Rucaparib (AG-014699) phosphate

Name: Rucaparib (AG-014699) phosphate
Brand: Selleck Chemicals
SKU: S1098
Rating: 5 (91 reviews)

For research use only.

Catalog No.S1098 Synonyms: PF-01367338

91 publications

Rucaparib (AG-014699) phosphate Chemical Structure

CAS No. 459868-92-9

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.

Selleck's Rucaparib (AG-014699) phosphate has been cited by 91 publications

Cancer Cell, 2020, 37(2):157-167

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Nature, 2015, 12;518(7538):258-62.

PubMed: 25642963 ( click the link to review the publication )

Cancer Discov, 2021, 11(2):362-383

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Cell Death Differ, 2021, 10.1038/s41418-020-00733-4

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Oncol Lett, 2021, 21(2):139

PubMed: 33552258 ( click the link to review the publication )

J Steroid Biochem Mol Biol, 2021, 209:105853

PubMed: 33617965 ( click the link to review the publication )

Nat Commun, 2021, 12(1):736

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Cell Rep, 2020, 33(2):108240

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Elife, 2020, 9e60637

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EBioMedicine, 2020, 59:102971

PubMed: 32846370 ( click the link to review the publication )

Cancers (Basel), 2020, 4;12(4)

PubMed: 32260355 ( click the link to review the publication )

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

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

Cells, 2020, 28;9(5)

PubMed: 32354165 ( click the link to review the publication )

Am J Cancer Res, 2020, 10(8):2649-2676

PubMed: 32905466 ( 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-19-0507

PubMed: 32229503 ( click the link to review the publication )

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

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

J Biol Chem, 2020, jbc.RA120.015138

PubMed: 33051211 ( click the link to review the publication )

Genes (Basel), 2020, 25;11(4):347

PubMed: 32218170 ( click the link to review the publication )

Cancer Res Treat, 2020, 10.4143/crt.2020.1013

PubMed: 33332934 ( click the link to review the publication )

Biochemistry, 2020, 10.1021/acs.biochem.0c00256

PubMed: 32357296 ( click the link to review the publication )

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

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

Am J Cancer Res, 2020, 10(6):1900-1918

PubMed: 32642299 ( click the link to review the publication )

Cancer Res, 2020, 10.1158

PubMed: 32127357 ( click the link to review the publication )
Commun Biol, 2020, 3(1):388

PubMed: 32681145 ( click the link to review the publication )

NAR Cancer, 2020, 2(3):zcaa013

PubMed: 32776008 ( click the link to review the publication )

Proc Natl Acad Sci U S A, 2020, 201919445

PubMed: 32826329 ( click the link to review the publication )

bioRxiv, 2020, 30;2020.4.17.47480

PubMed: 32511303 ( click the link to review the publication )

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

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

Cell Rep, 2020, 32(5):107985

PubMed: 32755579 ( click the link to review the publication )

Nat Microbiol, 2019, 4(11):1872-1884

PubMed: 30988430 ( click the link to review the publication )

Nat Commun, 2019, 10(1):2910

PubMed: 31266951 ( click the link to review the publication )

J Clin Invest, 2019, 129(3):1211-1228

PubMed: 30589644 ( click the link to review the publication )

Nat Chem Biol, 2019, 15(12):1223-1231

PubMed: 31659317 ( click the link to review the publication )

Nucleic Acids Res, 2019, 47(11):5634-5647

PubMed: 31006810 ( 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 )

EMBO Rep, 2019, 20(5)

PubMed: 30940648 ( 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-17-0256

PubMed: 31575654 ( 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 )

Mol Cancer Res, 2019, 17(2):431-445

PubMed: 30401718 ( click the link to review the publication )

Mol Cancer Res, 2019, 17(2):409-419

PubMed: 30429212 ( click the link to review the publication )

Biochem Pharmacol, 2019, 10.1016/j.bcp.2019.05.007

PubMed: 31075269 ( click the link to review the publication )

Mol Carcinog, 2019, 58(10):1770-1782

PubMed: 31219654 ( 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 )

