Rucaparib (AG-014699) phosphate

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 Ki 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

Purity & Quality Control

Choose Selective PARP Inhibitors

Biological Activity

Description Rucaparib (AG-014699, PF-01367338) is an inhibitor of PARP with Ki 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=>
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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=
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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-
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A2780 NGfEPVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnTVTWM2OD1|Lkm0JOKyKDBwMkWg{txO MnrqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5Mkm0NFIoRjJ|N{K5OFAzRC:jPh?=
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DU145 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHBfYExNTNizszN M{TmUVE1KGR? NFq3ZXhFVVOR M4XLfIRm[3KnYYPld{Bkd2yxbomgcpVu[mW{IHTvd4Uh\GWyZX7k[Y51dHl? MnroQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3NkWyOFQoRjJ|NU[1NlQ1RC:jPh?=
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MDA-MB-231 NVu2N4U2S2WubDDWbYFjcWyrdImgRZN{[Xl? NXrKTZl[UUN3ME2xN{DPxE1? M2XZZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{Nke4NVYyLz5{Mk[3PFE3OTxxYU6=
Cal-51 M4TDVmNmdGxiVnnhZoltcXS7IFHzd4F6 M13qdmlEPTB;OD62JO69VQ>? NWDvcFNJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2O|gyPjFpPkKyOlc5OTZzPD;hQi=>
LoVo Mke4SpVv[3Srb36gZZN{[Xl? NGHJ[nM{OCCvaX7z NV\Cfop1UW6qaXLpeIlwdiCxZjDQRXJRKGmwIHj1cYFvKEyxVn:gZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCyb3z5LGFFWClvcnnic5NmKHCxbInt[ZJqgmG2aX;uJIZweiB|MDDtbY5{KGK7IH\seY9z\XOlZX7j[UBie3OjeTygSWM2OCB;IECuNFA1PjlizszNMi=> NITv[3k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nk[1NlcyPyd-Mk[2OVI4OTd:L3G+
MX1 Mk[wR5l1d3SxeHnjbZR6KGG|c3H5 NGHMPJZEgXSxdH;4bYNqfHliYXfhbY5{fCCEUlPBNU1l\W[rY3nlcpQhcHWvYX6gUXgyKGOnbHzzMEBGSzVyIE2gNE4xODV|IN88UU4> MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjZ3MkexO{c,OjZ4NUK3NVc9N2F-
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=>
LoVo MkTIR5l1d3SxeHnjbZR6KGG|c3H5 MYKwMlQhfU1? MlrYOUBl[Xm| MoCwVI91\W62aXH0bY9vKG:oIITlcY97d2yxbXnk[U1qdmS3Y3XkJIN6fG:2b4jpZ4l1gSCrbjDoeY1idiCOb2\vJINmdGy|IHHzd4V{e2WmIHHzJJRmdW:8b3zvcYll\SCJSUWwJIF1KDBwNDD1UUBi\nSncjC1JIRigXNiYomgR4VtdHSrdHXyMWdtdyCjc4PhfUwhT0l3MDC9JFAvOTR2IN88UU4> MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjZ3MkexO{c,OjZ4NUK3NVc9N2F-
Capan1 NV;VXZE4S3m2b4TvfIlkcXS7IHHzd4F6 NHiyOmdEgXSxdH;4bYNqfHliYXfhbY5{fCCEUlPBNk1l\W[rY3nlcpQhcHWvYX6gR4Fx[W5zIHPlcIx{NCCHQ{WwJF0hOC54MEmg{txONg>? NGD4Z3o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nk[1NlcyPyd-Mk[2OVI4OTd:L3G+
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     


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     


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     


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     


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     


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     


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     


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

Ki 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. Ki 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)

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

Molecular Weight 421.36
Formula

C19H18FN3O.H3PO4

CAS No. 459868-92-9
Storage powder
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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Clinical Trial Information

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID