Niraparib (MK-4827)

Name: Niraparib (MK-4827)
Brand: Selleck Chemicals
SKU: S2741
Rating: 5 (37 reviews)

For research use only.

Catalog No.S2741

37 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 37 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 )

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 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	MYfGeY5kfGmxbjDhd5NigQ>?			NF\iS2dKdmirYnn0bY9vKG:oIGDBVnAhcW5iaInkdo9o\W5icHXyc5hq\GVvaX7keYNm\CCqdX3hckBJ\UyjIHPlcIx{KGG\|c3Xzd4VlKGG\|IHnubIljcXSrb36gSG5CNWSjbXHn[U1qdmS3Y3XkJHBCWnmuYYTpc44tKEWFNUC9NE4xODRizszN	MmDjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl6N{O5PFEoRjF7OEezPVgyRC:jPh?=
A549 cells	M1jrUWN6fG:2b4jpZ4l1gSCjc4PhfS=>		MWO1MVch\GG7cx?=	NYjUZYw4S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTV2OTDj[YxteyC2cnHud4Zm[3SnZDD3bZRpKEKUQ1GyJJNpWk6DIHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiY3XscEBxem:uaX\ldoF1cW:wIHHmeIVzKDVidH:gO{Bl[Xm\|IHL5JGNmdGyWaYTldk1DdHWnIHHzd4F6NCCFQ{WwQVAvODFzIN88US=>	M{m2Z\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{[xNFk3Lz5{NUe2NVA6PjxxYU6=
MDA-MB-436 cells	M{DnS3Bzd2yrZnXyZZRqd25iYYPzZZk>		NInpbZk3KGSjeYO=	NVLQS5FISW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvNEO2JINmdGy\|IHX4dJJme3OrbnegRnJESTFiNUO5OkAsKDGJPlGgcZV1[W62IHHmeIVzKDZiZHH5d{BjgSClZXzsJJRqfGW{LXLseYUh[XO\|YYmsJGNEPTB;MUigcm0>	NYjjfI4yRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm4O\|M6QDFpPkG5PFc{QThzPD;hQi=>
SUM1315MO2 cells	MlnDR5l1d3SxeHnjbZR6KGG\|c3H5		Mnf5NVIh\GG7cx?=	NGrxTW9EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUXU1zM{G1UW8zKGOnbHzzJINienK7aX7nJGJTS0FzIH31eIFvfCCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdiCjZoTldkAyOiCmYYnzJIJ6KEOnbHzUbZRmei2EbIXlJIF{e2G7LDDDR\|UxRTBwMEKg{txO	MnTOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5NkGwPVYoRjJ3N{[xNFk3RC:jPh?=
DoTc2-4510 cells	Ml:zR5l1d3SxeHnjbZR6KGG\|c3H5		NGCwb3I2NTdiZHH5dy=>	MWDDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDEc3RkOi12NUGwJINmdGy\|IHPhdpJ6cW6pIFLSR2EzKG23dHHueEBie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJINmdGxicILvcIln\XKjdHnvckBi\nSncjC1JJRwKDdiZHH5d{BjgSCFZXzsWIl1\XJvQnz1[UBie3OjeTygR2M2OD1yLkCyN{DPxE1?	MkXSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5NkGwPVYoRjJ3N{[xNFk3RC:jPh?=
SUM149PT cells	MVfDfZRwfG:6aXPpeJkh[XO\|YYm=		Mn7GOU04KGSjeYO=	M1jEfmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNWVTF2OWDUJINmdGy\|IHPhdpJ6cW6pIFLSR2EyKG23dHHueEBie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJINmdGxicILvcIln\XKjdHnvckBi\nSncjC1JJRwKDdiZHH5d{BjgSCFZXzsWIl1\XJvQnz1[UBie3OjeTygR2M2OD1yLkCyOEDPxE1?	MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd4MUC5Okc,OjV5NkGwPVY9N2F-
UWB1.289 cells	MkL3R5l1d3SxeHnjbZR6KGG\|c3H5		NFTrXmQ2NTdiZHH5dy=>	MX7DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDVW2IyNjJ6OTDj[YxteyClYYLyfYlv\yCEUlPBNUBufXSjboSgZZN{\XO\|ZXSgZZMhcW6qaXLpeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36gZYZ1\XJiNTD0c{A4KGSjeYOgZpkhS2WubGTpeIVzNUKudXWgZZN{[XluIFPDOVA:OC5yNU[g{txO	Ml;XQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5NkGwPVYoRjJ3N{[xNFk3RC:jPh?=
Capan1 cells	NUPCb4w5S3m2b4TvfIlkcXS7IHHzd4F6			MYrDfZRwfG:6aXPpeJkh[WejaX7zeEBDWkODMj3k[YZq[2mnboSgbJVu[W5iQ3HwZY4yKGOnbHzzMEBESzVyPUCuNFkh\|ryP	MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd4MUC5Okc,OjV5NkGwPVY9N2F-
Jurkat cells	Ml\0SpVv[3Srb36gZZN{[Xl?			NH;MS4RKdmirYnn0bY9vKG:oIGDBVnAyKGmwIHj1cYFvKEq3cnvheEBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hd2ZiY3XscEB3cWGkaXzpeJkh[W[2ZYKgPVYhcHK\|IHL5JG1VWyCjc4PhfUBqdiCycnXz[Y5k\SCxZjCxNFAhfU1ib3[geIVud3qxbH;tbYRmNCCHQ{WwQVAvOiEQvF2=	NXy1d4h5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OVAyQTlpPkKzPFUxOTl7PD;hQi=>
BT20 cells	MlHSR5l1d3SxeHnjbZR6KGG\|c3H5		MVq1MVch\GG7cx?=	MXTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDCWFIxKGOnbHzzJIF{e2W\|c3XkJIF{KGmwaHnibZRqd25ib3[gZ4VtdCCycn;sbYZmemG2aX;uJIFnfGW{IEWgeI8hPyCmYYnzJIJ6KEOnbHzUbZRmei2EbIXlJIF{e2G7LDDDR\|UxRTJwMjFOwG0>	NYi3SHUzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3OlExQTZpPkK1O\|YyODl4PD;hQi=>
Antiproliferative assay	M1vpR2hmVGF?		NFzUTmU4KGSjeYO=	M4fhVWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgRnJESTFiZHXmbYNq\W62IHj1cYFvKEinTHGgZ4VtdHNiYX\0[ZIhPyCmYYnzJIJ6KGOnbHygeIl1\XJvYnz1[UBie3OjeTygR2M2OCB;IECuNFM{KM7:TT6=	NX;mfYYzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm4O\|M6QDFpPkG5PFc{QThzPD;hQi=>
Function assay	NETVboVJ\Uyj			NEj1W2NKdmirYnn0bY9vKG:oIGDBVnAhcW5iaInkdo9o\W5icHXyc5hq\GVvaX7keYNm\CCqdX3hckBJ\UyjIHPlcIx{KGG\|c3Xzd4VlKGG\|IHnubIljcXSrb36gSG5CNWSjbXHn[U1qdmS3Y3XkJHBCWnmuYYTpc44tKEWFOUCgQUAxNjB2NTFOwG0v	MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTh5M{m4NUc,OTl6N{O5PFE9N2F-
Antiproliferative assay	MVvDZZBidjF?		MmTDNVMh\GG7cx?=	NXnHbVQ5SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDDZZBidjFiY3XscJMh\XiycnXzd4lv\yCEUlPBNkA3OTd2ZHXsWEBufXSjdHnvckBidmRibH;zd{Bw\iC5aXzkMZR6eGViYXzs[YxmKGGodHXyJFE{KGSjeYOgZpkh[2WubDD0bZRmei2kbIXlJIF{e2G7LDDDR\|UxKD1iMD6wPUDPxE1w	NWT1VlY{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm4O\|M6QDFpPkG5PFc{QThzPD;hQi=>
Antiproliferative assay	MmS1TIVN[Q>?		M{S3fFch\GG7cx?=	MX3BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEinTHGgZ4VtdHNiZYjwdoV{e2mwZzD3bYxlKHS7cHWgRnJESTFiYX\0[ZIhPyCmYYnzJIJ6KGOnbHygeIl1\XJvYnz1[UBie3OjeTygR2M2OCB;IECuPFYh\|ryPLh?=	NV6yelg4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm4O\|M6QDFpPkG5PFc{QThzPD;hQi=>
Function assay	MULKeZJs[XR?		M1LZXlk3KGi{cx?=	NFfR[m5KdmirYnn0bY9vKG:oIGDBVnAyKGmwIHj1cYFvKEq3cnvheEBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hd2ZiY3XscEB3cWGkaXzpeJkh[W[2ZYKgPVYhcHK\|IHL5JG1VWyCjc4PhfUwhTUN3MDC9JFMyKM7:TT6=	NH7FbJQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i1NFE6QSd-MkO4OVAyQTl:L3G+
Function assay	MofPR2FRSU5vMR?=			NUTvUYpOUW6qaXLpeIlwdiCxZjDQRXJRKGmwIFLSR2EzNWSnZnnjbYVvfCCqdX3hckBESVCDTj2xJINmdGy\|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiaInkdo9o\W5icHXyc5hq\GVvaX7keYNm\CCSQWL5cIF1cW:wIHL5JINmdGxvYnHz[YQh[XO\|YYmsJGlEPTBiPTCwMlAxOzVizszNMi=>	MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd4MUC5Okc,OjV5NkGwPVY9N2F-
Function assay	M4GwdWhmVGF?			M1TuO2lvcGmkaYTpc44hd2ZiUFHSVEBqdiCqdX3hckBJ\UyjIHPlcIx{KGG\|c3Xzd4VlKGG\|IHnubIljcXSrb36gc4YhcHmmcn;n[Y4heGW{b4jp[IUucW6mdXPl[EBRSVK7bHH0bY9vKGK7IHPlcIwu[mG\|ZXSgZZN{[XluIFXDOVAhRSByLkCwOEDPxE1w	NHTVSYI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe2NVA6Pid-MkW3OlExQTZ:L3G+
Function assay	M3;oc2EzPzhy			NYHnUHFjUW6qaXLpeIlwdiCxZjDQRXJRKGmwIHj1cYFvKEF{N{iwJINmdGy\|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiaInkdo9o\W5icHXyc5hq\GVvaX7keYNm\CCSQWL5cIF1cW:wIHL5JINmdGxvYnHz[YQh[XO\|YYmsJGlEPTBiPTCwMlAxPCEQvF2u	NH7z[GE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe2NVA6Pid-MkW3OlExQTZ:L3G+
Cytotoxicity assay	M33VSW1FSS2PQj20N\|Y>			NXS5[lc5S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDLV3CMVQ{PiClZXzsd{Bk[XK{eXnu[{BDWkODMTDteZRidnRiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25uIFPDOVAhRSByLkCxPEDPxE1w	NYLUdJc4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3OlExQTZpPkK1O\|YyODl4PD;hQi=>
Cytotoxicity assay	NVzMOpBjUGWOYR?=		NXnJV4ZVPSC2bzC3JIRigXN?	NECwUZNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJ\UyjIHPlcIx{KHS{YX7z[oVkfGWmIIfpeIghSlKFQUGgd4hTVkFiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJI9nKGOnbHygeoli[mmuaYT5JIFnfGW{IEWgeI8hPyCmYYnzJIJ6KEOnbHzUbZRmei2EbIXlJIF{e2G7LDDDR\|UxKD1iMD6wN\|Qh\|ryPLh?=	MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd4MUC5Okc,OjV5NkGwPVY9N2F-
Function assay	MojBTIVN[Q>?			M2fEcGlvcGmkaYTpc44hd2ZiUFHSVEBqdiCqdX3hckBJ\UyjIHPlcIx{KGG\|c3Xzd4VlKGG\|IHnubIljcXSrb36gc4YhcHmmcn;n[Y4heGW{b4jp[IUucW6mdXPl[EBRSVK7bHH0bY9vKGK7IHPlcIwu[mG\|ZXSgZZN{[XluIFnDPVAhRSByLkC0OkDPxE1w	MnTZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5NkGwPVYoRjJ3N{[xNFk3RC:jPh?=
Function assay	M3G0U2NCWEGQLUG=			NFW4T4VKdmirYnn0bY9vKG:oIGDBVnAhcW5iQmLDRVIu\GWoaXPp[Y51KGi3bXHuJGNCWEGQLUGgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCqeXTyc4dmdiCyZYLvfIll\S2rbnT1Z4VlKFCDUonsZZRqd25iYomgZ4VtdC2kYYPl[EBie3OjeTygTWM6OCB;IECuNFUh\|ryPLh?=	NV\qbIZuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3OlExQTZpPkK1O\|YyODl4PD;hQi=>
Function assay	MnXmRVI4QDB?			MX;Jcohq[mm2aX;uJI9nKFCDUmCgbY4hcHWvYX6gRVI4QDBiY3XscJMh[XO\|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBpgWS{b3flckBx\XKxeHnk[U1qdmS3Y3XkJHBCWnmuYYTpc44h[nliY3XscE1j[XOnZDDhd5NigSxiSVO5NEA:KDBwMEWyJO69VS5?	M1nrSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{[xNFk3Lz5{NUe2NVA6PjxxYU6=
Cytotoxicity assay	NXuxRmpJUGWOYR?=		M330ZlUhfG9iNzDkZZl{	Mlv1R5l1d3SxeHnjbZR6KGGpYXnud5Qhf2muZDD0fZBmKGi3bXHuJGhmVGFiY3XscJMh[XO\|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBk\WyuIIDyc4xq\mW{YYTpc44h[W[2ZYKgOUB1dyB5IHThfZMh[nliQ3XscHRqfGW{LVLseYUh[XO\|YYmsJGNEPTBiPTCwMlg2OiEQvF2u	MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd4MUC5Okc,OjV5NkGwPVY9N2F-
Cytotoxicity assay	M4L3TXVYSjFwMki5		MoizOUB1dyB5IHThfZM>	MYrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDVW2IyNjJ6OTDj[YxteyCneIDy[ZN{cW6pIFLSR2EyKGG\|c3Xzd4VlKGG\|IHnubIljcXSrb36gc4Yh[2WubDDwdo9tcW[ncnH0bY9vKGGodHXyJFUhfG9iNzDkZZl{KGK7IFPlcIxVcXSncj3CcJVmKGG\|c3H5MEBESzVyIE2gNE46PzVizszNMi=>	M2PZTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{[xNFk3Lz5{NUe2NVA6PjxxYU6=
Cytotoxicity assay	MlvPRVU1QQ>?		M1jXb\|UhfG9iNzDkZZl{	NIC4cYREgXSxdH;4bYNqfHliYXfhbY5{fCC5aXzkJJR6eGViaIXtZY4hSTV2OTDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdiCjZoTldkA2KHSxIEeg[IF6eyCkeTDD[YxtXGm2ZYKtRox2\SCjc4PhfUwhS0N3MDC9JFEvPzZizszNMi=>	MnywQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5NkGwPVYoRjJ3N{[xNFk3RC:jPh?=
Cytotoxicity assay	NXrHSo5vS2GyYX6x			MkjWR5l1d3SxeHnjbZR6KGGpYXnud5QhSlKFQUKt[IVncWOrZX70JIh2dWGwIFPhdIFvOSClZXzsd{whTUN3MDC9JFAvPjVizszNMi=>	MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjZ3MkexO{c,OjZ4NUK3NVc9N2F-
Antitumor assay	NX;MRnlMVUSDLV3CMVQ{Pg>?	NFvHPGk2OCCvZz;r[y=>	M4i4eVM{KGSjeYO=	NI[wdXVCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvNEO2JINmdGy\|IHX4dJJme3OrbnegRnJESTFiNUO5OkAsKDGJPlGgcZV1[W62IIjlco9oemGodHXkJIlvKEOGMTDtc5V{\SCjc4Pld5Nm\CCjczD0eY1weiC{ZXfy[ZN{cW:wIHH0JFUxKG2pL3vnMEBxdyCkaXSg[o9zKDN\|IHThfZM>	M2\tNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OEezPVgyLz5zOUi3N\|k5OTxxYU6=
Antitumor assay	MUPNSGEuVUJvNEO2	M{LFWVExOCCvZz;r[y=>	MmXzN\|Mh\GG7cx?=	NYPCV2ZQSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUSzOkBk\WyuczDlfJBz\XO\|aX7nJGJTS0FzIEWzPVYhMyBzR{7BJI12fGGwdDD4[Y5w\3KjZoTl[EBqdiCFREGgcY92e2ViYYPz[ZN{\WRiYYOgeJVud3JicnXndoV{e2mxbjDheEAyODBibXevb4ctKHCxIIHkJIZweiB\|MzDkZZl{	Mn3BQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl6N{O5PFEoRjF7OEezPVgyRC:jPh?=
Antitumor assay	M4m2OG1FSS2PQj20N\|Y>	MV[4NEBu\y:tZx?=	M3HEXFEhfG9iMjD3[YVsew>?	M3fIXGFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi12M{[gZ4VtdHNiaHHyZo9zcW6pIFLSR2EyKG23dHHueEB5\W6xZ4Lh[pRm\CCrbjDpcY12dm:lb33wdo9ucXOnZDDtc5V{\SCjc4Pld5Nm\CCjczD0eY1weiCpcn;3eIghcW6qaXLpeIlwdiCjdDC4NEBu\y:tZzygdI8heWRiZn;yJFEhfG9iMjD3[YVsew>?	MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd4MUC5Okc,OjV5NkGwPVY9N2F-
Antitumor assay	MUHNSGEuVUJvNEO2	MlfhPFAhdWdxa3e=	NGWzUXY1KHenZXvz	NYr0Rm5nSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUSzOkBk\WyuczDoZZJjd3KrbnegRnJESTFibYX0ZY51KHinbn;ndoFnfGWmIHnuJIludXWwb3PvcZBzd22rc3XkJI1wfXOnIHHzd4V{e2WmIHHzJINwdXCuZYTlJIFv\CC\|dYP0ZYlv\WRidIXtc5IhemWpcnXzd4lwdiCjdDC4NEBu\y:tZzygdI8heWRiZn;yJFQhf2Wna4O=	MmjYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5NkGwPVYoRjJ3N{[xNFk3RC:jPh?=
Antitumor assay	MorMUWRCNU2ELUSzOi=>	NFW0XGc2OCCvZz;r[y=>		NUH4U2RLSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUSzOkBk\WyuczDoZZJjd3KrbnegRnJESTFibYX0ZY51KHinbn;ndoFnfGWmIHnuJIludXWwb3PvcZBzd22rc3XkJI1wfXOnIHHzd4V{e2WmIHHzJJR2dW:{IHfyc5d1cCCrbnjpZol1cW:wIHH0JFUxKG2pL3vnMEBxdyCjZH3pcol{fGW{ZXSg[IFqdHl?	NYLaWo4zRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3OlExQTZpPkK1O\|YyODl4PD;hQi=>
Antitumor assay	M4XQVW1FSS2PQj20N\|Y>	M2n1S\|gxKG2pL3vn	Mn7vN{B4\WWtcx?=	NVvtTYs2SW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUSzOkBk\WyuczDoZZJjd3KrbnegRnJESTFibYX0ZY51KHinbn;ndoFnfGWmIHnuJIludXWwb3PvcZBzd22rc3XkJI1wfXOnIHHzd4V{e2WmIHHzJJR2dW:{IIPodolvc2GpZTDheEA5OCCvZz;r[{wheG9icXSg[o9zKDNid3Xlb5M>	MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd4MUC5Okc,OjV5NkGwPVY9N2F-
qHTS assay	MWfUR\|Mz			MkLYdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKFSFM{KgZ4VtdHN?	NHWwZZU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
qHTS assay	MYTBOlc{			MkHFdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKEF4N{OgZ4VtdHN?	MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
qHTS assay	M4CyR25DOTZ2Mx?=			NX\aU2xmeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IF7CNVY1OyClZXzsdy=>	MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
qHTS assay	NFr5c\|NCPjd\|			MVjxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDBOlc{KGOnbHzzLS=>	NY\DcndMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
qHTS assay	NHLWNZlDXC1\|Nx?=			MlfadWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgRnQuOzdiY3XscJM>	NXPFVoI1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
qHTS assay	MkHKV2suVi2PQx?=			NUj5XGlOeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IGPLMW4uVUNiY3XscJM>	MkTZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
qHTS assay	NHPwOWtPSi2HQnOx			MknhdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKE6ELVXCZ\|Eh[2WubIO=	Mk\iQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
qHTS assay	MWXMRW4uPQ>?			Ml6zdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKEyDTj21JINmdGy\|	NX\sVYJLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
qHTS assay	MlnSV2suVi2PQx?=			M2Lp[ZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHNMNU5vTVOgZ4VtdHN?	Ml3qQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
qHTS assay	NUG4fVBEXEN\|Mh?=			Ml\rdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgWGM{OiClZXzsdy=>	MXG8ZUB1[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 2020-01-06)

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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NU1025 (NSC 696807) is a potent PARP inhibitor with IC50 of 400 nM.
SCR7 ^New

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)