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, 10.1158/1078-0432.CCR-17-1118

PubMed: 30108102 ( click the link to review the publication )
Mol Oncol, 2018, 12(4):561-576

PubMed: 29465803 ( click the link to review the publication )

Gynecol Oncol, 2018, 149(3):575-584

PubMed: 29567272 ( click the link to review the publication )

J Immunol, 2018,

PubMed: 29445007 ( click the link to review the publication )

Biochem Pharmacol, 2018, 10.1016/j.bcp.2018.10.011

PubMed: 30342021 ( click the link to review the publication )

Cancer Manag Res, 2018, 10:1439-1448

PubMed: 29922088 ( click the link to review the publication )

SLAS Discov, 2018, 23(6):545-553

PubMed: 29676938 ( click the link to review the publication )

Oncotarget, 2018, 9(53):30115-30127

PubMed: 30046392 ( click the link to review the publication )

Nat Cell Biol, 2017, 19(11):1371-1378

PubMed: 29035360 ( click the link to review the publication )

Mol Cell, 2017, 66(4):503-516

PubMed: 28525742 ( click the link to review the publication )

Clin Cancer Res, 2017, 23(14):3711-3720

PubMed: 28167507 ( click the link to review the publication )

Mol Med Rep, 2017, 16(1):208-214

PubMed: 28498459 ( click the link to review the publication )

Nucleic Acids Res, 2017, 45(19):11174-11192

PubMed: 28977496 ( click the link to review the publication )

Oncotarget, 2017, 8(31):50376-50392

PubMed: 28881569 ( click the link to review the publication )

Sci Transl Med, 2016, 8(333):333ra48

PubMed: 27053772 ( click the link to review the publication )

Cancer Res, 2016, 76(9):2778-90

PubMed: 27197267 ( click the link to review the publication )

Cell Rep, 2016, 15(11):2488-99

PubMed: 27264184 ( click the link to review the publication )

PLoS Genet, 2016, 12(12):e1006465

PubMed: 27906959 ( click the link to review the publication )

DNA Repair , 2016, 45:44-55

PubMed: 27334689 ( click the link to review the publication )

Neuropharmacology, 2016, 110(Pt A):287-296

PubMed: 27497606 ( click the link to review the publication )

BMC Cancer, 2016, 16:621

PubMed: 27515310 ( click the link to review the publication )

Parasit Vectors, 2016, 9:173

PubMed: 27007296 ( click the link to review the publication )

J Hepatol, 2015, 63(5):1164-72

PubMed: 26095183 ( click the link to review the publication )

Cancer Discov, 2015, 5(7):752-67

PubMed: 26069190 ( click the link to review the publication )

J Vet Emerg Crit Care (San Antonio), 2015, 25(4):528-37

PubMed: 26040949 ( click the link to review the publication )
Nat Commun, 2014, 5:3361

PubMed: 24553445 ( click the link to review the publication )

Eur J Cancer, 2014, 50(15):2725-34

PubMed: 25128455 ( click the link to review the publication )

Acta Neuropathol Commun, 2014, 10.1186/2051-5960-2-57

PubMed: 24887326 ( click the link to review the publication )

Mol Cancer Ther, 2014, 13(3):724-32

PubMed: 24356817 ( click the link to review the publication )

Oral Oncol, 2014, 50(9):825-31

PubMed: 25017803 ( click the link to review the publication )

J Biomol Screen, 2014, 19(10):1372-82

PubMed: 25117203 ( click the link to review the publication )

Oncotarget, 2014, 5(10):3023-8

PubMed: 24632590 ( click the link to review the publication )

Urol Oncol, 2014, 32(5):720-6

PubMed: 24837011 ( click the link to review the publication )

Clin Cancer Res, 2013, 19(18):5003-15

PubMed: 23881923 ( click the link to review the publication )

J Nucl Med, 2013, 54(6):913-21

PubMed: 23564760 ( click the link to review the publication )

Mol Cancer Res, 2013, 11(10):1179-92

PubMed: 23913164 ( click the link to review the publication )

J Viral Hepat, 2013, 20(9):658-65

PubMed: 23910651 ( click the link to review the publication )

Int J Radiat Oncol Biol Phys, 2013, 88(2):385-94

PubMed: 24411611 ( click the link to review the publication )

EJNMMI Res, 2013, 4(1):2

PubMed: 24387284 ( click the link to review the publication )

Tumour Biol, 2013, 35(5):4469-77

PubMed: 24420152 ( click the link to review the publication )

Nat Neurosci, 2013, 16(10):1392-400

PubMed: 23974709 ( click the link to review the publication )

Cancer Lett, 2012, 319(2):232-41

PubMed: 22266096 ( click the link to review the publication )

Nucl Med Commun, 2011, 32(11):1046-51

PubMed: 23038248 ( click the link to review the publication )

Nature, 2011, 470(7334):419-23

PubMed: 21278727 ( click the link to review the publication )

Purity & Quality Control

Choose Selective PARP Inhibitors

Biological Activity

Description

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.

Targets

PARP ^[1]
(Cell-free assay)

1.4 nM(Ki)

In vitro

Rucaparib is a potent inhibitor of purified full-length human PARP-1 and shows higher inhibition of cellular PARP in LoVo and SW620 cells. Besides, Rucaparib binds detectably to eight other PARP domains, including PARP2, 3, 4, 10, 15, 16, TNKS1 and TNKS2. ^[1] ^[2] The radio-sensitization by Rucaparib is due to downstream inhibition of activation of NF-κB, and is independent of SSB repair inhibition. Rucaparib could target NF-κB activated by DNA damage and overcome toxicity observed with classical NF-κB inhibitors without compromising other vital inflammatory functions. ^[3] Rucaparib inhibits PARP-1 activity by 97.1% at a concentration of 1 μM in permeabilised D283Med cells. ^[4]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
BT-474	NHi3XFZHfW6ldHnvckBCe3OjeR?=	NIqzXG8xNjFxMT:1NFAwOTByMDDuUS=>			NXXNcXV2cW6qaXLpeJMhWEGUUDDhZ5Rqfmm2eTDheEB{fGG{dHnu[{Bkd26lZYLueJJifGmxbjDv[kA2ODBibl2=	MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTF{OES1OUc,OjVzMki0OVU9N2F-
BT474	M3m4fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	Mnv0OVAxKG6P	M3rvdlEx6oDVMUZCpIQ>		NGDnc4Zz\WS3Y3XzJINmdGxiZ4Lve5RpKGmwIITo[UBnd3W{IHzpcoV{KGGwZDDzbYdvcW[rY3HueIx6	NHH1[JY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUGyPFQ2PSd-MkWxNlg1PTV:L3G+
SKBR3	M1f4Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M{HIW\|UxOCCwTR?=	M4jrUVEx6oDVMUZCpIQ>		NEXTeJBz\WS3Y3XzJINmdGxiZ4Lve5RpKGmwIITo[UBnd3W{IHzpcoV{KGGwZDDzbYdvcW[rY3HueIx6	M{HKUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MUK4OFU2Lz5{NUGyPFQ2PTxxYU6=
AU565	NFPsN4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M17ZelUxOCCwTR?=	Mn7ENVDjiJNzNdMg[C=>		M1[wb5Jm\HWlZYOgZ4VtdCCpcn;3eIghcW5idHjlJIZwfXJibHnu[ZMh[W6mIIPp[45q\mmlYX70cJk>	NXfzb\|VLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWxNlg1PTVpPkK1NVI5PDV3PD;hQi=>
EFM192A	MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MUW1NFAhdk1?	NGriSoQyOOLCk{G1xsBl		NFL2VoVz\WS3Y3XzJINmdGxiZ4Lve5RpKGmwIITo[UBnd3W{IHzpcoV{KGGwZDDzbYdvcW[rY3HueIx6	MkXmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVzMki0OVUoRjJ3MUK4OFU2RC:jPh?=
MDA-MB-231	M1zxTmZ2dmO2aX;uJGF{e2G7	MmPpNVAwOjBxNECg{txO	NIPVTHAzPCCq		MljDbY5kemWjc3XzJJAuSUuWIHzleoVteyCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>?	MlfjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2MkCxOVIoRjJ2NEKwNVUzRC:jPh?=
MDA-MB-231	NYHi[GlDS2WubDDWbYFjcWyrdImgRZN{[Xl?	NX3GVoJIOC5zLUSwJO69VQ>?	NEXCc\|czPCCq		NFfHU5RKSzVy4pEJQgKBkTF5Lke3xsDPxE1?	NEH5bGU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESyNFE2Oid-MkS0NlAyPTJ:L3G+
MDA-MB-231	MXfBdI9xfG:\|aYOgRZN{[Xl?	M{TCPVExNzJyL{SwJO69VQ>?	MWCyOEBp		MULpcoR2[2W\|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7	M3KzUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEKwNVUzLz5{NESyNFE2OjxxYU6=
MDA-MB-231	NIHJZZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NF3zVVUyOC9{MD:0NEDPxE1?	NV20WFl1OjRiaB?=		NHXUdVZjdG:la4OgZ4VtdCCleXPs[UBxem:pcnXzd4lwdiCrbjDHNk9OKHCqYYPl	Moj3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2MkCxOVIoRjJ2NEKwNVUzRC:jPh?=
H460	NXzTOZF1T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	Mnm0OFAxKG6P	NULx[I5uOjUEoHi=		MkLtbY5kemWjc3XzJINmdGy3bHHyJJJi\Gmxc3Xud4l1cX[rdIm=	NIXtSVk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESxNVYyOSd-MkS0NVE3OTF:L3G+
A549	M13IVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M1jLXlQxOCCwTR?=	NH7JbHQzPMLiaB?=		NWntcYJPcW6lcnXhd4V{KGOnbHz1cIFzKHKjZHnvd4Vve2m2aY\peJk>	MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDRzMU[xNUc,OjR2MUG2NVE9N2F-
DT40	MlHlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MUnJR\|UxRTJzIH7N	Mkf5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR\|NU[4NVMoRjJ2M{W2PFE{RC:jPh?=
DU145	NIPwVIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				MUjJR\|UxRTF6IH7N	NUi2WplKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOVY5OTNpPkK0N\|U3QDF\|PD;hQi=>
COLO704	NYPK[5l[T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NVfHSXhTUUN3ME2yMlUzKMLzIECuOlch\|ryP	MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd{OUSwNkc,OjN5Mkm0NFI9N2F-
OVMANAb	MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				NEXKPJhKSzVyPUKuOVghyrFiMD6zPEDPxE1?	NHHPZVg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{eyPVQxOid-MkO3Nlk1ODJ:L3G+
OV177	MnPSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MYnJR\|UxRTJwN{igxtEhOC55MTFOwG0>	NX;2Xo9WRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3Nlk1ODJpPkKzO\|I6PDB{PD;hQi=>
OAW28	MkDDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MnLsTWM2OD1\|Lk[xJOKyKDBwMkig{txO	MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd{OUSwNkc,OjN5Mkm0NFI9N2F-
OVSAHO	MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				MUXJR\|UxRTNwNkSgxtEhOC5\|MzFOwG0>	NITq[2U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{eyPVQxOid-MkO3Nlk1ODJ:L3G+
OVKATE	NV7zZVNJT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NFSwOmRKSzVyPUOuOlQhyrFiMT63PUDPxE1?	NXTOfoNxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3Nlk1ODJpPkKzO\|I6PDB{PD;hQi=>
OVCAR3	MnfPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MUXJR\|UxRTNwN{SgxtEhOC52MDFOwG0>	M2PmNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|N{K5OFAzLz5{M{eyPVQxOjxxYU6=
