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Olaparib (AZD2281)

For research use only.

Catalog No.S1060 Synonyms: Ku-0059436

636 publications

Olaparib (AZD2281) Chemical Structure

CAS No. 763113-22-0

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.

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Selleck's Olaparib (AZD2281) has been cited by 636 publications

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Choose Selective PARP Inhibitors

Biological Activity

Description 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).
Targets
PARP2 [1]
(Cell-free assay)		 PARP1 [1]
(Cell-free assay)
1 nM 5 nM
In vitro

Olaparib would act against BRCA1 or BRCA2 mutations. Olaparib is not sensitive to tankyrase-1 (IC50 >1 μM). Olaparib could ablate the PARP-1 activity at concentrations of 30-100 nM in SW620 cells. Olaparib is hypersensitive to BRCA1-deficient cell lines (MDA-MB-463 and HCC1937), compared with BRCA1- and BRCA2-proficient cell lines (Hs578T, MDA-MB-231, and T47D). [1] Olaparib is strongly sensitive to KB2P cells due to suppression of base excision repair by PARP inhibition, which may result in the conversion of single-strand breaks to double-strand breaks during DNA replication, thus activating BRCA2-dependent recombination pathways. [2]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Hep3B NV;SXVZtTnWwY4Tpc44hSXO|YYm= MYq0NEDPxE1? Moe2NlQhcA>? Mnv4SG1UVw>? MYfJcoR2[2W|IGLPV{Bxem:mdXP0bY9vKHerdHigSGhOTVF? MnzlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyN{K3OVIoRjJ3MEeyO|UzRC:jPh?=
Huh7 MmDpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWS0NEDPxE1? MVu3NkBp NH7VbWFFVVOR MX3TfY5memerc4TpZ4FtdHliaX7obYJqfHNiY3XscEBoem:5dHige4l1cCCGSF3FVS=> NWfHUmlYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwO|I4PTJpPkK1NFczPzV{PD;hQi=>
Hep3B MnrmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkL4OFAh|ryP NV3qfnNDPzJiaB?= MVPEUXNQ MWjTfY5memerc4TpZ4FtdHliaX7obYJqfHNiY3XscEBoem:5dHige4l1cCCGSF3FVS=> NYTTfmtiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwO|I4PTJpPkK1NFczPzV{PD;hQi=>
TE-6 MVzGeY5kfGmxbjDBd5NigQ>? MXO1JO69VQ>? NVzjNWYxOjRiaB?= M4rqb2ROW09? NY\SV41tUW6lcnXhd4V{KGmwIHTveYJt\SC|dILhcoQh[nKnYXvzJEhFW0K|KR?= M{HOZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MkG5NVY1Lz5{NEKxPVE3PDxxYU6=
TE-6 Ml;FSpVv[3Srb36gRZN{[Xl? NYXQdWV{PSEQvF2= NXP3enRlOTJiaB?= NVi0N|huTE2VTx?= NGDzO5VKdmS3Y3XzJGczN01iYYLy[ZN1 NFjDZ|c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEKxPVE3PCd-MkSyNVkyPjR:L3G+
HT29 M2\xUWZ2dmO2aX;uJGF{e2G7 MnG3NVAhdk1? MWOxNkBp M17FXWROW09? NVH0T5dWUW6lcnXhd4V{KESQQTDkc5VjdGVvc4TyZY5lKGK{ZXHrd{BqdmS3Y3XkJIJ6KFOQLUO4 MkLXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3N{e5OFEoRjJ2NUe3PVQyRC:jPh?=
HCT116 NYrzNJk{TnWwY4Tpc44hSXO|YYm= M3HyWlExKG6P NVHmeYp5OTJiaB?= M4rwOWROW09? Ml3zTY5kemWjc3XzJGRPSSCmb4XicIUue3S{YX7kJIJz\WGtczDpcoR2[2WmIHL5JHNPNTN6 Mn3TQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3N{e5OFEoRjJ2NUe3PVQyRC:jPh?=
RKO M4[wc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3SzeFExOCEQvF2= NXn4c3BnPDhiaB?= MlfJSG1UVw>? MkfKVI91\W62aXH0[ZMhW05vM{igZ5l1d3SxeHnjbZR6 Mof0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3N{e5OFEoRjJ2NUe3PVQyRC:jPh?=
C-1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TWT|ExOCEQvF2= M4DK[lQ5KGh? M{LhOmROW09? MWjQc5RmdnSrYYTld{BUVi1|ODDjfZRwfG:6aXPpeJk> NWfIb5JGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1O|c6PDFpPkK0OVc4QTRzPD;hQi=>
SW48 M3nTRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUexNFAh|ryP M4LBR|Q5KGh? M13Vc2ROW09? NFO1XVdRd3SnboTpZZRmeyCVTj2zPEBkgXSxdH;4bYNqfHl? MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV5N{m0NUc,OjR3N{e5OFE9N2F-
LoVo MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXz3Wok4OTByIN88US=> MVS0PEBp NV3iZZVuTE2VTx?= NWnKPJltWG:2ZX70bYF1\XNiU16tN|gh[3m2b4TvfIlkcXS7 M4jXW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NUe3PVQyLz5{NEW3O|k1OTxxYU6=
HT29 NUPSRZJ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfMZmhyOTByIN88US=> NF2xVGs1QCCq NFPTWXlFVVOR MnvGVI91\W62aXH0[ZMhW05vM{igZ5l1d3SxeHnjbZR6 Mor6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3N{e5OFEoRjJ2NUe3PVQyRC:jPh?=
SW1116 M{f0Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV6xNFAh|ryP NWnWZVNDPDhiaB?= NGTRN4xFVVOR MVrQc5RmdnSrYYTld{BUVi1|ODDjfZRwfG:6aXPpeJk> NVqyN2hXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1O|c6PDFpPkK0OVc4QTRzPD;hQi=>
HCT116 NWTKTW1FT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVmxNFAh|ryP MUm0PEBp MWfEUXNQ M3jq[HBwfGWwdHnheIV{KFOQLUO4JIN6fG:2b4jpZ4l1gQ>? MnnGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3N{e5OFEoRjJ2NUe3PVQyRC:jPh?=
RKO NUPqToNNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;lNVAxKM7:TR?= M37BSVQ5KGh? MkLHSG1UVw>? MWHJR|UxRTVwOTFOwG0> NVzPcmtFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1O|c6PDFpPkK0OVc4QTRzPD;hQi=>
C-1 NGL3OoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVexNFAh|ryP NH7uUVY1QCCq NH;DWFhFVVOR M3rTUmlEPTB;Nz62JO69VQ>? MkTtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3N{e5OFEoRjJ2NUe3PVQyRC:jPh?=
SW48 MkjzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\IUlZbOTByIN88US=> NWL1OFlUPDhiaB?= NXzFV3ZSTE2VTx?= MkC0TWM2OD17LkWg{txO NUHx[mFERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1O|c6PDFpPkK0OVc4QTRzPD;hQi=>
HCT-15 MmXJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDENVAxKM7:TR?= MlnSOFghcA>? MXTEUXNQ NFG5XmFKSzVyPUGwJO69VQ>? NHX0b4g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW3O|k1OSd-MkS1O|c6PDF:L3G+
LoVo NInBU3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIjQeIYyODBizszN M{DXZlQ5KGh? MYfEUXNQ NE[0TJJKSzVyPUGzMlQh|ryP MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV5N{m0NUc,OjR3N{e5OFE9N2F-
HT29 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkT1NVAxKM7:TR?= NXXFe4VjPDhiaB?= NWD4bJUxTE2VTx?= NHnoTWhKSzVyPUG0Mlch|ryP NFHRdXY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW3O|k1OSd-MkS1O|c6PDF:L3G+
SW1116 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LQc|ExOCEQvF2= Mn[4OFghcA>? NHOwUY9FVVOR NF23cG1KSzVyPUGwNEDPxE1? M1e1flxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NUe3PVQyLz5{NEW3O|k1OTxxYU6=
HCT116 NX3HcHBlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXxNVAxKM7:TR?= MlmxOFghcA>? MmS3SG1UVw>? MV7JR|UxRTJwNTFOwG0> NGHHOVQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW3O|k1OSd-MkS1O|c6PDF:L3G+
T47D MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XkXlUh\GG7 NX7Dc4oyUUN3ME25MlYh|ryP M2[4SVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{[wOFk3Lz5{M{e2NFQ6PjxxYU6=
MCF7 MnPXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYW1JIRigQ>? M32zSmlEPTB;NT64JO69VQ>? NF72U5g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{e2NFQ6Pid-MkO3OlA1QTZ:L3G+
CAMA1 NITj[JJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDNfIFLPSCmYYm= M3HiXWlEPTB;MUWuPEDPxE1? NWWzWm9ERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3OlA1QTZpPkKzO|YxPDl4PD;hQi=>
SUM159 NXjm[ng4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX61JIRigQ>? MnHYTWM2OD12LkKg{txO M2X4[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{[wOFk3Lz5{M{e2NFQ6PjxxYU6=
SKBR3 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MorCOUBl[Xl? M1vzSmlEPTB;MUGuNUDPxE1? NFK3XZY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{e2NFQ6Pid-MkO3OlA1QTZ:L3G+
JIMT1 M4O3TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVS1JIRigQ>? Ml3lTWM2OD15Lkeg{txO NG\LUos9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{e2NFQ6Pid-MkO3OlA1QTZ:L3G+
BT474 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTEcm02KGSjeR?= M4H5ZmlEPTB;MUmuPEDPxE1? MkPmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5NkC0PVYoRjJ|N{[wOFk3RC:jPh?=
Hs578t(si) MnXsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{i1e|Uh\GG7 NVXHO|RqUUN3ME23MlUh|ryP M1fHe|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{[wOFk3Lz5{M{e2NFQ6PjxxYU6=
Hs578t NXXMPFNNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnUR5VDPSCmYYm= NGXNb2RKSzVyPUWuOkDPxE1? Mmn6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5NkC0PVYoRjJ|N{[wOFk3RC:jPh?=
HCC1937 NHm0fm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jqflUh\GG7 MVXJR|UxRTF{Lk[g{txO M{LDWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{[wOFk3Lz5{M{e2NFQ6PjxxYU6=
HCC1143 NVPUdHVTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vVXlUh\GG7 NUD2OGRTUUN3ME2xNU4yKM7:TR?= NYTiSFhFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3OlA1QTZpPkKzO|YxPDl4PD;hQi=>
BT20 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3izblUh\GG7 NW\1WFM{UUN3ME23Mlch|ryP M3TvNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{[wOFk3Lz5{M{e2NFQ6PjxxYU6=
MDA-MB-468 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHn5b4k2KGSjeR?= MXvJR|UxRTVwMDFOwG0> Mn\UQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5NkC0PVYoRjJ|N{[wOFk3RC:jPh?=
MDA-MB-231 M1nQWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVO1JIRigQ>? MoDDTWM2OD14Lkmg{txO M3nEUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{[wOFk3Lz5{M{e2NFQ6PjxxYU6=
PC-9PTEN− MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXe2T|Z2OjBizszN MkjFNVQ1KGh? MmDsTWM2OD14LkWyJO69VQ>? M3m0RVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MkO5PFA6Lz5{M{KzPVgxQTxxYU6=
PC-9 NGrQSHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWHMVVVOOjBizszN NEHvW3IyPDRiaB?= MXrJR|UxRTVwOEig{txO M3\ZWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MkO5PFA6Lz5{M{KzPVgxQTxxYU6=
H1650PTEN+ NH\4eVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\xTnhWOjBizszN NX;SPVlTOTR2IHi= M3vjeWlEPTB;NUCuPFMh|ryP NV7mcFQxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOyN|k5ODlpPkKzNlM6QDB7PD;hQi=>
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Mouse ATM−/− ES Cells M1vVOWN6fG:2b4jpZ{BCe3OjeR?= M3XBcFIvPSEQvF2= MY[yNEBp MoThV4lodmmoaXPhcpRtgSCrbnjpZol1eyClZXzsJJN2en[rdnHs M2LkWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{W1OFg6Lz5{M{O1OVQ5QTxxYU6=
Mouse H2AX−/− ES Cells M2DiRmN6fG:2b4jpZ{BCe3OjeR?= NULhR3VrOi53IN88US=> MYWyNEBp MUfTbYdvcW[rY3HueIx6KGmwaHnibZR{KGOnbHygd5Vzfmm4YXy= NXX1V4Q6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzOVU1QDlpPkKzN|U2PDh7PD;hQi=>
VCaP NVP0OFZ[UW64YYPpeoUhSXO|YYm= NGC2VJczPSEQvF2= M1TSXlQ5KGh? NVLmWm1RTE2VTx?= MVzTbYdvcW[rY3HueIx6KHKnZIXj[ZMhTVKJLXTybZZmdiClZXzsJIlvfmG|aX;u M4m2fVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNUe1PFY2Lz5{MUW3OVg3PTxxYU6=
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T98G MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4H5b2lEPTB;NEiuOFY{OyEQvF2= MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1NlE3QDZxJ{7TRW5ITVJ:L3G+
NCI-H1573 NXTqcGR3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHJeGRKSzVyPUS5MlQ1PjJizszN MkPFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVIyPjh4Lze+V2FPT0WUPD;hQi=>
MEG-01 MkLVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrCVGtoUUN3ME20PU44PDFzIN88US=> MoTyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVIyPjh4Lze+V2FPT0WUPD;hQi=>
WM-115 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjleFd6UUN3ME20PU46OjJ{IN88US=> M1zUT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFUzOTZ6Nj:nQnNCVkeHUkyvZV4>

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western Blot
DR5/CHOP; 

PubMed: 25531448     


(A) U87 GBM cells were treated with Olaparib (10 µM) for the indicated time points, subjected to immunoblotting and analyzed for the expression of DR5. B-D) U87 (B), U373 (C) and LN229 GBM cells (D) were treated with increasing concentrations of Olaparib (µM) for 7 hours, subjected to immunoblotting and analyzed for the expression of CHOP and DR5. E–F) MDA-MB-468 (E) and MDA-MB-436 (F) were treated with increasing concentrations (µM) of Olaparib for 7 hours, harvested for immunoblotting and analyzed for the expression of DR5.

γH2AX/H2AX; 

PubMed: 22933245     


FK866 exacerbates levels of γH2AX caused by olaparib. CAL51 cells were exposed to FK866 and/or olaparib for 48 h and cell lysates generated and immunoblotted for total and γH2AX.

pATM; 

PubMed: 27686740     


(C) Western blot analysis in HN9-cisR cells according to changes in olaparib doses. Olaparib induced pATM and 53BP1 activation in a dose-dependent manner in HN9-cisR cells. 

53BP1; 

PubMed: 27686740     


(C) Western blot analysis in HN9-cisR cells according to changes in olaparib doses. Olaparib induced pATM and 53BP1 activation in a dose-dependent manner in HN9-cisR cells. 

NF-kB; 

PubMed: 27686740     


(C) Western blot analysis in HN9-cisR cells according to changes in olaparib doses. Olaparib induced pATM and 53BP1 activation in a dose-dependent manner in HN9-cisR cells. 

pS6/S6; 

PubMed: 24831086     


HCC1937 cells (BRCA1-inactive) were treated with 10 nM olaparib with indicated times. Whole-cell lysates were prepared and analyzed by Western blotting with the indicated antibodies. 

25531448 22933245 27686740 24831086
Immunofluorescence
DNA damage; 

PubMed: 27686740     


(A) A comet assay and (B) γH2AX immunofluorescence assay were performed 72 h after olaparib treatment to identify DNA damage. A relatively higher level of DNA damage was observed in HN9-cisR cells; however, olaparib also induced slight DNA damage in olaparib-resistant HN4-cisR cells. Magnification: × 100 (comet assay); × 400 (γH2AX).

γH2AX; 

PubMed: 28069876     


Representative images of immunofluorescence (IF) staining for γH2AX in 22RV1 cells treated with of BI2536 (5 nM), Olaparib (10 µM) or both for 24 h. 22RV1 cells (1 × 105) were plated in 6-well plates on day 0 and then treated with BI2536, Olaparib or both for 24 h.

27686740 28069876
Growth inhibition assay
Cell viability ; 

PubMed: 25531448     


A-D): U87 (A), U373 (B), LN229 (C) and MDA-MB-468 (D) cells were treated with suboptimal dosages of TRAIL (A: 100 ng/ml, B: 25 ng/ml, C: TRAIL 200 ng/ml, D: 10 ng/ml), Olaparib (A–C: 10 µM, D: 5 µM) or the combination of both reagents for 48 hours. Thereafter, MTT assays were performed to determine cellular viability.

25531448
ELISA
IL-8; 

PubMed: 28456021     


ELISA measuring PAR levels in Akata-EBV cells. Cells were treated with 2.5 μM olaparib for 24 h to inhibit PARP activity. Data are shown as pg of PAR per μg of protein. 

GLP-1; 

PubMed: 29392078     


Olaparib enhances promotes GLP-1 secretion in NCI-H716 cells Cells were stimulated for 30 minutes with or without 16 mM glucose. GLP-1 was measured by ELISA. Bars represent the mean of three independent experiments normalized to the control. Error bars indicate standard deviation. Statistical analyses were performed by two-tailed Student’s t-test and significance is denoted by asterisks where *P<0.05.

28456021 29392078
In vivo Combining with temozolomide, Olaparib (10 mg/kg, p.o.) significantly suppresses tumor growth in SW620 xenografts. [1] Olaparib shows great response to Brca1-/-;p53-/- mammary tumors (50 mg/kg i.p. per day), while no responses to HR-deficient Ecad-/-;p53-/- mammary tumors. Olaparib even does not show dose-limiting toxicity in tumor-bearing mice. [3] Olaparib has been used to treat with BRCA mutated tumors, such as ovarian, breast and prostate cancers. Moreover, Olaparib shows selectively inhibition to ATM (Ataxia Telangiectasia Mutated)-deficient tumor cells, which indicates to be a potential agent for treating ATM mutant lymphoid tumors. [4]

Protocol

Kinase Assay:

[1]
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FlashPlate assay (96-well screening assay):

To columns 1 through 10, 1 μL of Olaparib (in DMSO) is added, and 1 μL DMSO only is added to the positive (POS) and negative (NEG) control wells (columns 11 and 12, respectively) of a pretreated FlashPlate. PARP-1 is diluted 1:40 in buffer (buffer B: 10% glycerol (v/v), 25 mM HEPES, 12.5 mM MgCl2,50 mM KCl, 1 mM DTT, 0.01% NP-40 (v/v), pH 7.6) and 40 μL added to all 96 wells (final PARP-1 concentration in the assay is ~1 ng/μL). The plate is sealed and shaken at RT for 15 min. Following this, 10 μL of positive reaction mix (0.2 ng/μL of double-stranded oligonucleotide [M3/M4] DNA per well, 5 μM of NAD+ final assay concentration, and 0.075 μCi 3H-NAD+ per well) is added to the appropriate wells (columns 1-11). The negative reaction mix, lacking the DNA oligonucleotide, is added to column 12 (with the mean negative control value used as the background). The plate is resealed and shaken for a further 60 min at RT to allow the reaction to continue. Then, 50 μL of ice-cold acetic acid (30%) is added to each well to stop the reaction, and the plate is sealed and shaken for a further 60 min at RT. Tritiated signal bound to the FlashPlate is then determined in counts per minute (CPM) using the TopCount plate reader.
Cell Research:

[1]
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  • Cell lines: Breast cancer cell lines including SW620 colon, A2780 ovarian, HCC1937, Hs578T, MDA-MB-231, MDA-MB-436, and T47D
  • Concentrations: 1-300 nM
  • Incubation Time: 7-14 days
  • Method:

    The cytotoxicity of Olaparib is measured by clonogenic assay. Olaparib is dissolved in DMSO and diluted by culture media before use. The cells are seeded in six well plates and left to attach overnight. Then Olaparib is added at various concentrations and the cells are incubated for 7-14 days. After that the surviving colonies are counted for calculating the IC50.


    (Only for Reference)
Animal Research:

[3]
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  • Animal Models: Brca1-/-;p53-/- mammary tumors are generated in K14cre;Brca1F/F;p53F/F mice.
  • Dosages: 50 mg/kg
  • Administration: Administered via i.p. injection at 10 μL/g of body weight
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 86 mg/mL warmed (197.94 mM)
Water 0.002 mg/mL (0.0 mM)
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
4% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing. 		5mg/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 434.46
Formula

C24H23FN4O3
CAS No. 763113-22-0
Storage powder
in solvent
Synonyms Ku-0059436
Smiles C1CC1C(=O)N2CCN(CC2)C(=O)C3=C(C=CC(=C3)CC4=NNC(=O)C5=CC=CC=C54)F

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
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Bio Calculators

Molarity Calculator

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)

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*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

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 )

  • C1
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* 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

  • 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

Molecular Weight Calculator

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

Total Molecular Weight: g/mol

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

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04644289 Not yet recruiting Drug: olaparib|Drug: durvalumab Epithelial Ovarian Cancer AGO Research GmbH July 2021 Phase 2
NCT04641728 Not yet recruiting Drug: Pembrolizumab|Drug: Olaparib Cervical Cancer Saitama Medical University International Medical Center|Tokyo University|National Cancer Center Japan|Cancer Institute Hospital Japan|Aichi Cancer Center January 1 2021 Phase 2
NCT04515836 Not yet recruiting Drug: Olaparib Mesothelioma|Homologous Recombination Deficiency University of Chicago|AstraZeneca December 15 2020 Phase 2
NCT04024254 Recruiting Drug: Folic Acid Tablet Ovarian Cancer|Breast Cancer|Folic Acid Deficiency Rush University Medical Center July 21 2020 Phase 2|Phase 3

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.

  • * Indicates a Required Field

Frequently Asked Questions

  • Question 1:

    How to prepare the solution of the compound (S1060) for in vivo study?

  • Answer:

    We recommend the following formulation: 4% DMSO+30% PEG300+ 66%H2O. It is a clear solution and can be used for IP injection.

  • Question 2:

    I saw that the solubility of the compound for in vivo on the website had been changed, why the change has been made?

  • Answer:

    For the formulation for in vivo, the compound dissolving in 15% Captisol (former solubility) is a suspension, and it is fine for oral gavage. And now, dissolving in 4% DMSO+30% PEG 300+ddH2O is a clear solution, and is for injection.

  • Question 3:

    How long can the chemical compound be stable in DMEM at 4 °C?

  • Answer:

    The compound is stable in DMEM at 4 degree for one week.

selleck catalog

PARP Signaling Pathway Map

PARP Inhibitors with Unique Features

  • Selective PARP Inhibitors

    AG-14361 : PARP1-selective, Ki<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

    BMN 673 : Novel PARP inhibitor with IC50 of 0.58 nM. Also a potent inhibitor of PARP-2, but does not inhibit PARG and highly sensitive to PTEN mutation.

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.

  • Veliparib (ABT-888)

    Veliparib (ABT-888, NSC 737664) is a potent inhibitor of PARP1 and PARP2 with Ki 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 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.

  • 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 Ki 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 Ki 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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID