCCycn;sbYZmemG2aX;uJIFnfGW{IEWgeI8hPyCmYYnzJIJ6KEOnbHzUbZRmei2EbIXlJIF{e2G7LDDDR|UxRTJwMjFOwG0> M{nKZVI2PzZzMEm2
A2780 cells M2LKe2Z2dmO2aX;uJIF{e2G7 MWnJcohq[mm2aX;uJI9nKFCDUmCgbY4hcHWvYX6gRVI4QDBiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBpgWS{b3flckBx\XKxeHnk[U1qdmS3Y3XkJHBCWnmuYYTpc44h[nliY3XscE1j[XOnZDDhd5NigQ>? M{nOUlI2PzZzMEm2

... 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].

Protocol

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
Formula

C19H20N4O

CAS No. 1038915-60-4
Storage powder
Synonyms

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Related Antibodies

PARP Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID