Rucaparib (AG-014699) phosphate

Name: Rucaparib (AG-014699) phosphate
Brand: Selleck Chemicals
SKU: S1098
Rating: 5 (103 reviews)

For research use only.

Catalog No.S1098 Synonyms: PF-01367338

103 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 103 publications

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

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

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Cell Rep, 2021, 36(4):109429

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J Exp Clin Cancer Res, 2021, 40(1):276

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Cell Death Dis, 2021, 12(6):546

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

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

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Gynecol Oncol, 2021, S0090-8258(21)00325-5

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J Pharmacol Exp Ther, 2021, 377(3):385-397

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Cell Signal, 2021, S0898-6568(21)00195-9

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bioRxiv, 2021, 10.1101/2020.10.18.333070

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NPJ Breast Cancer, 2021, 7(1):111

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Nat Cancer, 2021, 2(6):598-610

PubMed: 34179826 ( click the link to review the publication )

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 )

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

PubMed: 33531658 ( click the link to review the publication )

Nat Commun, 2021, 12(1):736

PubMed: 33531508 ( 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 )

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(9):2813-2831

PubMed: 33042619 ( 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 )

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

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

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

Proc Natl Acad Sci U S A, 2020, 201919445

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NAR Cancer, 2020, 2(3):zcaa013

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

Cell Rep, 2020, 32(5):107985

PubMed: 32755579 ( 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 )

Commun Biol, 2020, 3(1):388

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

bioRxiv, 2020, 30;2020.4.17.47480

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

Cancer Res, 2020, 10.1158

PubMed: 32127357 ( 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-19-0242

PubMed: 31534014 ( 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 Res, 2019, 17(2):409-419

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

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

PubMed: 30401718 ( 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 )

Chem Biol Drug Des, 2016, 87(3):478-82

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Parasit Vectors, 2016, 9:173

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

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

Cancer Res, 2015, 75(4):628-34

PubMed: 25634215 ( click the link to review the publication )

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

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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

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

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

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

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EJNMMI Res, 2013, 4(1):2

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

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

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

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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	NIT0W2NHfW6ldHnvckBCe3OjeR?=	MY[wMlEwOS93MECvNVAxOCCwTR?=			MoPQbY5pcWKrdIOgVGFTWCCjY4Tpeol1gSCjdDDzeIFzfGmwZzDjc45k\XKwdILheIlwdiCxZjC1NFAhdk1?	MkX2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVzMki0OVUoRjJ3MUK4OFU2RC:jPh?=
BT474	NHrZfJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M4fSSlUxOCCwTR?=	MnLlNVDjiJNzNdMg[C=>		MmS0doVlfWOnczDj[YxtKGe{b4f0bEBqdiC2aHWg[o92eiCuaX7ld{BidmRic3nncolncWOjboTsfS=>	NXrFdo45RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWxNlg1PTVpPkK1NVI5PDV3PD;hQi=>
SKBR3	MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M33SfFUxOCCwTR?=	NVHDN2VYOTEkgKOxOeKh\A>?		NXrDN2JiemWmdXPld{Bk\WyuIHfyc5d1cCCrbjD0bIUh\m:3cjDsbY5meyCjbnSgd4lodmmoaXPhcpRtgQ>?	MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTF{OES1OUc,OjVzMki0OVU9N2F-
AU565	M1X5U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	Mn7NOVAxKG6P	M4nQUFEx6oDVMUZCpIQ>		MYHy[YR2[2W\|IHPlcIwh\3Kxd4ToJIlvKHSqZTDmc5VzKGyrbnXzJIFv\CC\|aXfubYZq[2GwdHz5	NGqyeVQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUGyPFQ2PSd-MkWxNlg1PTV:L3G+
EFM192A	MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NW\DXWdtPTByIH7N	MWixNQKBmzF3wrDk		NYnpeIRNemWmdXPld{Bk\WyuIHfyc5d1cCCrbjD0bIUh\m:3cjDsbY5meyCjbnSgd4lodmmoaXPhcpRtgQ>?	M2G0WFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MUK4OFU2Lz5{NUGyPFQ2PTxxYU6=
MDA-MB-231	MXHGeY5kfGmxbjDBd5NigQ>?	M2jBRlExNzJyL{SwJO69VQ>?	MlXFNlQhcA>?		NHv1OHFqdmO{ZXHz[ZMheC2DS2SgcIV3\Wy\|IHnuJIEh\G:\|ZT3k[ZBmdmSnboSgcYFvdmW{	M3\uWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEKwNVUzLz5{NESyNFE2OjxxYU6=
MDA-MB-231	Mme2R4VtdCCYaXHibYxqfHliQYPzZZk>	MkS5NE4yNTRyIN88US=>	NGfqe5AzPCCq		M362emlEPTEkgJm95qCKOTdwN{hCpO69VQ>?	M1PHVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEKwNVUzLz5{NESyNFE2OjxxYU6=
MDA-MB-231	NXnBfIJtSXCxcITvd4l{KEG\|c3H5	MWSxNE8zOC92MDFOwG0>	NIfmT4szPCCq		MYLpcoR2[2W\|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7	M3izRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEKwNVUzLz5{NESyNFE2OjxxYU6=
MDA-MB-231	NEfIUJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MYOxNE8zOC92MDFOwG0>	NV;TdZRwOjRiaB?=		MoXQZoxw[2u\|IHPlcIwh[3mlbHWgdJJw\3Knc4Ppc44hcW5iR{KvUUBxcGG\|ZR?=	NYGye2w5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0NlAyPTJpPkK0OFIxOTV{PD;hQi=>
H460	NYnudIgxT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MmfOOFAxKG6P	MWeyOOKhcA>?		NXGyZnBZcW6lcnXhd4V{KGOnbHz1cIFzKHKjZHnvd4Vve2m2aY\peJk>	M2e3VVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEGxOlEyLz5{NESxNVYyOTxxYU6=
A549	M1m5TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M1zMXVQxOCCwTR?=	NWGzVlByOjUEoHi=		MkXXbY5kemWjc3XzJINmdGy3bHHyJJJi\Gmxc3Xud4l1cX[rdIm=	MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDRzMU[xNUc,OjR2MUG2NVE9N2F-
DT40	NFTad3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				Mk\PTWM2OD1{MTDuUS=>	NUHaNHFrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOVY5OTNpPkK0N\|U3QDF\|PD;hQi=>
DU145	NIX0c4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NVP2dItLUUN3ME2xPEBvVQ>?	MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN3NkixN{c,OjR\|NU[4NVM9N2F-
COLO704	NW\lVGNVT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				MlTMTWM2OD1{LkWyJOKyKDBwNkeg{txO	M3zRO\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|N{K5OFAzLz5{M{eyPVQxOjxxYU6=
OVMANAb	MnrwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NE\6dGZKSzVyPUKuOVghyrFiMD6zPEDPxE1?	MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd{OUSwNkc,OjN5Mkm0NFI9N2F-
OV177	MorZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				M4HDPWlEPTB;Mj63PEDDuSByLkexJO69VQ>?	NWOxPFR4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3Nlk1ODJpPkKzO\|I6PDB{PD;hQi=>
OAW28	MkHXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NVfUOZRTUUN3ME2zMlYyKMLzIECuNlgh\|ryP	MlXnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5Mkm0NFIoRjJ\|N{K5OFAzRC:jPh?=
OVSAHO	M2TiWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NIrRVmdKSzVyPUOuOlQhyrFiMD6zN{DPxE1?	MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd{OUSwNkc,OjN5Mkm0NFI9N2F-
OVKATE	NIqwN21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				MojtTWM2OD1\|Lk[0JOKyKDFwN{mg{txO	NIiwUIo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{eyPVQxOid-MkO3Nlk1ODJ:L3G+
OVCAR3	NIC5TIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				M4DYcGlEPTB;Mz63OEDDuSByLkSwJO69VQ>?	M{nneFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|N{K5OFAzLz5{M{eyPVQxOjxxYU6=
PEO14	NYr3[3JsT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				MlT5TWM2OD1\|Lki0JOKyKDBwN{[g{txO	MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd{OUSwNkc,OjN5Mkm0NFI9N2F-
A2780	NGfEPVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				MnTVTWM2OD1\|Lkm0JOKyKDBwMkWg{txO	MnrqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5Mkm0NFIoRjJ\|N{K5OFAzRC:jPh?=
OVTOKO	M4LYcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MYXJR\|UxRTRwMUSgxtEhOS53MzFOwG0>	MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd{OUSwNkc,OjN5Mkm0NFI9N2F-
KURAMOCHIb	M{XnPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				M2jLPWlEPTB;ND6zOEDDuSByLkK5JO69VQ>?	M4fzOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|N{K5OFAzLz5{M{eyPVQxOjxxYU6=
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MDA-MB-231	NVu2N4U2S2WubDDWbYFjcWyrdImgRZN{[Xl?				NXrKTZl[UUN3ME2xN{DPxE1?	M2XZZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{Nke4NVYyLz5{Mk[3PFE3OTxxYU6=
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Rosetta2 (DE3)	Moj5SpVv[3Srb36gZZN{[Xl?				MWjJcohq[mm2aX;uJI9nKGi3bXHuJG4ufGW{bXnuZYwhPniqaYOteIFo\2WmIFHSWGQ3KCh6N{OgeI8hOTF4MTmg[ZhxemW\|c3XkJIlvKEW\|Y3jldolkcGmjIHPvcIkhWm:\|ZYT0ZVIhMESHMzmgZ4VtdHNidYPpcochVkGGKzDhd{B{fWK\|dILheIUh[nliZnz1c5Jme2OnbnPlJIF{e2G7LDDJR\|UxKD1iMD6wNVQh\|ryPLh?=	NFT6NWg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmwNFc4OCd-MkS5NFA4PzB:L3G+
Rosetta2 (DE3)	MULGeY5kfGmxbjDhd5NigQ>?				MnfmTY5pcWKrdHnvckBw\iCqdX3hckA3gGircz30ZYdo\WRiQWLUSFUhMDFyM{CgeI8hOTNzNzmg[ZhxemW\|c3XkJIlvKEW\|Y3jldolkcGmjIHPvcIkhWm:\|ZYT0ZVIhMESHMzmgZ4VtdHNidYPpcochVkGGKzDhd{B{fWK\|dILheIUh[nliZnz1c5Jme2OnbnPlJIF{e2G7LDDJR\|UxKD1iMD6wNlUh\|ryPLh?=	NUPV[29uRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFA4PzBpPkK0PVAxPzdyPD;hQi=>
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MDA-MB-436	M3LrfWFvfGmlYX7j[ZIh[XO\|YYm=		NV34VW9TQTZiaILz		M3XKSWFvfGmlYX7j[ZIh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDCVmNCOS2mZX\pZ4lmdnRiTVTBMW1DNTR\|NjDj[YxteyCjZoTldkA6PiCqcoOgZpkhVVSWIHHzd4F6NCCFQ{WwJF0hOyEQvF2u	MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN2Mki2PEc,OjZ\|NEK4Olg9N2F-
OVCAR3	M2TMfGFvfGmycn;sbYZmemG2aY\lJIF{e2G7		NInPXpIzPCCqcoO=		NYLpRlN{SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDPWmNCWjNiY3XscJMh[W[2ZYKgNlQhcHK\|IHL5JG1VXCCjc4PhfUwhUUN3MDC9JFMvOzFizszNMi=>	NVj5[nl6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0OVYyODZpPkK5OFU3OTB4PD;hQi=>
MRC5	MYnDfZRwfG:6aXPpeJkh[XO\|YYm=				MWPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNVmM2KGOnbHzzMEBGSzVyIE2gPE42OyEQvF2u	MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjZ3MkexO{c,OjZ4NUK3NVc9N2F-
MCF7	M{j6RWFvfGmlYX7j[ZIh[XO\|YYm=		MXK5OkBpenN?		NU\tZpFLSW62aXPhcoNmeiCjY4Tpeol1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMh[W[2ZYKgPVYhcHK\|IHL5JG1VXCCjc4PhfUwhS0N3MDC9JFE6NjR5IN88UU4>	NVnYRlhQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[zOFI5PjhpPkK2N\|QzQDZ6PD;hQi=>
A673	NXHvbJlTeUiWUzDhd5NigQ>?				MYXxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSTZ5MzDj[Yxtew>?	M2S5V\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
A673	NInNN3VyUFSVIHHzd4F6				MmrVdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgRVY4OyClZXzsd{k>	MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
Rh41	NYizVWpueUiWUzDhd5NigQ>?				MlnOdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgVog1OSClZXzsdy=>	MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
SK-N-MC	MULxTHRUKGG\|c3H5				Mnq5dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgV2suVi2PQzDj[Yxtew>?	MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
TC32	M1PNSJFJXFNiYYPzZZk>				M4rHfpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHREOzJiY3XscJM>	MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	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. 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.	24085845 27960087
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	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. 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. 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. 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.	23565244 27515310 30589644

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

- Collapse

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

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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.
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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2021-09-06)

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	Active not 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
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	August 23 2019	Phase 2

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PARP Signaling Pathway Map

PARP Inhibitors with Unique Features

Selective PARP Inhibitors

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

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Blasticidin S HCl ^New

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Veliparib (ABT-888)

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AG-14361

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Rucaparib (AG-014699) phosphate