Niraparib (MK-4827)

For research use only.

Catalog No.S2741

49 publications

Niraparib (MK-4827) Chemical Structure

CAS No. 1038915-60-4

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. Niraparib can form PARP–DNA complexes resulting in DNA damage, apoptosis, and cell death. Phase 3.

Size Price Stock Quantity  
10mM (1mL in DMSO) USD 170 In stock
USD 170 In stock
USD 320 In stock
USD 970 In stock
USD 2470 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Selleck's Niraparib (MK-4827) has been cited by 49 publications

Purity & Quality Control

Choose Selective PARP Inhibitors

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. Niraparib can form PARP–DNA complexes resulting in DNA damage, apoptosis, and cell death. 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 M37kcGZ2dmO2aX;uJIF{e2G7 M2nESWlvcGmkaYTpc44hd2ZiUFHSVEBqdiCqeXTyc4dmdiCyZYLvfIll\S2rbnT1Z4VlKGi3bXHuJGhmVGFiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDEUmEu\GGvYXflMYlv\HWlZXSgVGFTgWyjdHnvckwhTUN3ME2wMlAxPCEQvF2= MkjjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl6N{O5PFEoRjF7OEezPVgyRC:jPh?=
A549 cells M3frd2N6fG:2b4jpZ4l1gSCjc4PhfS=> NHfjWpg2NTdiZHH5dy=> NFTLTINEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPTR7IHPlcIx{KHS{YX7z[oVkfGWmIIfpeIghSlKFQUKgd4hTVkFiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25iYX\0[ZIhPSC2bzC3JIRigXNiYomgR4VtdFSrdHXyMWJtfWViYYPzZZktKEOFNUC9NE4xOTFizszN NHGxWIc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe2NVA6Pid-MkW3OlExQTZ:L3G+
MDA-MB-436 cells MYHQdo9tcW[ncnH0bY9vKGG|c3H5 M2nHZlYh\GG7cx?= MUPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2GQT3NRk01OzZiY3XscJMh\XiycnXzd4lv\yCEUlPBNUA2Ozl4IDugNWc,SSCvdYThcpQh[W[2ZYKgOkBl[Xm|IHL5JINmdGxidHn0[ZIu[my3ZTDhd5NigSxiQ1O1NF0yQCCwTR?= M3zsTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OEezPVgyLz5zOUi3N|k5OTxxYU6=
SUM1315MO2 cells MVfDfZRwfG:6aXPpeJkh[XO|YYm= NV7lSWxCOTJiZHH5dy=> Mle5R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV3VOOTNzNV3PNkBk\WyuczDjZZJzgWmwZzDCVmNCOSCvdYThcpQh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBk\WyuIIDyc4xq\mW{YYTpc44h[W[2ZYKgNVIh\GG7czDifUBE\WyuVHn0[ZIuSmy3ZTDhd5NigSxiQ1O1NF0xNjB{IN88US=> M2CyW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{[xNFk3Lz5{NUe2NVA6PjxxYU6=
DoTc2-4510 cells MXHDfZRwfG:6aXPpeJkh[XO|YYm= M2DvVVUuPyCmYYnz Mn[0R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gSI9V[zJvNEWxNEBk\WyuczDjZZJzgWmwZzDCVmNCOiCvdYThcpQh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBk\WyuIIDyc4xq\mW{YYTpc44h[W[2ZYKgOUB1dyB5IHThfZMh[nliQ3XscHRqfGW{LVLseYUh[XO|YYmsJGNEPTB;MD6wNlMh|ryP NIjRSY49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe2NVA6Pid-MkW3OlExQTZ:L3G+
SUM149PT cells NVq5[lQxS3m2b4TvfIlkcXS7IHHzd4F6 NFvvN2Q2NTdiZHH5dy=> MVHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTWW0yPDmSVDDj[YxteyClYYLyfYlv\yCEUlPBNUBufXSjboSgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36gZYZ1\XJiNTD0c{A4KGSjeYOgZpkhS2WubGTpeIVzNUKudXWgZZN{[XluIFPDOVA:OC5yMkSg{txO MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd4MUC5Okc,OjV5NkGwPVY9N2F-
UWB1.289 cells MWDDfZRwfG:6aXPpeJkh[XO|YYm= MXu1MVch\GG7cx?= MX7DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDVW2IyNjJ6OTDj[YxteyClYYLyfYlv\yCEUlPBNUBufXSjboSgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36gZYZ1\XJiNTD0c{A4KGSjeYOgZpkhS2WubGTpeIVzNUKudXWgZZN{[XluIFPDOVA:OC5yNU[g{txO NXvEOmg2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3OlExQTZpPkK1O|YyODl4PD;hQi=>
Capan1 cells MlzyR5l1d3SxeHnjbZR6KGG|c3H5 MUnDfZRwfG:6aXPpeJkh[WejaX7zeEBDWkODMj3k[YZq[2mnboSgbJVu[W5iQ3HwZY4yKGOnbHzzMEBESzVyPUCuNFkh|ryP NIH4NXA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe2NVA6Pid-MkW3OlExQTZ:L3G+
Jurkat cells M1yzU2Z2dmO2aX;uJIF{e2G7 M1;XfWlvcGmkaYTpc44hd2ZiUFHSVFEhcW5iaIXtZY4hUnW{a3H0JINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBw\iClZXzsJJZq[WKrbHn0fUBi\nSncjC5OkBpenNiYomgUXRUKGG|c3H5JIlvKHC{ZYPlcoNmKG:oIEGwNEB2VSCxZjD0[Y1wgm:ub33p[IUtKEWFNUC9NE4zKM7:TR?= M1m5SFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OEWwNVk6Lz5{M{i1NFE6QTxxYU6=
BT20 cells M{DwdmN6fG:2b4jpZ4l1gSCjc4PhfS=> NX\J[GFZPS15IHThfZM> NYrwUYFZS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSlR{MDDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdiCjZoTldkA2KHSxIEeg[IF6eyCkeTDD[YxtXGm2ZYKtRox2\SCjc4PhfUwhS0N3ME2yMlIh|ryP NGnrc4g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe2NVA6Pid-MkW3OlExQTZ:L3G+
Antiproliferative assay M4WzdWhmVGF? M2e4e|ch\GG7cx?= NELYWnNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JGJTS0FzIHTl[olkcWWwdDDoeY1idiCKZVzhJINmdGy|IHHmeIVzKDdiZHH5d{BjgSClZXzsJJRqfGW{LXLseYUh[XO|YYmsJGNEPTBiPTCwMlA{OyEQvF2u M{HPdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OEezPVgyLz5zOUi3N|k5OTxxYU6=
Function assay NV3t[5Y4UGWOYR?= NXnUb|I{UW6qaXLpeIlwdiCxZjDQRXJRKGmwIHj5[JJw\2WwIIDldo95cWSnLXnu[JVk\WRiaIXtZY4hUGWOYTDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJGRPSS2mYX3h[4UucW6mdXPl[EBRSVK7bHH0bY9vNCCHQ{mwJF0hOC5yNEWg{txONg>? NFf2fFg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUi3N|k5OSd-MUm4O|M6QDF:L3G+
Antiproliferative assay MV3DZZBidjF? MlrwNVMh\GG7cx?= MXzBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEOjcHHuNUBk\WyuczDlfJBz\XO|aX7nJGJTS0F{IE[xO|Rl\WyWIH31eIF1cW:wIHHu[EBtd3O|IH;mJJdqdGRvdInw[UBidGynbHWgZYZ1\XJiMUOg[IF6eyCkeTDj[YxtKHSrdHXyMYJtfWViYYPzZZktKEOFNUCgQUAxNjB7IN88UU4> MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTh5M{m4NUc,OTl6N{O5PFE9N2F-
Antiproliferative assay MkHNTIVN[Q>? Mn3YO{Bl[Xm| NVzwNmFpSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDI[WxiKGOnbHzzJIV5eHKnc4Ppcochf2muZDD0fZBmKEKUQ1GxJIFnfGW{IEeg[IF6eyCkeTDj[YxtKHSrdHXyMYJtfWViYYPzZZktKEOFNUCgQUAxNjh4IN88UU4> NFjq[FE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUi3N|k5OSd-MUm4O|M6QDF:L3G+
Function assay NX;hT2pMUnW{a3H0 M4D2flk3KGi{cx?= NWLRTJNmUW6qaXLpeIlwdiCxZjDQRXJROSCrbjDoeY1idiCMdYLrZZQh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKG:oIHPlcIwhfmmjYnnsbZR6KGGodHXyJFk3KGi{czDifUBOXFNiYYPzZZktKEWFNUCgQUA{OSEQvF2u M1L0OVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OEWwNVk6Lz5{M{i1NFE6QTxxYU6=
Function assay MUDDRXBCVi1z MXrJcohq[mm2aX;uJI9nKFCDUmCgbY4hSlKFQUKt[IVncWOrZX70JIh2dWGwIFPBVGFPNTFiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBpgWS{b3flckBx\XKxeHnk[U1qdmS3Y3XkJHBCWnmuYYTpc44h[nliY3XscE1j[XOnZDDhd5NigSxiSVO1NEA:KDBwMECzOUDPxE1w MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd4MUC5Okc,OjV5NkGwPVY9N2F-
Function assay NFPJTIdJ\Uyj NYfIfYNOUW6qaXLpeIlwdiCxZjDQRXJRKGmwIHj1cYFvKEinTHGgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCqeXTyc4dmdiCyZYLvfIll\S2rbnT1Z4VlKFCDUonsZZRqd25iYomgZ4VtdC2kYYPl[EBie3OjeTygSWM2OCB;IECuNFA1KM7:TT6= MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd4MUC5Okc,OjV5NkGwPVY9N2F-
Function assay MnLSRVI4QDB? Mn\1TY5pcWKrdHnvckBw\iCSQWLQJIlvKGi3bXHuJGEzPzhyIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhcHmmcn;n[Y4heGW{b4jp[IUucW6mdXPl[EBRSVK7bHH0bY9vKGK7IHPlcIwu[mG|ZXSgZZN{[XluIFnDOVAhRSByLkCwOEDPxE1w MkHZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5NkGwPVYoRjJ3N{[xNFk3RC:jPh?=
Cytotoxicity assay MV\NSGEuVUJvNEO2 M1u0eGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1FSS2PQj20N|Yh[2WubIOgZ4FzenmrbnegRnJESTFibYX0ZY51KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yh[2WubDDwdo9tcW[ncnH0bY9vNCCFQ{WwJF0hOC5yMUig{txONg>? NXnmc2NiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3OlExQTZpPkK1O|YyODl4PD;hQi=>
Cytotoxicity assay MXTI[Wxi MVS1JJRwKDdiZHH5dy=> NGLlXYJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJ\UyjIHPlcIx{KHS{YX7z[oVkfGWmIIfpeIghSlKFQUGgd4hTVkFiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJI9nKGOnbHygeoli[mmuaYT5JIFnfGW{IEWgeI8hPyCmYYnzJIJ6KEOnbHzUbZRmei2EbIXlJIF{e2G7LDDDR|UxKD1iMD6wN|Qh|ryPLh?= NFj2WXI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe2NVA6Pid-MkW3OlExQTZ:L3G+
Function assay M1HLfGhmVGF? MnXUTY5pcWKrdHnvckBw\iCSQWLQJIlvKGi3bXHuJGhmVGFiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBpgWS{b3flckBx\XKxeHnk[U1qdmS3Y3XkJHBCWnmuYYTpc44h[nliY3XscE1j[XOnZDDhd5NigSxiSVO5NEA:KDBwMES2JO69VS5? MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd4MUC5Okc,OjV5NkGwPVY9N2F-
Function assay MnnBR2FRSU5vMR?= MVPJcohq[mm2aX;uJI9nKFCDUmCgbY4hSlKFQUKt[IVncWOrZX70JIh2dWGwIFPBVGFPNTFiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBpgWS{b3flckBx\XKxeHnk[U1qdmS3Y3XkJHBCWnmuYYTpc44h[nliY3XscE1j[XOnZDDhd5NigSxiSVO5NEA:KDBwMEWg{txONg>? M1vBO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{[xNFk3Lz5{NUe2NVA6PjxxYU6=
Function assay MWHBNlc5OA>? MWfJcohq[mm2aX;uJI9nKFCDUmCgbY4hcHWvYX6gRVI4QDBiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBpgWS{b3flckBx\XKxeHnk[U1qdmS3Y3XkJHBCWnmuYYTpc44h[nliY3XscE1j[XOnZDDhd5NigSxiSVO5NEA:KDBwMEWyJO69VS5? Mo\sQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5NkGwPVYoRjJ3N{[xNFk3RC:jPh?=
Cytotoxicity assay MlzVTIVN[Q>? M17NXVUhfG9iNzDkZZl{ MV3DfZRwfG:6aXPpeJkh[WejaX7zeEB4cWymIIT5dIUhcHWvYX6gTIVN[SClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJINmdGxicILvcIln\XKjdHnvckBi\nSncjC1JJRwKDdiZHH5d{BjgSCFZXzsWIl1\XJvQnz1[UBie3OjeTygR2M2OCB;IECuPFUzKM7:TT6= MlTKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5NkGwPVYoRjJ3N{[xNFk3RC:jPh?=
Cytotoxicity assay M1niVnVYSjFwMki5 M3HGfFUhfG9iNzDkZZl{ NY\PSoJRS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hXVeEMT6yPFkh[2WubIOg[ZhxemW|c3nu[{BDWkODMTDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHPlcIwheHKxbHnm[ZJifGmxbjDh[pRmeiB3IITvJFch\GG7czDifUBE\WyuVHn0[ZIuSmy3ZTDhd5NigSxiQ1O1NEA:KDBwOUe1JO69VS5? M1;TRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{[xNFk3Lz5{NUe2NVA6PjxxYU6=
Cytotoxicity assay NEHUfYFCPTR7 MV61JJRwKDdiZHH5dy=> NEPOXZZEgXSxdH;4bYNqfHliYXfhbY5{fCC5aXzkJJR6eGViaIXtZY4hSTV2OTDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdiCjZoTldkA2KHSxIEeg[IF6eyCkeTDD[YxtXGm2ZYKtRox2\SCjc4PhfUwhS0N3MDC9JFEvPzZizszNMi=> M1;RfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{[xNFk3Lz5{NUe2NVA6PjxxYU6=
Cytotoxicity assay M2HV[mNieGGwMR?= NFPHSZBEgXSxdH;4bYNqfHliYXfhbY5{fCCEUlPBNk1l\W[rY3nlcpQhcHWvYX6gR4Fx[W5zIHPlcIx{NCCHQ{WwJF0hOC54NTFOwG0v Mo\RQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ4NUK3NVcoRjJ4NkWyO|E4RC:jPh?=
Antitumor assay MlnGUWRCNU2ELUSzOi=> NVH4VZJ[PTBibXevb4c> M3q1d|M{KGSjeYO= NILNZXpCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvNEO2JINmdGy|IHX4dJJme3OrbnegRnJESTFiNUO5OkAsKDGJPlGgcZV1[W62IIjlco9oemGodHXkJIlvKEOGMTDtc5V{\SCjc4Pld5Nm\CCjczD0eY1weiC{ZXfy[ZN{cW:wIHH0JFUxKG2pL3vnMEBxdyCkaXSg[o9zKDN|IHThfZM> MmLvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl6N{O5PFEoRjF7OEezPVgyRC:jPh?=
