Niraparib (MK-4827)

Name: Niraparib (MK-4827)
Brand: Selleck Chemicals
SKU: S2741
Rating: 5 (43 reviews)

For research use only.

Catalog No.S2741

43 publications

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.

Selleck's Niraparib (MK-4827) has been cited by 43 publications

Cancer Cell, 2020, 15 pii: S1535-6108(20)30164-1

PubMed: 32359397 ( click the link to review the publication )

Nat Med, 2019, 25(5):838-849

PubMed: 31011202 ( click the link to review the publication )

Cancer Discov, 2019, 9(7):852-871

PubMed: 31053628 ( click the link to review the publication )

Cell, 2018, 172(1-2):373-386

PubMed: 29224780 ( click the link to review the publication )

J Exp Clin Cancer Res, 2021, 40(1):15

PubMed: 33407715 ( click the link to review the publication )

Cell Death Dis, 2021, 12(2):183

PubMed: 33589588 ( click the link to review the publication )

J Invest Dermatol, 2021, S0022-202X(21)00155-X

PubMed: 33610559 ( click the link to review the publication )

Nat Commun, 2021, 12(1):736

PubMed: 33531508 ( click the link to review the publication )

Sci Adv, 2020, 6(51)eabb8626

PubMed: 33355125 ( click the link to review the publication )

Nat Commun, 2020, 11(1):752

PubMed: 32029722 ( click the link to review the publication )

Nat Commun, 2020, 22;11(1):2573

PubMed: 32444794 ( click the link to review the publication )

Cell Rep, 2020, 33(2):108240

PubMed: 33053351 ( click the link to review the publication )

Elife, 2020, 9e60637

PubMed: 32844745 ( click the link to review the publication )

J Clin Med, 2020, 30;9(4)

PubMed: 32235451 ( click the link to review the publication )

Am J Cancer Res, 2020, 10(9):2813-2831

PubMed: 33042619 ( click the link to review the publication )

Mol Cancer Res, 2020, 10.1158/1541-7786.MCR-19-0669

PubMed: 32238439 ( click the link to review the publication )

Sci Rep, 2020, 17;10(1):2585

PubMed: 32066817 ( click the link to review the publication )

Front Pharmacol, 2020, 11:610205

PubMed: 33519476 ( click the link to review the publication )

Front Genet, 2020, 11:1036

PubMed: 33133138 ( click the link to review the publication )

Head Neck, 2020, 10.1002/hed.26155

PubMed: 32323895 ( click the link to review the publication )

SLAS Discov, 2020, 25(3):241-252

PubMed: 31855104 ( click the link to review the publication )

Nat Commun, 2020, 11(1):6118

PubMed: 33257658 ( click the link to review the publication )

EMBO Mol Med, 2020, 12(12):e12391

PubMed: 33231937 ( click the link to review the publication )

Oncotarget, 2020, 11(23):2141-2159

PubMed: 32577161 ( click the link to review the publication )
BMC Cancer, 2020, 20(1):775

PubMed: 32811446 ( click the link to review the publication )

Biol Blood Marrow Transplant, 2020, 10.1016

PubMed: 32194286 ( click the link to review the publication )

Nat Commun, 2019, 10(1):5661

PubMed: 31827092 ( click the link to review the publication )

Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-19-2409

PubMed: 31831554 ( click the link to review the publication )

Cell Rep, 2019, 27(12):3422-3432

PubMed: 31216465 ( click the link to review the publication )

Mol Cancer Ther, 2019, 10.1158/1535-7163.MCT-19-0242

PubMed: 31534014 ( click the link to review the publication )

Endocrinology, 2019, 160(11):2600-2617

PubMed: 31322702 ( click the link to review the publication )

Biochem Biophys Res Commun, 2019, 510(4):501-507

PubMed: 30737031 ( click the link to review the publication )

Spectrochim Acta A Mol Biomol Spectrosc, 2019, 206:126-134

PubMed: 30096696 ( click the link to review the publication )

Nat Commun, 2018, 9(1):2678

PubMed: 29992957 ( click the link to review the publication )

Nat Commun, 2018, 9(1):176

PubMed: 29330466 ( click the link to review the publication )

Clin Cancer Res, 2018, 24(23):6066-6077

PubMed: 30061362 ( click the link to review the publication )

Elife, 2018, 7

PubMed: 30088474 ( click the link to review the publication )

Cancer Biol Ther, 2018, 19(9):786-796

PubMed: 30024813 ( click the link to review the publication )

Cancer Lett, 2018, 432:84-92

PubMed: 29859298 ( click the link to review the publication )

Cell Death Dis, 2017, 8(10):e3070

PubMed: 28981112 ( click the link to review the publication )

Theranostics, 2017, 7(17):4340-4349

PubMed: 29158830 ( click the link to review the publication )

Acta Pharmacol Sin, 2017, 38(7):1038-1047

PubMed: 28414200 ( click the link to review the publication )

Oncogene, 2013, 32(47):5377-87

PubMed: 23934192 ( click the link to review the publication )

Purity & Quality Control

Choose Selective PARP Inhibitors

Biological Activity

Description

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	Activity Description	PMID
HeLa cells	NWHudnhFTnWwY4Tpc44h[XO\|YYm=			MVfJcohq[mm2aX;uJI9nKFCDUmCgbY4hcHmmcn;n[Y4heGW{b4jp[IUucW6mdXPl[EBpfW2jbjDI[WxiKGOnbHzzJIF{e2W\|c3XkJIF{KGmwaHnibZRqd25iRF7BMYRidWGpZT3pcoR2[2WmIGDBVplt[XSrb36sJGVEPTB;MD6wNFQh\|ryP	NV3nc291RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm4O\|M6QDFpPkG5PFc{QThzPD;hQi=>
A549 cells	NFjxfVhEgXSxdH;4bYNqfHliYYPzZZk>		NYm4PWNQPS15IHThfZM>	NEj0PGlEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPTR7IHPlcIx{KHS{YX7z[oVkfGWmIIfpeIghSlKFQUKgd4hTVkFiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25iYX\0[ZIhPSC2bzC3JIRigXNiYomgR4VtdFSrdHXyMWJtfWViYYPzZZktKEOFNUC9NE4xOTFizszN	MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd4MUC5Okc,OjV5NkGwPVY9N2F-
MDA-MB-436 cells	Mlm0VJJwdGmoZYLheIlwdiCjc4PhfS=>		MX:2JIRigXN?	MlrKRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCPRFGtUWIuPDN4IHPlcIx{KGW6cILld5NqdmdiQmLDRVEhPTN7NjCrJFFIRkFibYX0ZY51KGGodHXyJFYh\GG7czDifUBk\WyuIITpeIVzNWKudXWgZZN{[XluIFPDOVA:OThibl2=	NF3NZYM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUi3N\|k5OSd-MUm4O\|M6QDF:L3G+
SUM1315MO2 cells	M4PNW2N6fG:2b4jpZ4l1gSCjc4PhfS=>		Ml61NVIh\GG7cx?=	NYCwUII2S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW1WPMUOxOW1QOiClZXzsd{Bk[XK{eXnu[{BDWkODMTDteZRidnRiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25iYX\0[ZIhOTJiZHH5d{BjgSCFZXzsWIl1\XJvQnz1[UBie3OjeTygR2M2OD1yLkCyJO69VQ>?	MnnaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5NkGwPVYoRjJ3N{[xNFk3RC:jPh?=
DoTc2-4510 cells	NUOxW\|NVS3m2b4TvfIlkcXS7IHHzd4F6		MX61MVch\GG7cx?=	NX:4eYtpS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hTG:WY{KtOFUyOCClZXzsd{Bk[XK{eXnu[{BDWkODMjDteZRidnRiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25iYX\0[ZIhPSC2bzC3JIRigXNiYomgR4VtdFSrdHXyMWJtfWViYYPzZZktKEOFNUC9NE4xOjNizszN	M1fYdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{[xNFk3Lz5{NUe2NVA6PjxxYU6=
SUM149PT cells	MW\DfZRwfG:6aXPpeJkh[XO\|YYm=		MVm1MVch\GG7cx?=	M3rjVWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNWVTF2OWDUJINmdGy\|IHPhdpJ6cW6pIFLSR2EyKG23dHHueEBie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJINmdGxicILvcIln\XKjdHnvckBi\nSncjC1JJRwKDdiZHH5d{BjgSCFZXzsWIl1\XJvQnz1[UBie3OjeTygR2M2OD1yLkCyOEDPxE1?	NUCyPVRTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3OlExQTZpPkK1O\|YyODl4PD;hQi=>
UWB1.289 cells	M1PINGN6fG:2b4jpZ4l1gSCjc4PhfS=>		NEC5R282NTdiZHH5dy=>	NYjpb5FIS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hXVeEMT6yPFkh[2WubIOgZ4FzenmrbnegRnJESTFibYX0ZY51KGG\|c3Xzd4VlKGG\|IHnubIljcXSrb36gc4Yh[2WubDDwdo9tcW[ncnH0bY9vKGGodHXyJFUhfG9iNzDkZZl{KGK7IFPlcIxVcXSncj3CcJVmKGG\|c3H5MEBESzVyPUCuNFU3KM7:TR?=	MmW0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5NkGwPVYoRjJ3N{[xNFk3RC:jPh?=
Capan1 cells	NVGwOJNqS3m2b4TvfIlkcXS7IHHzd4F6			MXLDfZRwfG:6aXPpeJkh[WejaX7zeEBDWkODMj3k[YZq[2mnboSgbJVu[W5iQ3HwZY4yKGOnbHzzMEBESzVyPUCuNFkh\|ryP	NFvlRXI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe2NVA6Pid-MkW3OlExQTZ:L3G+
Jurkat cells	NFLVd2NHfW6ldHnvckBie3OjeR?=			NXPwPYhDUW6qaXLpeIlwdiCxZjDQRXJROSCrbjDoeY1idiCMdYLrZZQh[2WubIOgZZN{\XO\|ZXSgZZMhemWmdXP0bY9vKG:oIHPlcIwhfmmjYnnsbZR6KGGodHXyJFk3KGi{czDifUBOXFNiYYPzZZkhcW5icILld4Vv[2Vib3[gNVAxKHWPIH;mJJRmdW:8b3zvcYll\SxiRVO1NF0xNjJizszN	NWXVS5BMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OVAyQTlpPkKzPFUxOTl7PD;hQi=>
BT20 cells	Mo\iR5l1d3SxeHnjbZR6KGG\|c3H5		M{P1e\|UuPyCmYYnz	MX;DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDCWFIxKGOnbHzzJIF{e2W\|c3XkJIF{KGmwaHnibZRqd25ib3[gZ4VtdCCycn;sbYZmemG2aX;uJIFnfGW{IEWgeI8hPyCmYYnzJIJ6KEOnbHzUbZRmei2EbIXlJIF{e2G7LDDDR\|UxRTJwMjFOwG0>	NF\4XII9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe2NVA6Pid-MkW3OlExQTZ:L3G+
Antiproliferative assay	MkDvTIVN[Q>?		M4TTfFch\GG7cx?=	MWXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IFLSR2EyKGSnZnnjbYVvfCCqdX3hckBJ\UyjIHPlcIx{KGGodHXyJFch\GG7czDifUBk\WyuIITpeIVzNWKudXWgZZN{[XluIFPDOVAhRSByLkCzN{DPxE1w	MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTh5M{m4NUc,OTl6N{O5PFE9N2F-
Function assay	M4r4[mhmVGF?			M4\jOGlvcGmkaYTpc44hd2ZiUFHSVEBqdiCqeXTyc4dmdiCyZYLvfIll\S2rbnT1Z4VlKGi3bXHuJGhmVGFiY3XscJMh[XO\|ZYPz[YQh[XNiaX7obYJqfGmxbjDEUmEu\GGvYXflMYlv\HWlZXSgVGFTgWyjdHnvckwhTUN7MDC9JFAvODR3IN88UU4>	MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTh5M{m4NUc,OTl6N{O5PFE9N2F-
Antiproliferative assay	NInVPXRE[XCjbkG=		NFu1Vm0yOyCmYYnz	M3\2c2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQ3HwZY4yKGOnbHzzJIV5eHKnc4PpcochSlKFQUKgOlE4PGSnbGSgcZV1[XSrb36gZY5lKGyxc4Ogc4Yhf2muZD30fZBmKGGubHXs[UBi\nSncjCxN{Bl[Xm\|IHL5JINmdGxidHn0[ZIu[my3ZTDhd5NigSxiQ1O1NEA:KDBwMEmg{txONg>?	NEjjVIY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUi3N\|k5OSd-MUm4O\|M6QDF:L3G+
Antiproliferative assay	NUfPOIs4UGWOYR?=		M1PmUFch\GG7cx?=	NVy4dlNRSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDI[WxiKGOnbHzzJIV5eHKnc4Ppcochf2muZDD0fZBmKEKUQ1GxJIFnfGW{IEeg[IF6eyCkeTDj[YxtKHSrdHXyMYJtfWViYYPzZZktKEOFNUCgQUAxNjh4IN88UU4>	M4jQd\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OEezPVgyLz5zOUi3N\|k5OTxxYU6=
Function assay	MYrKeZJs[XR?		NYjsXHlTQTZiaILz	NXLlNYhoUW6qaXLpeIlwdiCxZjDQRXJROSCrbjDoeY1idiCMdYLrZZQh[2WubIOgZZN{\XO\|ZXSgZZMhemWmdXP0bY9vKG:oIHPlcIwhfmmjYnnsbZR6KGGodHXyJFk3KGi{czDifUBOXFNiYYPzZZktKEWFNUCgQUA{OSEQvF2u	NHSzb\|I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i1NFE6QSd-MkO4OVAyQTl:L3G+
Function assay	NXW1NGFbS0GSQV6tNS=>			MnPpTY5pcWKrdHnvckBw\iCSQWLQJIlvKEKUQ1GyMYRm\mmlaXXueEBpfW2jbjDDRXBCVi1zIHPlcIx{KGG\|c3Xzd4VlKGG\|IHnubIljcXSrb36gc4YhcHmmcn;n[Y4heGW{b4jp[IUucW6mdXPl[EBRSVK7bHH0bY9vKGK7IHPlcIwu[mG\|ZXSgZZN{[XluIFnDOVAhRSByLkCwN\|Uh\|ryPLh?=	MmXvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5NkGwPVYoRjJ3N{[xNFk3RC:jPh?=
Function assay	M3LaTmhmVGF?			NIXEZVRKdmirYnn0bY9vKG:oIGDBVnAhcW5iaIXtZY4hUGWOYTDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGi7ZILv[4VvKHCncn;4bYRmNWmwZIXj[YQhWEGUeXzheIlwdiCkeTDj[YxtNWKjc3XkJIF{e2G7LDDFR\|UxKD1iMD6wNFQh\|ryPLh?=	NXjWWpZVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3OlExQTZpPkK1O\|YyODl4PD;hQi=>
Function assay	NIf4dJVCOjd6MB?=			M3mwSmlvcGmkaYTpc44hd2ZiUFHSVEBqdiCqdX3hckBCOjd6MDDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGi7ZILv[4VvKHCncn;4bYRmNWmwZIXj[YQhWEGUeXzheIlwdiCkeTDj[YxtNWKjc3XkJIF{e2G7LDDJR\|UxKD1iMD6wNFQh\|ryPLh?=	M2fyeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{[xNFk3Lz5{NUe2NVA6PjxxYU6=
Cytotoxicity assay	NGfxO\|dOTEFvTVKtOFM3			MX7DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvNEO2JINmdGy\|IHPhdpJ6cW6pIFLSR2EyKG23dHHueEBie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJINmdGxicILvcIln\XKjdHnvckwhS0N3MDC9JFAvODF6IN88UU4>	M{e0Z\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{[xNFk3Lz5{NUe2NVA6PjxxYU6=
Cytotoxicity assay	MUPI[Wxi		NX74eGpHPSC2bzC3JIRigXN?	M4nMNGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhmVGFiY3XscJMhfHKjboPm[YN1\WRid3n0bEBDWkODMTDzbHJPSSCjc4Pld5Nm\CCjczDy[YR2[3Srb36gc4Yh[2WubDD2bYFjcWyrdImgZYZ1\XJiNTD0c{A4KGSjeYOgZpkhS2WubGTpeIVzNUKudXWgZZN{[XluIFPDOVAhRSByLkCzOEDPxE1w	NI\jS3A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe2NVA6Pid-MkW3OlExQTZ:L3G+
Function assay	NUPUelNbUGWOYR?=			M17HZWlvcGmkaYTpc44hd2ZiUFHSVEBqdiCqdX3hckBJ\UyjIHPlcIx{KGG\|c3Xzd4VlKGG\|IHnubIljcXSrb36gc4YhcHmmcn;n[Y4heGW{b4jp[IUucW6mdXPl[EBRSVK7bHH0bY9vKGK7IHPlcIwu[mG\|ZXSgZZN{[XluIFnDPVAhRSByLkC0OkDPxE1w	MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd4MUC5Okc,OjV5NkGwPVY9N2F-
Function assay	M1fCUGNCWEGQLUG=			M{DXb2lvcGmkaYTpc44hd2ZiUFHSVEBqdiCEUlPBNk1l\W[rY3nlcpQhcHWvYX6gR2FRSU5vMTDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGi7ZILv[4VvKHCncn;4bYRmNWmwZIXj[YQhWEGUeXzheIlwdiCkeTDj[YxtNWKjc3XkJIF{e2G7LDDJR\|kxKD1iMD6wOUDPxE1w	NVTabVRiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3OlExQTZpPkK1O\|YyODl4PD;hQi=>
Function assay	NV3RdXlVSTJ5OEC=			NXXJTokxUW6qaXLpeIlwdiCxZjDQRXJRKGmwIHj1cYFvKEF{N{iwJINmdGy\|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiaInkdo9o\W5icHXyc5hq\GVvaX7keYNm\CCSQWL5cIF1cW:wIHL5JINmdGxvYnHz[YQh[XO\|YYmsJGlEQTBiPTCwMlA2OiEQvF2u	Mn7qQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5NkGwPVYoRjJ3N{[xNFk3RC:jPh?=
Cytotoxicity assay	NF\vR3VJ\Uyj		MX61JJRwKDdiZHH5dy=>	MV\DfZRwfG:6aXPpeJkh[WejaX7zeEB4cWymIIT5dIUhcHWvYX6gTIVN[SClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJINmdGxicILvcIln\XKjdHnvckBi\nSncjC1JJRwKDdiZHH5d{BjgSCFZXzsWIl1\XJvQnz1[UBie3OjeTygR2M2OCB;IECuPFUzKM7:TT6=	MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd4MUC5Okc,OjV5NkGwPVY9N2F-
Cytotoxicity assay	M2DDOXVYSjFwMki5		NUDwcFA3PSC2bzC3JIRigXN?	NXXoToQ{S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hXVeEMT6yPFkh[2WubIOg[ZhxemW\|c3nu[{BDWkODMTDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHPlcIwheHKxbHnm[ZJifGmxbjDh[pRmeiB3IITvJFch\GG7czDifUBE\WyuVHn0[ZIuSmy3ZTDhd5NigSxiQ1O1NEA:KDBwOUe1JO69VS5?	M{P4V\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{[xNFk3Lz5{NUe2NVA6PjxxYU6=
Cytotoxicity assay	NGnvUldCPTR7		NY\yTXFbPSC2bzC3JIRigXN?	NVjTOIU2S3m2b4TvfIlkcXS7IHHnZYlve3Rid3ns[EB1gXCnIHj1cYFvKEF3NEmgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25iYX\0[ZIhPSC2bzC3JIRigXNiYomgR4VtdFSrdHXyMWJtfWViYYPzZZktKEOFNUCgQUAyNjd4IN88UU4>	MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd4MUC5Okc,OjV5NkGwPVY9N2F-
Cytotoxicity assay	MV\DZZBidjF?			M17qfmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KEKUQ1GyMYRm\mmlaXXueEBpfW2jbjDDZZBidjFiY3XscJMtKEWFNUCgQUAxNjZ3IN88UU4>	Mn7XQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ4NUK3NVcoRjJ4NkWyO\|E4RC:jPh?=
Antitumor assay	Mm\sUWRCNU2ELUSzOi=>	NHzMcW02OCCvZz;r[y=>	NYrsSVVsOzNiZHH5dy=>	MU\BcpRqfHWvb4KgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCPRFGtUWIuPDN4IHPlcIx{KGW6cILld5NqdmdiQmLDRVEhPTN7NjCrJFFIRkFibYX0ZY51KHinbn;ndoFnfGWmIHnuJGNFOSCvb4Xz[UBie3Onc4Pl[EBieyC2dX3vdkBz\We{ZYPzbY9vKGG2IEWwJI1oN2upLDDwc{BjcWRiZn;yJFM{KGSjeYO=	NWfkcmJ3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm4O\|M6QDFpPkG5PFc{QThzPD;hQi=>
Antitumor assay	NF;q[lVOTEFvTVKtOFM3	MmX5NVAxKG2pL3vn	Mly4N\|Mh\GG7cx?=	NEntc5pCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvNEO2JINmdGy\|IHX4dJJme3OrbnegRnJESTFiNUO5OkAsKDGJPlGgcZV1[W62IIjlco9oemGodHXkJIlvKEOGMTDtc5V{\SCjc4Pld5Nm\CCjczD0eY1weiC{ZXfy[ZN{cW:wIHH0JFExOCCvZz;r[{wheG9icXSg[o9zKDN\|IHThfZM>	MoLKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl6N{O5PFEoRjF7OEezPVgyRC:jPh?=
Antitumor assay	NHPpXFhOTEFvTVKtOFM3	NUDEcVN3QDBibXevb4c>	M{jxRlEhfG9iMjD3[YVsew>?	MUPBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCPRFGtUWIuPDN4IHPlcIx{KGijcnLvdolv\yCEUlPBNUBufXSjboSgfIVvd2e{YX\0[YQhcW5iaX3teY5w[2:vcILvcYl{\WRibX;1d4Uh[XO\|ZYPz[YQh[XNidIXtc5Ih\3Kxd4ToJIlvcGmkaYTpc44h[XRiOECgcYcwc2duIIDvJJFlKG[xcjCxJJRwKDJid3Xlb5M>	MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd4MUC5Okc,OjV5NkGwPVY9N2F-
Antitumor assay	NEjlXo5OTEFvTVKtOFM3	MmTOPFAhdWdxa3e=	MVe0JJdm\Wu\|	NVPyUZNYSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUSzOkBk\WyuczDoZZJjd3KrbnegRnJESTFibYX0ZY51KHinbn;ndoFnfGWmIHnuJIludXWwb3PvcZBzd22rc3XkJI1wfXOnIHHzd4V{e2WmIHHzJINwdXCuZYTlJIFv\CC\|dYP0ZYlv\WRidIXtc5IhemWpcnXzd4lwdiCjdDC4NEBu\y:tZzygdI8heWRiZn;yJFQhf2Wna4O=	MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd4MUC5Okc,OjV5NkGwPVY9N2F-
Antitumor assay	NVKw[nF5VUSDLV3CMVQ{Pg>?	MnHoOVAhdWdxa3e=		NHfC[oNCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvNEO2JINmdGy\|IHjhdoJwemmwZzDCVmNCOSCvdYThcpQhgGWwb3fyZYZ1\WRiaX6gbY1ufW6xY3;tdJJwdWm\|ZXSgcY92e2ViYYPz[ZN{\WRiYYOgeJVud3JiZ4Lve5RpKGmwaHnibZRqd25iYYSgOVAhdWdxa3esJJBwKGGmbXnubZN1\XKnZDDkZYltgQ>?	NWK5[mZuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3OlExQTZpPkK1O\|YyODl4PD;hQi=>
Antitumor assay	M{j4WG1FSS2PQj20N\|Y>	MmPPPFAhdWdxa3e=	NXrKdZNYOyC5ZXXrdy=>	MlLRRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTR\|NjDj[YxteyCqYYLic5JqdmdiQmLDRVEhdXW2YX70JJhmdm:pcnHmeIVlKGmwIHntcZVvd2OxbYDyc41qe2WmIH3veZNmKGG\|c3Xzd4VlKGG\|IIT1cY9zKHOqcnnub4Fo\SCjdDC4NEBu\y:tZzygdI8heWRiZn;yJFMhf2Wna4O=	MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd4MUC5Okc,OjV5NkGwPVY9N2F-
qHTS assay	M2PhUHREOzJ?			NGnlOJhyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiVFOzNkBk\Wyucx?=	Ml\vQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
qHTS assay	MVXBOlc{			M4rFRZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCDNkezJINmdGy\|	NHnVOIQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
qHTS assay	M1;lSG5DOTZ2Mx?=			M3\6NJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQkG2OFMh[2WubIO=	MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
qHTS assay	MWrBOlc{			NYnIXXM6eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhSTZ5MzDj[Yxteyl?	MoewQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
qHTS assay	NXfTcI9qSlRvM{e=			NULs[\|hxeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhSlRvM{egZ4VtdHN?	Ml\pQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
qHTS assay	NGrNRphUUy2QLV3D			MUXxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?=	NWXVdmdLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
qHTS assay	NX3BS4M{VkJvRVLjNS=>			M3TlW5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQj3FRoMyKGOnbHzz	NHLHbHc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
qHTS assay	Mn[4UGFPNTV?			MYfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVEGQLUWgZ4VtdHN?	MmTCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
qHTS assay	NXq5XGl1W0tvTj3NRy=>			NGCwPGVyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBUUy2QLV3DJINmdGy\|	M1uzOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
qHTS assay	MWTUR\|Mz			NXvofZZ6eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhXEN\|MjDj[Yxtew>?	MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	c-PARP /c-caspase 3 / γ-H2AX; PubMed: 29158830 Theranostics 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 Gynecol Oncol 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]

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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]

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Animal Models: Female nude mice
Dosages: 25 mg/kg twice daily or 50 mg/kg once daily
Administration: oral administration
(Only for Reference)

References

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): 10% DMSO+40% PEG 300+5% Tween 80+ddH2O For best results, use promptly after mixing.	10mg/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 Download Niraparib (MK-4827) SDF

Molecular Weight	320.39
Formula	C₁₉H₂₀N₄O
CAS No.	1038915-60-4
Storage	3 years-20°C powder 2 years-80°C 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

Dosing volume per animal

Number of animals

Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)

% DMSO+ % + % Tween 80+ % ddH₂O

Calculate Reset

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.

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.

Bio Calculators

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)

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

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 )

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

The Serial Dilution Calculator Equation

Serial Dilutions
Concertration (start):
Dilution-folds:

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

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

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

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2021-01-06)

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
NCT04149145	Not yet recruiting	Drug: M4344+Niraparib	Ovarian Cancer Recurrent	University of Alabama at Birmingham	December 1 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.

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

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SCR7 is a specific DNA Ligase IV inhibitor, which blocks nonhomologous end-joining (NHEJ). It increases the efficiency of HDR-mediated genome editing up to 19-fold using CRISPR/Cas9 in mammalian cells and mouse embryos.
Olaparib (AZD2281)

Olaparib (AZD2281, KU0059436) is a selective inhibitor of PARP1/2 with IC50 of 5 nM/1 nM in cell-free assays, 300-times less effective against tankyrase-1. Olaparib induces significant autophagy that is associated with mitophagy in cells with BRCA mutations.

Features:A potent PARP inhibitor (currently in late stage clinical trials).
Veliparib (ABT-888)

Veliparib (ABT-888, NSC 737664) is a potent inhibitor of PARP1 and PARP2 with K_i of 5.2 nM and 2.9 nM in cell-free assays, respectively. It is inactive to SIRT2. Veliparib increases autophagy and apoptosis. Phase 3.

Features:Increases the efficacy of common cancer therapies such as radiation and alkylating agents.
Rucaparib (AG-014699) phosphate

Rucaparib (AG-014699, PF-01367338) is an inhibitor of PARP with K_i of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains. Phase 3.

Features:The first PARP inhibitor used in clinical trials combined with temozolomide.
Talazoparib (BMN 673)

Talazoparib (BMN 673, LT-673) is a novel PARP inhibitor with IC50 of 0.57 nM for PARP1 in a cell-free assay. It is also a potent inhibitor of PARP-2, but does not inhibit PARG and is highly sensitive to PTEN mutation. Phase 3.

Features:Most potent and selective PARPi reported thus far.
Iniparib (BSI-201)

Iniparib (BSI-201, NSC-746045, IND-71677) is a PARP1 inhibitor with demonstrated effectiveness in triple-negative breast cancer (TNBC). Phase 3.
PJ34 HCl

PJ34 HCl is the hydrochloride salt of PJ34, which is a PARP inhibitor with EC50 of 20 nM and is equally potent to PARP1/2.

Features:Water-soluble PARP1/2 inhibitor with >10,000-fold potentcy vs. 3-aminobenzamide (prototypical PARP inhibitor). Potential uses in cardiovascular diseases (stroke, cerebral ischemia, & myocardial ischemia).
AG-14361

AG14361 is a potent inhibitor of PARP1 with K_i of <5 nM in a cell-free assay. It is at least 1000-fold more potent than the benzamides.

Features:The 1st high-potency PARP-1 inhibitor with the specificity & in vivo activity to enhance chemotherapy and radiation therapy of human cancers.

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Niraparib (MK-4827)