PEO14	M17FT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NYP3dFdSUUN3ME2zMlg1KMLzIECuO\|Yh\|ryP	M1jndlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|N{K5OFAzLz5{M{eyPVQxOjxxYU6=
A2780	MnnnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MkjtTWM2OD1\|Lkm0JOKyKDBwMkWg{txO	NVzLUoNZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3Nlk1ODJpPkKzO\|I6PDB{PD;hQi=>
OVTOKO	NYX6SIUyT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				MYDJR\|UxRTRwMUSgxtEhOS53MzFOwG0>	M{GwNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|N{K5OFAzLz5{M{eyPVQxOjxxYU6=
KURAMOCHIb	MojIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MYHJR\|UxRTRwM{SgxtEhOC5{OTFOwG0>	MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd{OUSwNkc,OjN5Mkm0NFI9N2F-
TOV21G	NHThPHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NF;KOmhKSzVyPUWuNFchyrFiMT6zNEDPxE1?	MnriQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5Mkm0NFIoRjJ\|N{K5OFAzRC:jPh?=
OVISE	MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				NEH5UVJKSzVyPUWuOlghyrFiMD6yN{DPxE1?	NFPD[\|k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{eyPVQxOid-MkO3Nlk1ODJ:L3G+
KK	M2jk[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				M2WwPGlEPTB;Nj6xOUDDuSBzLkSyJO69VQ>?	MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd{OUSwNkc,OjN5Mkm0NFI9N2F-
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MDA-MB-231	M3XFbmNmdGxiVnnhZoltcXS7IFHzd4F6				MYDJR\|UxRTF\|IN88US=>	MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ5OEG2NUc,OjJ4N{ixOlE9N2F-
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Rosetta2 (DE3)	M1XWZ2Z2dmO2aX;uJIF{e2G7				M3XYT2lvcGmkaYTpc44hd2ZiaIXtZY4hPniqaYOteIFo\2WmIFHSWGQ2KChzMEOwJJRwKDF\|MUepJIV5eHKnc4Pl[EBqdiCHc3Po[ZJq[2irYTDjc4xqKFKxc3X0eIEzKCiGRUOpJINmdGy\|IIXzbY5oKE6DRDugZZMhe3Wkc4TyZZRmKGK7IH\seY9z\XOlZX7j[UBie3OjeTygTWM2OCB;IECuNFI2KM7:TT6=	MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyMEe3NEc,OjR7MEC3O\|A9N2F-
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MDA-MB-436	M2XtTmFvfGmlYX7j[ZIh[XO\|YYm=		M3raXlk3KGi{cx?=		MUjBcpRq[2GwY3XyJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQmLDRVEu\GWoaXPp[Y51KE2GQT3NRk01OzZiY3XscJMh[W[2ZYKgPVYhcHK\|IHL5JG1VXCCjc4PhfUwhS0N3MDC9JFMh\|ryPLh?=	M{fmdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{SyPFY5Lz5{NkO0Nlg3QDxxYU6=
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MCF7	NVvRNopFSW62aXPhcoNmeiCjc4PhfS=>		M4HXVVk3KGi{cx?=		M3u0PGFvfGmlYX7j[ZIh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIFnfGW{IEm2JIhzeyCkeTDNWHQh[XO\|YYmsJGNEPTBiPTCxPU41PyEQvF2u	NIHjZZo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkO0Nlg3QCd-Mk[zOFI5Pjh:L3G+
A673	MVTxTHRUKGG\|c3H5				NEPobIVyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQU[3N{Bk\Wyucx?=	M4nJR\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
A673	M2f1bJFJXFNiYYPzZZk>				NH70[ppyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBCPjd\|IHPlcIx{MQ>?	Mo\yQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
Rh41	NUTFfo9meUiWUzDhd5NigQ>?				MoTqdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgVog1OSClZXzsdy=>	MlvWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
SK-N-MC	NVXsdXlXeUiWUzDhd5NigQ>?				M2rOV5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHNMNU5vTVOgZ4VtdHN?	MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
TC32	MYrxTHRUKGG\|c3H5				MlPzdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgWGM{OiClZXzsdy=>	NHL3NmU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	PAR; PubMed: 27960087 Cancer Cell MCF-7 cells were pretreated ± Rucaparib (15 µM, 2 hr), then ± Rucaparib (15 µM) or two different doses of β-lap (2.0 or 5.0 µM) for 2 hr. Levels of PAR (PARP hyperactivation) formation were assessed with α-tubulin as loading controls. BRCA1; PubMed: 24085845 Proc Natl Acad Sci U S A MCF7 cells, MDA-MB-436 parental cells and resistant clones RR-1, RR-5, and RR-6 were treated with DMSO (−) or 1 µM rucaparib (+) for 24 h, and BRCA1 protein levels were assessed by using BRCA1 N- or C-terminal-specific antibodies by Western blot.	27960087 24085845
Growth inhibition assay	Cell viability; PubMed: 31119062 Adv Wound Care (New Rochelle) The effect of rucaparib on proliferation of keloid fibroblasts. (A) Keloid cell growth following treatment with rucaparib at various concentration (0, 2, 10, 20 μM) was evaluated by MTT assays. Data are expression as mean standard deviation of percent changes of triplicate optical densities. (B) Rucaparib (20 μM) significantly decreased proliferation of keloid fibroblasts. The combination of rucaparib (20 μM) and triamcinolone (50 μM) showed additive suppressive effect on keloid fibroblasts as compared with rucaparib single therapy. Data are expression as mean standard deviation of percent changes of triplicate optical densities. MTT, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide.	31119062
Immunofluorescence	α-tubulin; PubMed: 30589644 J Clin Invest Representative immunofluorescence images of DMSO-, rucaparib- (Ruca-), and Ola-exposed A549-ERCC1(WT/WT) and A549-ERCC1(–/–) cells. Cells were exposed to 15 μM Ruca or 40 μM Ola during 72 hours. White arrows, CCFs; yellow arrows, micronuclei. Scale bar: 20 μm. PAR; PubMed: 27515310 BMC Cancer Cells were treated with 20 mM hydrogen peroxide (H2O2) in order to stimulate PARP-1 activity in the presence or absence of the PARP-1 inhibitors rucaparib and olaparib. Poly(ADP-ribose) (PAR) chain synthesis was detected using an anti-PAR monoclonal Alexa Fluor 488-conjugated antibody (green). The nucleus was visualised using the nuclear counterstain DAPI (blue). Representative images obtained from the analysis of anti-PAR staining of SK-N-BE(2c) cells are shown. γH2AX; PubMed: 23565244 PLoS One γH2AX foci was determined by immunofluoresecence microscopy at 24 h following combined treatment with radiation and rucaparib in PC3 and LNCaP cells. 53BP1; PubMed: 23565244 PLoS One 53BP1 foci was determined by immunofluoresecence microscopy at 24 h following combined treatment with radiation and rucaparib in PC3 and LNCaP cells.	30589644 27515310 23565244

In vivo

Rucaparib is not toxic but significantly enhances temozolomide-induced TGD in the DNA repair protein-competent D384Med xenografts. Pharmacokinetics studies also show that Rucaparib is detected in the brain tissue, which indicates that Rucaparib has potential in intra-cranial malignancy therapy. ^[4] Rucaparib significantly potentiates the cytotoxicity of topotecan and temozolomide in NB-1691, SH-SY-5Y, and SKNBE (2c) cells. Rucaparib enhances the antitumor activity of temozolomide and indicates complete and sustained tumor regression in NB1691 and SHSY5Y xenografts. ^[5]

Protocol

Kinase Assay:^[1]	- Collapse K_i Determination: Inhibition of human full-length recombinant PARP-1 by [³²P]NAD⁺ incorporation is measured. The [³²P]ADP-ribose incorporated into acid insoluble material is quantified using a PhosphorImager. K_i is calculated by nonlinear regression analysis.
Cell Research:^[4]	- Collapse Cell lines: D425Med, D283Med and D384Med cells Concentrations: 0.4 μM Incubation Time: 3 or 5 days Method: Medulloblastoma cell lines are seeded in 96-well plates at a density of 1 × 10³, 3 × 10³ and 3 × 10³, respectively. At 24 hours (D384Med) or 48 hours (D283Med and D425Med) after seeding, the cells are exposed to various concentrations of temozolomide in the presence or absence of 0.4 μM Rucaparib. After 3 days (D425Med and D384Med) or 5 days (D283Med) of culture, cell viability is evaluated by a XTT cell proliferation kit assay. Cell growth is expressed as a percentage in relation to DMSO or 0.4 μM Rucaparib-alone controls. The concentration of temozolomide, alone or in combination with Rucaparib that inhibited growth by 50% (GI50) is calculated. The potentiation factor 50 (PF50) is defined as the ratio of the GI50 of temozolomide in the presence of Rucaparib to the GI50 of temozolomide alone. (Only for Reference)
Animal Research:^[4]	- Collapse Animal Models: CD-1 nude mice bearing established D283Med xenografts Dosages: 1 mg/kg Administration: One or four daily by i.p. (Only for Reference)

References

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Solubility (25°C)

In vitro	DMSO	84 mg/mL (199.35 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 2% DMSO+30% PEG 300+2% 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 Rucaparib (AG-014699) phosphate SDF

Molecular Weight	421.36
Formula	C₁₉H₁₈FN₃O.H₃PO₄
CAS No.	459868-92-9
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	PF-01367338
Smiles	CNCC1=CC=C(C=C1)C2=C3CCNC(=O)C4=C3C(=CC(=C4)F)N2.OP(=O)(O)O

In vivo Formulation Calculator (Clear solution)

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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.

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The Serial Dilution Calculator Equation

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Computed Result

C1=C0/X	C1:	LOG(C1):
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Molecular Weight Calculator

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

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

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04539327	Recruiting	Drug: Rucaparib	Epithelial Ovarian Cancer\|Fallopian Tube Cancer\|Primary Peritoneal Cancer	Grupo Español de Investigación en Cáncer de Ovario\|Clovis Oncology Inc.	July 29 2020	--
NCT04179396	Recruiting	Drug: Rucaparib\|Drug: Enzalutamide\|Drug: Abiraterone	Metastatic Castration Resistant Prostate Cancer	Clovis Oncology Inc.	December 5 2019	Phase 1
NCT04171700	Recruiting	Drug: Rucaparib	Solid Tumor	Clovis Oncology Inc.	November 21 2019	Phase 2
NCT03954366	Active not recruiting	Drug: Rucaparib\|Drug: Rosuvastatin\|Drug: Oral Contraceptives	Neoplasms	Clovis Oncology Inc.	May 8 2019	Phase 1
NCT03824704	Terminated	Drug: Rucaparib\|Drug: Nivolumab	Epithelial Ovarian Cancer\|Fallopian Tube Cancer\|Primary Peritoneal Carcinoma\|High Grade Serous Carcinoma\|Endometrioid Adenocarcinoma	Clovis Oncology Inc.\|Bristol-Myers Squibb\|Foundation Medicine	May 15 2019	Phase 2

Tech Support

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PARP Signaling Pathway Map

PARP Inhibitors with Unique Features

Selective PARP Inhibitors

AG-14361 : PARP1-selective, K_i<5 nM.
Selective PARP Inhibitors

UPF 1069 : PARP2-selective, IC50=0.3 μM.
Most Potent PARP Inhibitor

MK-4827 (Niraparib) : PARP1, IC50=3.8 nM; PARP2, IC50=2.1 nM.
PARP Inhibitor in Clinical Trial

Iniparib (BSI-201) : Phase III for solid tumors.
Newest PARP Inhibitor

PJ34 HCl ^New : PARP inhibitor with EC50 of 20 nM and is equally potent to PARP1/2.

Related PARP Products

G007-LK ^New

G007-LK is a potent and selective tankyrase inhibitor with IC50 of 46 nM and 25 nM for TNKS1/2, respectively.
NU1025 ^New

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.
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.
A-966492

A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with K_i of 1 nM and 1.5 nM, respectively.

Features:A promising, structurally diverse benzimidazole analogue that is being further characterized preclinically.

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Rucaparib (AG-014699) phosphate