Niraparib (MK-4827)

Catalog No.S2741

For research use only.

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.

Niraparib (MK-4827) Chemical Structure

CAS No. 1038915-60-4

Selleck's Niraparib (MK-4827) has been cited by 59 publications

Purity & Quality Control

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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. 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 MmfYSpVv[3Srb36gZZN{[Xl? MoD4TY5pcWKrdHnvckBw\iCSQWLQJIlvKGi7ZILv[4VvKHCncn;4bYRmNWmwZIXj[YQhcHWvYX6gTIVN[SClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIFTORU1l[W2jZ3WtbY5lfWOnZDDQRXJ6dGG2aX;uMEBGSzVyPUCuNFA1KM7:TR?= MlfaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl6N{O5PFEoRjF7OEezPVgyRC:jPh?=
A549 cells MlPnR5l1d3SxeHnjbZR6KGG|c3H5 NH;KXVQ2NTdiZHH5dy=> NGrDUG5EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPTR7IHPlcIx{KHS{YX7z[oVkfGWmIIfpeIghSlKFQUKgd4hTVkFiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25iYX\0[ZIhPSC2bzC3JIRigXNiYomgR4VtdFSrdHXyMWJtfWViYYPzZZktKEOFNUC9NE4xOTFizszN NWLnO29URGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3OlExQTZpPkK1O|YyODl4PD;hQi=>
MDA-MB-436 cells NGfUZWZRem:uaX\ldoF1cW:wIHHzd4F6 M4CwVlYh\GG7cx?= NV3zS|dpSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvNEO2JINmdGy|IHX4dJJme3OrbnegRnJESTFiNUO5OkAsKDGJPlGgcZV1[W62IHHmeIVzKDZiZHH5d{BjgSClZXzsJJRqfGW{LXLseYUh[XO|YYmsJGNEPTB;MUigcm0> NWTMV3NIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm4O|M6QDFpPkG5PFc{QThzPD;hQi=>
SUM1315MO2 cells MV7DfZRwfG:6aXPpeJkh[XO|YYm= NGfQOGgyOiCmYYnz MWnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTWW0yOzF3TV:yJINmdGy|IHPhdpJ6cW6pIFLSR2EyKG23dHHueEBie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJINmdGxicILvcIln\XKjdHnvckBi\nSncjCxNkBl[Xm|IHL5JGNmdGyWaYTldk1DdHWnIHHzd4F6NCCFQ{WwQVAvODJizszN MlHIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5NkGwPVYoRjJ3N{[xNFk3RC:jPh?=
DoTc2-4510 cells NHHwe4hEgXSxdH;4bYNqfHliYYPzZZk> M3W5[VUuPyCmYYnz NITDSGxEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBFd1SlMj20OVExKGOnbHzzJINienK7aX7nJGJTS0F{IH31eIFvfCCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdiCjZoTldkA2KHSxIEeg[IF6eyCkeTDD[YxtXGm2ZYKtRox2\SCjc4PhfUwhS0N3ME2wMlAzOyEQvF2= M1f3ZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{[xNFk3Lz5{NUe2NVA6PjxxYU6=
SUM149PT cells Mlz0R5l1d3SxeHnjbZR6KGG|c3H5 MUG1MVch\GG7cx?= M3uwbGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNWVTF2OWDUJINmdGy|IHPhdpJ6cW6pIFLSR2EyKG23dHHueEBie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJINmdGxicILvcIln\XKjdHnvckBi\nSncjC1JJRwKDdiZHH5d{BjgSCFZXzsWIl1\XJvQnz1[UBie3OjeTygR2M2OD1yLkCyOEDPxE1? NWj3fGFWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3OlExQTZpPkK1O|YyODl4PD;hQi=>
UWB1.289 cells NIDzS4dEgXSxdH;4bYNqfHliYYPzZZk> MkXROU04KGSjeYO= NV7LOGRZS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hXVeEMT6yPFkh[2WubIOgZ4FzenmrbnegRnJESTFibYX0ZY51KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yh[2WubDDwdo9tcW[ncnH0bY9vKGGodHXyJFUhfG9iNzDkZZl{KGK7IFPlcIxVcXSncj3CcJVmKGG|c3H5MEBESzVyPUCuNFU3KM7:TR?= MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd4MUC5Okc,OjV5NkGwPVY9N2F-
Capan1 cells NXrRdXg3S3m2b4TvfIlkcXS7IHHzd4F6 NV;wT2VvS3m2b4TvfIlkcXS7IHHnZYlve3RiQmLDRVIu\GWoaXPp[Y51KGi3bXHuJGNieGGwMTDj[YxteyxiQ1O1NF0xNjB7IN88US=> NXLCeYM5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3OlExQTZpPkK1O|YyODl4PD;hQi=>
Jurkat cells NGPYOYJHfW6ldHnvckBie3OjeR?= NX7xZ|dUUW6qaXLpeIlwdiCxZjDQRXJROSCrbjDoeY1idiCMdYLrZZQh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKG:oIHPlcIwhfmmjYnnsbZR6KGGodHXyJFk3KGi{czDifUBOXFNiYYPzZZkhcW5icILld4Vv[2Vib3[gNVAxKHWPIH;mJJRmdW:8b3zvcYll\SxiRVO1NF0xNjJizszN NYnzUJR7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OVAyQTlpPkKzPFUxOTl7PD;hQi=>
BT20 cells NX7xd2hyS3m2b4TvfIlkcXS7IHHzd4F6 MoO5OU04KGSjeYO= MUXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDCWFIxKGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gZ4VtdCCycn;sbYZmemG2aX;uJIFnfGW{IEWgeI8hPyCmYYnzJIJ6KEOnbHzUbZRmei2EbIXlJIF{e2G7LDDDR|UxRTJwMjFOwG0> MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd4MUC5Okc,OjV5NkGwPVY9N2F-
Antiproliferative assay NF\aOHlJ\Uyj NYPNT291PyCmYYnz NH\KendCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JGJTS0FzIHTl[olkcWWwdDDoeY1idiCKZVzhJINmdGy|IHHmeIVzKDdiZHH5d{BjgSClZXzsJJRqfGW{LXLseYUh[XO|YYmsJGNEPTBiPTCwMlA{OyEQvF2u M120cVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OEezPVgyLz5zOUi3N|k5OTxxYU6=
Function assay M3jldGhmVGF? MkT5TY5pcWKrdHnvckBw\iCSQWLQJIlvKGi7ZILv[4VvKHCncn;4bYRmNWmwZIXj[YQhcHWvYX6gTIVN[SClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIFTORU1l[W2jZ3WtbY5lfWOnZDDQRXJ6dGG2aX;uMEBGSzlyIE2gNE4xPDVizszNMi=> MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTh5M{m4NUc,OTl6N{O5PFE9N2F-
Antiproliferative assay MXnDZZBidjF? NYm2c40xOTNiZHH5dy=> MluwRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCFYYDhclEh[2WubIOg[ZhxemW|c3nu[{BDWkODMjC2NVc1\GWuVDDteZRifGmxbjDhcoQhdG:|czDv[kB4cWymLYT5dIUh[WyuZXzlJIFnfGW{IEGzJIRigXNiYomgZ4VtdCC2aYTldk1jdHWnIHHzd4F6NCCFQ{WwJF0hOC5yOTFOwG0v M4SxPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OEezPVgyLz5zOUi3N|k5OTxxYU6=
Antiproliferative assay M3vpOWhmVGF? M3P5V|ch\GG7cx?= M{DJOGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSHXMZUBk\WyuczDlfJBz\XO|aX7nJJdqdGRidInw[UBDWkODMTDh[pRmeiB5IHThfZMh[nliY3XscEB1cXSncj3icJVmKGG|c3H5MEBESzVyIE2gNE45PiEQvF2u Mm\uQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl6N{O5PFEoRjF7OEezPVgyRC:jPh?=
Function assay MoDLTpVzc2G2 M3HZe|k3KGi{cx?= MYPJcohq[mm2aX;uJI9nKFCDUmCxJIlvKGi3bXHuJGp2emujdDDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gc4Yh[2WubDD2bYFjcWyrdImgZYZ1\XJiOU[gbJJ{KGK7IF3UV{Bie3OjeTygSWM2OCB;IEOxJO69VS5? M1LwNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OEWwNVk6Lz5{M{i1NFE6QTxxYU6=
Function assay M1HhXWNCWEGQLUG= M3nMWWlvcGmkaYTpc44hd2ZiUFHSVEBqdiCEUlPBNk1l\W[rY3nlcpQhcHWvYX6gR2FRSU5vMTDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGi7ZILv[4VvKHCncn;4bYRmNWmwZIXj[YQhWEGUeXzheIlwdiCkeTDj[YxtNWKjc3XkJIF{e2G7LDDJR|UxKD1iMD6wNFM2KM7:TT6= MlfBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5NkGwPVYoRjJ3N{[xNFk3RC:jPh?=
Function assay MYrI[Wxi NYrhdJpJUW6qaXLpeIlwdiCxZjDQRXJRKGmwIHj1cYFvKEinTHGgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCqeXTyc4dmdiCyZYLvfIll\S2rbnT1Z4VlKFCDUonsZZRqd25iYomgZ4VtdC2kYYPl[EBie3OjeTygSWM2OCB;IECuNFA1KM7:TT6= MnyzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5NkGwPVYoRjJ3N{[xNFk3RC:jPh?=
Function assay NH3rNZpCOjd6MB?= M{nYOmlvcGmkaYTpc44hd2ZiUFHSVEBqdiCqdX3hckBCOjd6MDDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGi7ZILv[4VvKHCncn;4bYRmNWmwZIXj[YQhWEGUeXzheIlwdiCkeTDj[YxtNWKjc3XkJIF{e2G7LDDJR|UxKD1iMD6wNFQh|ryPLh?= NGPwfXc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe2NVA6Pid-MkW3OlExQTZ:L3G+
Cytotoxicity assay NYf3OIFNVUSDLV3CMVQ{Pg>? NUjSb5NsS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDLV3CMVQ{PiClZXzsd{Bk[XK{eXnu[{BDWkODMTDteZRidnRiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25uIFPDOVAhRSByLkCxPEDPxE1w MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd4MUC5Okc,OjV5NkGwPVY9N2F-
Cytotoxicity assay MYrI[Wxi NIHEblI2KHSxIEeg[IF6ew>? NX3yb|g2S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUGWOYTDj[YxteyC2cnHud4Zm[3SnZDD3bZRpKEKUQ1GxJJNpWk6DIHHzd4V{e2WmIHHzJJJm\HWldHnvckBw\iClZXzsJJZq[WKrbHn0fUBi\nSncjC1JJRwKDdiZHH5d{BjgSCFZXzsWIl1\XJvQnz1[UBie3OjeTygR2M2OCB;IECuNFM1KM7:TT6= MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd4MUC5Okc,OjV5NkGwPVY9N2F-
Function assay NUL5UmNbUGWOYR?= NVnWVm5TUW6qaXLpeIlwdiCxZjDQRXJRKGmwIHj1cYFvKEinTHGgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCqeXTyc4dmdiCyZYLvfIll\S2rbnT1Z4VlKFCDUonsZZRqd25iYomgZ4VtdC2kYYPl[EBie3OjeTygTWM6OCB;IECuNFQ3KM7:TT6= M3rIclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{[xNFk3Lz5{NUe2NVA6PjxxYU6=
Function assay Mn7vR2FRSU5vMR?= MY\Jcohq[mm2aX;uJI9nKFCDUmCgbY4hSlKFQUKt[IVncWOrZX70JIh2dWGwIFPBVGFPNTFiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBpgWS{b3flckBx\XKxeHnk[U1qdmS3Y3XkJHBCWnmuYYTpc44h[nliY3XscE1j[XOnZDDhd5NigSxiSVO5NEA:KDBwMEWg{txONg>? M2TNZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{[xNFk3Lz5{NUe2NVA6PjxxYU6=
Function assay MVPBNlc5OA>? NY\QVoZxUW6qaXLpeIlwdiCxZjDQRXJRKGmwIHj1cYFvKEF{N{iwJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiaInkdo9o\W5icHXyc5hq\GVvaX7keYNm\CCSQWL5cIF1cW:wIHL5JINmdGxvYnHz[YQh[XO|YYmsJGlEQTBiPTCwMlA2OiEQvF2u M4Xm[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{[xNFk3Lz5{NUe2NVA6PjxxYU6=
Cytotoxicity assay M1Sy[2hmVGF? NXLQSllvPSC2bzC3JIRigXN? NIPiNmdEgXSxdH;4bYNqfHliYXfhbY5{fCC5aXzkJJR6eGViaIXtZY4hUGWOYTDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdiCjZoTldkA2KHSxIEeg[IF6eyCkeTDD[YxtXGm2ZYKtRox2\SCjc4PhfUwhS0N3MDC9JFAvQDV{IN88UU4> NUDpSIV7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3OlExQTZpPkK1O|YyODl4PD;hQi=>
Cytotoxicity assay NV;adJc6XVeEMT6yPFk> NYP6fIQ5PSC2bzC3JIRigXN? MYXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDVW2IyNjJ6OTDj[YxteyCneIDy[ZN{cW6pIFLSR2EyKGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yh[2WubDDwdo9tcW[ncnH0bY9vKGGodHXyJFUhfG9iNzDkZZl{KGK7IFPlcIxVcXSncj3CcJVmKGG|c3H5MEBESzVyIE2gNE46PzVizszNMi=> M3TSTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{[xNFk3Lz5{NUe2NVA6PjxxYU6=
Cytotoxicity assay NFXyTXdCPTR7 NYLGUFhWPSC2bzC3JIRigXN? NID0XnBEgXSxdH;4bYNqfHliYXfhbY5{fCC5aXzkJJR6eGViaIXtZY4hSTV2OTDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdiCjZoTldkA2KHSxIEeg[IF6eyCkeTDD[YxtXGm2ZYKtRox2\SCjc4PhfUwhS0N3MDC9JFEvPzZizszNMi=> NFXBXFQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe2NVA6Pid-MkW3OlExQTZ:L3G+
Cytotoxicity assay NG\DeFRE[XCjbkG= NF7kU|dEgXSxdH;4bYNqfHliYXfhbY5{fCCEUlPBNk1l\W[rY3nlcpQhcHWvYX6gR4Fx[W5zIHPlcIx{NCCHQ{WwJF0hOC54NTFOwG0v NEPCeZQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nk[1NlcyPyd-Mk[2OVI4OTd:L3G+
Antitumor assay NInKTZhOTEFvTVKtOFM3 Ml36OVAhdWdxa3e= NUS0WpN1OzNiZHH5dy=> MVPBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuPDN4IHPlcIx{KGW6cILld5NqdmdiQmLDRVEhPTN7NjCrJFFIRkFibYX0ZY51KHinbn;ndoFnfGWmIHnuJGNFOSCvb4Xz[UBie3Onc4Pl[EBieyC2dX3vdkBz\We{ZYPzbY9vKGG2IEWwJI1oN2upLDDwc{BjcWRiZn;yJFM{KGSjeYO= NIfE[G89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUi3N|k5OSd-MUm4O|M6QDF:L3G+
Antitumor assay MV\NSGEuVUJvNEO2 NInSdo4yODBibXevb4c> NI[5PFk{OyCmYYnz NYPmR3BKSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUSzOkBk\WyuczDlfJBz\XO|aX7nJGJTS0FzIEWzPVYhMyBzR{7BJI12fGGwdDD4[Y5w\3KjZoTl[EBqdiCFREGgcY92e2ViYYPz[ZN{\WRiYYOgeJVud3JicnXndoV{e2mxbjDheEAyODBibXevb4ctKHCxIIHkJIZweiB|MzDkZZl{ M1Lhc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OEezPVgyLz5zOUi3N|k5OTxxYU6=
Antitumor assay NVXpcm9XVUSDLV3CMVQ{Pg>? NUPxSJBIQDBibXevb4c> Ml7hNUB1dyB{IIfl[Yt{ NXS0UYI6SW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUSzOkBk\WyuczDoZZJjd3KrbnegRnJESTFibYX0ZY51KHinbn;ndoFnfGWmIHnuJIludXWwb3PvcZBzd22rc3XkJI1wfXOnIHHzd4V{e2WmIHHzJJR2dW:{IHfyc5d1cCCrbnjpZol1cW:wIHH0JFgxKG2pL3vnMEBxdyCzZDDmc5IhOSC2bzCyJJdm\Wu| NH;yNJo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe2NVA6Pid-MkW3OlExQTZ:L3G+
Antitumor assay MYHNSGEuVUJvNEO2 MVW4NEBu\y:tZx?= NULGS3RwPCC5ZXXrdy=> NXfkWJlOSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUSzOkBk\WyuczDoZZJjd3KrbnegRnJESTFibYX0ZY51KHinbn;ndoFnfGWmIHnuJIludXWwb3PvcZBzd22rc3XkJI1wfXOnIHHzd4V{e2WmIHHzJINwdXCuZYTlJIFv\CC|dYP0ZYlv\WRidIXtc5IhemWpcnXzd4lwdiCjdDC4NEBu\y:tZzygdI8heWRiZn;yJFQhf2Wna4O= MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd4MUC5Okc,OjV5NkGwPVY9N2F-
Antitumor assay M162R21FSS2PQj20N|Y> MXu1NEBu\y:tZx?= M{TxeWFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi12M{[gZ4VtdHNiaHHyZo9zcW6pIFLSR2EyKG23dHHueEB5\W6xZ4Lh[pRm\CCrbjDpcY12dm:lb33wdo9ucXOnZDDtc5V{\SCjc4Pld5Nm\CCjczD0eY1weiCpcn;3eIghcW6qaXLpeIlwdiCjdDC1NEBu\y:tZzygdI8h[WSvaX7pd5RmemWmIHThbYx6 Mon1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5NkGwPVYoRjJ3N{[xNFk3RC:jPh?=
Antitumor assay Mmj3UWRCNU2ELUSzOi=> MXu4NEBu\y:tZx?= NXTad2dDOyC5ZXXrdy=> NFvud5hCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvNEO2JINmdGy|IHjhdoJwemmwZzDCVmNCOSCvdYThcpQhgGWwb3fyZYZ1\WRiaX6gbY1ufW6xY3;tdJJwdWm|ZXSgcY92e2ViYYPz[ZN{\WRiYYOgeJVud3Jic3jybY5s[WenIHH0JFgxKG2pL3vnMEBxdyCzZDDmc5IhOyC5ZXXrdy=> MnvDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5NkGwPVYoRjJ3N{[xNFk3RC:jPh?=
qHTS assay M3LwXnREOzJ? NYT3bXpmeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGTDN|Ih[2WubIO= NIPvfYM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
qHTS assay NWXiUG1jSTZ5Mx?= NHHYOZNyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQU[3N{Bk\Wyucx?= MmrIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
qHTS assay MVLORlE3PDN? MknKdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE6EMU[0N{Bk\Wyucx?= NFKxWWo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
qHTS assay MXPBOlc{ MorkdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgRVY4OyClZXzsd{k> NUDwPFZNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
qHTS assay NULqeVZISlRvM{e= M1n6UJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJGJVNTN5IHPlcIx{ NHWzZVE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
qHTS assay NYTVbmpHW0tvTj3NRy=> NWrhRWp[eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPLMW4uVUNiY3XscJM> NX7YTHE5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
qHTS assay M1PsfG5DNUWEY{G= NI\FZpdyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKtSWJkOSClZXzsdy=> Moj3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
qHTS assay M{PaXGxCVi13 NWr5d|RmeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFzBUk02KGOnbHzz Moq1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
qHTS assay NHXZV45UUy2QLV3D MX3xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDTT{1PNU2FIHPlcIx{ NHzwWZI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
qHTS assay NIDiW4hVSzN{ MV;xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDUR|MzKGOnbHzz Ml;DQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Assay
Methods Test Index PMID
Western blot c-PARP /c-caspase 3 / γ-H2AX 29158830
Immunofluorescence Rad51 / Geminin 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 (from reference)

Cell Research:[2]
  • 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.
Animal Research:[1]
  • Animal Models: Female nude mice
  • Dosages: 25 mg/kg twice daily or 50 mg/kg once daily
  • Administration: oral administration

Solubility (25°C)

In vitro

DMSO 64 mg/mL warmed
(199.75 mM)
Water Insoluble
Ethanol '64 mg/mL

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

Chemical Information

Molecular Weight 320.39
Formula

C19H20N4O

CAS No. 1038915-60-4
Storage 3 years -20°C powder
2 years -80°C in solvent
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)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04149145 Not yet recruiting Drug: M4344+Niraparib Ovarian Cancer Recurrent University of Alabama at Birmingham December 2021 Phase 1
NCT05076513 Recruiting Drug: Niraparib|Radiation: Radiation therapy Glioblastoma|Glioblastoma Multiforme|Glioma|GBM|Glioma Malignant|Glioblastoma Multiforme of Brain Nader Sanai|Barrow Neurological Institute|Ivy Brain Tumor Center|University of California San Francisco|GlaxoSmithKline|St. Joseph''s Hospital and Medical Center Phoenix October 29 2021 Early Phase 1
NCT04986371 Not yet recruiting Drug: Niraparib Epithelial Ovarian Cancer Ling-Ying Wu|Chinese Academy of Medical Sciences August 10 2021 --
NCT04972110 Recruiting Drug: RP-3500 Advanced Solid Tumor Adult Repare Therapeutics July 21 2021 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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
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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.

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