Antitumor assay Mk\lUWRCNU2ELUSzOi=> MYGxNFAhdWdxa3e= NX;OVXU3OzNiZHH5dy=> NXj6NGFPSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUSzOkBk\WyuczDlfJBz\XO|aX7nJGJTS0FzIEWzPVYhMyBzR{7BJI12fGGwdDD4[Y5w\3KjZoTl[EBqdiCFREGgcY92e2ViYYPz[ZN{\WRiYYOgeJVud3JicnXndoV{e2mxbjDheEAyODBibXevb4ctKHCxIIHkJIZweiB|MzDkZZl{ MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTh5M{m4NUc,OTl6N{O5PFE9N2F-
Antitumor assay M2\wUW1FSS2PQj20N|Y> MlTkPFAhdWdxa3e= NHmxNFgyKHSxIEKge4Vmc3N? MW\BcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuPDN4IHPlcIx{KGijcnLvdolv\yCEUlPBNUBufXSjboSgfIVvd2e{YX\0[YQhcW5iaX3teY5w[2:vcILvcYl{\WRibX;1d4Uh[XO|ZYPz[YQh[XNidIXtc5Ih\3Kxd4ToJIlvcGmkaYTpc44h[XRiOECgcYcwc2duIIDvJJFlKG[xcjCxJJRwKDJid3Xlb5M> NYn4TnZQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3OlExQTZpPkK1O|YyODl4PD;hQi=>
Antitumor assay NVjpVVBsVUSDLV3CMVQ{Pg>? NH;VfnE5OCCvZz;r[y=> MnHaOEB4\WWtcx?= NVH5fW5PSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUSzOkBk\WyuczDoZZJjd3KrbnegRnJESTFibYX0ZY51KHinbn;ndoFnfGWmIHnuJIludXWwb3PvcZBzd22rc3XkJI1wfXOnIHHzd4V{e2WmIHHzJINwdXCuZYTlJIFv\CC|dYP0ZYlv\WRidIXtc5IhemWpcnXzd4lwdiCjdDC4NEBu\y:tZzygdI8heWRiZn;yJFQhf2Wna4O= M4jhcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{[xNFk3Lz5{NUe2NVA6PjxxYU6=
Antitumor assay MVfNSGEuVUJvNEO2 MXe1NEBu\y:tZx?= MVLBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuPDN4IHPlcIx{KGijcnLvdolv\yCEUlPBNUBufXSjboSgfIVvd2e{YX\0[YQhcW5iaX3teY5w[2:vcILvcYl{\WRibX;1d4Uh[XO|ZYPz[YQh[XNidIXtc5Ih\3Kxd4ToJIlvcGmkaYTpc44h[XRiNUCgcYcwc2duIIDvJIFldWmwaYP0[ZJm\CCmYXnsfS=> MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd4MUC5Okc,OjV5NkGwPVY9N2F-
Antitumor assay NF\XeGZOTEFvTVKtOFM3 NHTRR|M5OCCvZz;r[y=> NHizXo8{KHenZXvz M1zpTWFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi12M{[gZ4VtdHNiaHHyZo9zcW6pIFLSR2EyKG23dHHueEB5\W6xZ4Lh[pRm\CCrbjDpcY12dm:lb33wdo9ucXOnZDDtc5V{\SCjc4Pld5Nm\CCjczD0eY1weiC|aILpcoti\2ViYYSgPFAhdWdxa3esJJBwKHGmIH\vdkA{KHenZXvz NHW3TIw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe2NVA6Pid-MkW3OlExQTZ:L3G+
qHTS assay NXzM[lZpXEN|Mh?= MkW3dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFSFM{KgZ4VtdHN? M4ri[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
qHTS assay NXTISIt[STZ5Mx?= M1OxfJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCDNkezJINmdGy| M2PDWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
qHTS assay M2jSem5DOTZ2Mx?= NG\ic41yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKxOlQ{KGOnbHzz NVfoRYJuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
qHTS assay NGj6NnRCPjd| M{mweZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJGE3PzNiY3XscJMq Mk[yQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
qHTS assay MYjCWE0{Pw>? M2DlfJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJGJVNTN5IHPlcIx{ Mnq5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
qHTS assay NI[1epNUUy2QLV3D MX;xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?= NV:xVJV5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
qHTS assay MmXtUmIuTUKlMR?= NHrQNJpyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKtSWJkOSClZXzsdy=> MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
qHTS assay M4LnRmxCVi13 M2LkeJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCOQV6tOUBk\Wyucx?= MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
qHTS assay Mof1V2suVi2PQx?= NXe0PFh5eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?= NInLSVM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
qHTS assay M1j5cHREOzJ? M4f5[ZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHREOzJiY3XscJM> NXHtPHRnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
c-PARP /c-caspase 3 / γ-H2AX; 

PubMed: 29158830     


Western Blot data testing protein expression after treatment with Olaparib, Niraparib, and Talazoparib on Brca1-deficient cell line in W0069 cells.

29158830
Immunofluorescence
Rad51 / Geminin; 

PubMed: 27614696     


Immunofluorescence microscopy of niraparib-treated PDX cells (PH039) and irradiated cells showing RAD51 foci (arrow) within geminin positive cells and lack of RAD51 foci formation in control cells. 

27614696
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]
- Collapse
  • 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]
- Collapse
  • Animal Models: Female nude mice
  • 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
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+40% PEG 300+5% Tween 80+ 50% ddH2O
For best results, use promptly after mixing.
2.5mg/mL

* 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
in solvent
Synonyms
Smiles C1CC(CNC1)C2=CC=C(C=C2)N3C=C4C=CC=C(C4=N3)C(=O)N

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04655183 Not yet recruiting Drug: Niraparib|Drug: M4344 Advanced Solid Tumor|Breast Cancer EMD Serono Research & Development Institute Inc.|Merck KGaA Darmstadt Germany|EMD Serono December 1 2020 Phase 1|Phase 2
NCT04544995 Recruiting Drug: Niraparib|Drug: Dostarlimab Neoplasms GlaxoSmithKline October 6 2020 Phase 1
NCT04475939 Recruiting Drug: Niraparib|Drug: Pembrolizumab|Drug: Placebo Lung Cancer Non-Small Cell GlaxoSmithKline October 26 2020 Phase 3
NCT04546373 Recruiting Drug: Niraparib Epithelial Ovarian Cancer|Fallopian Tube Cancer|Primary Peritoneal Cancer Grupo Español de Investigación en Cáncer de Ovario September 30 2020 --

Tech Support

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Frequently Asked Questions

  • Question 1:

    How to reconstitute the compound for in vivo studies?

  • Answer:

    You can use the formulation 1% CMC-Na (suspension) for oral administration.

PARP Signaling Pathway Map

Related PARP Products

Tags: buy Niraparib (MK-4827) | Niraparib (MK-4827) supplier | purchase Niraparib (MK-4827) | Niraparib (MK-4827) cost | Niraparib (MK-4827) manufacturer | order Niraparib (MK-4827) | Niraparib (MK-4827) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID