Olaparib (AZD2281)

For research use only.

Catalog No.S1060 Synonyms: Ku-0059436

737 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.

Selleck's Olaparib (AZD2281) has been cited by 737 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 MWLGeY5kfGmxbjDBd5NigQ>? M2WxeVQxKM7:TR?= MlzINlQhcA>? MXrEUXNQ NHiyOWNKdmS3Y3XzJHJQWyCycn;keYN1cW:wIIfpeIghTEiPRWG= NHHsNmI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC3Nlc2Oid-MkWwO|I4PTJ:L3G+
Huh7 NVLi[ow{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPIc20zPDBizszN M1LRcFczKGh? NYTSfHpCTE2VTx?= NHftXFJUgW6ncnfpd5Rq[2GubImgbY5pcWKrdIOgZ4VtdCCpcn;3eIghf2m2aDDETG1GWQ>? NEHST4E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC3Nlc2Oid-MkWwO|I4PTJ:L3G+
Hep3B MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2TvclQxKM7:TR?= MmLiO|IhcA>? M{HvWGROW09? NEnOSZRUgW6ncnfpd5Rq[2GubImgbY5pcWKrdIOgZ4VtdCCpcn;3eIghf2m2aDDETG1GWQ>? NH\kNJM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC3Nlc2Oid-MkWwO|I4PTJ:L3G+
TE-6 MYPGeY5kfGmxbjDBd5NigQ>? NG[zeok2KM7:TR?= NWrH[4ZrOjRiaB?= M{jKdGROW09? NXnacWpCUW6lcnXhd4V{KGmwIHTveYJt\SC|dILhcoQh[nKnYXvzJEhFW0K|KR?= MkHsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR{MUmxOlQoRjJ2MkG5NVY1RC:jPh?=
TE-6 NWPyPFh3TnWwY4Tpc44hSXO|YYm= MVK1JO69VQ>? NVTGO5VOOTJiaB?= MkDPSG1UVw>? NGDDc5RKdmS3Y3XzJGczN01iYYLy[ZN1 MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJzOUG2OEc,OjR{MUmxOlQ9N2F-
HT29 MXfGeY5kfGmxbjDBd5NigQ>? M2PlbFExKG6P NWnR[FRjOTJiaB?= MoD0SG1UVw>? NULoVmhKUW6lcnXhd4V{KESQQTDkc5VjdGVvc4TyZY5lKGK{ZXHrd{BqdmS3Y3XkJIJ6KFOQLUO4 MoPxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3N{e5OFEoRjJ2NUe3PVQyRC:jPh?=
HCT116 MV7GeY5kfGmxbjDBd5NigQ>? NV7uTGNDOTBibl2= NFv2e4IyOiCq NWrTNpNTTE2VTx?= MUXJcoNz\WG|ZYOgSG5CKGSxdXLs[U1{fHKjbnSgZpJm[Wu|IHnu[JVk\WRiYomgV24uOzh? MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV5N{m0NUc,OjR3N{e5OFE9N2F-
RKO NEnZV2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVLtdJhtOTByIN88US=> NHOyN3g1QCCq M3uyU2ROW09? NWDBSZhuWG:2ZX70bYF1\XNiU16tN|gh[3m2b4TvfIlkcXS7 NGDpfWc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW3O|k1OSd-MkS1O|c6PDF:L3G+
C-1 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3e3W|ExOCEQvF2= M2f1TVQ5KGh? NEjEWVdFVVOR M{jZZXBwfGWwdHnheIV{KFOQLUO4JIN6fG:2b4jpZ4l1gQ>? MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV5N{m0NUc,OjR3N{e5OFE9N2F-
SW48 MoP5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXixNFAh|ryP NVHaNHVmPDhiaB?= M1PidmROW09? NUjMNJRUWG:2ZX70bYF1\XNiU16tN|gh[3m2b4TvfIlkcXS7 NU\KXXZDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1O|c6PDFpPkK0OVc4QTRzPD;hQi=>
LoVo NGnQS4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjtZm8yODBizszN MmXKOFghcA>? M{D0XGROW09? NV70d5pRWG:2ZX70bYF1\XNiU16tN|gh[3m2b4TvfIlkcXS7 NGHRUpA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW3O|k1OSd-MkS1O|c6PDF:L3G+
HT29 NWHq[Gc{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFrFZWEyODBizszN MlPJOFghcA>? MWTEUXNQ MXPQc5RmdnSrYYTld{BUVi1|ODDjfZRwfG:6aXPpeJk> MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV5N{m0NUc,OjR3N{e5OFE9N2F-
SW1116 M3XoUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\sdGhKOTByIN88US=> NITqNWI1QCCq MXTEUXNQ Mnm3VI91\W62aXH0[ZMhW05vM{igZ5l1d3SxeHnjbZR6 MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV5N{m0NUc,OjR3N{e5OFE9N2F-
HCT116 NGHmdJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7MNVAxKM7:TR?= NFG4clg1QCCq NXjYR29tTE2VTx?= NX7XbYFLWG:2ZX70bYF1\XNiU16tN|gh[3m2b4TvfIlkcXS7 NYnCOlI5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1O|c6PDFpPkK0OVc4QTRzPD;hQi=>
RKO NIjwWHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PoZ|ExOCEQvF2= Mor0OFghcA>? M3fTcmROW09? MVrJR|UxRTVwOTFOwG0> NV7aWnhwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1O|c6PDFpPkK0OVc4QTRzPD;hQi=>
C-1 NH;wem9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfCNVAxKM7:TR?= MWO0PEBp NGjJfWVFVVOR MXHJR|UxRTdwNjFOwG0> M3TBVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NUe3PVQyLz5{NEW3O|k1OTxxYU6=
SW48 MoDHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4D6eFExOCEQvF2= NEjne|g1QCCq NXLBcmRoTE2VTx?= M4HmTGlEPTB;OT61JO69VQ>? MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV5N{m0NUc,OjR3N{e5OFE9N2F-
HCT-15 NXnRZYxuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPMSoNnOTByIN88US=> NGHkeJg1QCCq M2XMXmROW09? M3n2fWlEPTB;MUCg{txO NXzTdJFMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1O|c6PDFpPkK0OVc4QTRzPD;hQi=>
LoVo M2X4[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVqxNFAh|ryP NHnoeWw1QCCq Mor4SG1UVw>? NYD2V29YUUN3ME2xN{41KM7:TR?= NHy0UGc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW3O|k1OSd-MkS1O|c6PDF:L3G+
HT29 NWS4PY5KT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\vNVAxKM7:TR?= MlTaOFghcA>? NVfCNHNvTE2VTx?= NHjIZ4JKSzVyPUG0Mlch|ryP MkKyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3N{e5OFEoRjJ2NUe3PVQyRC:jPh?=
SW1116 NWTSXYpzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmH0NVAxKM7:TR?= NXLoUlk1PDhiaB?= M4XNSWROW09? NXLY[W5yUUN3ME2xNFAh|ryP MnvmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3N{e5OFEoRjJ2NUe3PVQyRC:jPh?=
HCT116 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU[5Vmg3OTByIN88US=> Mn;4OFghcA>? Mmm3SG1UVw>? MoXhTWM2OD1{LkWg{txO NUnGWlNJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1O|c6PDFpPkK0OVc4QTRzPD;hQi=>
T47D MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXW1JIRigQ>? MULJR|UxRTlwNjFOwG0> MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd4MES5Okc,OjN5NkC0PVY9N2F-
MCF7 M{TkO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXr0clN[PSCmYYm= MX\JR|UxRTVwODFOwG0> M3vyV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{[wOFk3Lz5{M{e2NFQ6PjxxYU6=
CAMA1 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVS1JIRigQ>? MmjCTWM2OD1zNT64JO69VQ>? M3PzRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{[wOFk3Lz5{M{e2NFQ6PjxxYU6=
SUM159 NEOyV2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlz4OUBl[Xl? M4nQeWlEPTB;ND6yJO69VQ>? M2XuUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{[wOFk3Lz5{M{e2NFQ6PjxxYU6=
SKBR3 NU\CVYRTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fFdVUh\GG7 NFfCT3JKSzVyPUGxMlEh|ryP M3qzcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{[wOFk3Lz5{M{e2NFQ6PjxxYU6=
JIMT1 NE\MVm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1PkfFUh\GG7 M4PqcWlEPTB;Nz63JO69VQ>? Ml61QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5NkC0PVYoRjJ|N{[wOFk3RC:jPh?=
BT474 NWKyTZlZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPaOGo2KGSjeR?= MYjJR|UxRTF7Lkig{txO MlTQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5NkC0PVYoRjJ|N{[wOFk3RC:jPh?=
Hs578t(si) MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIX2SmE2KGSjeR?= NXXXXG9sUUN3ME23MlUh|ryP MlXzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5NkC0PVYoRjJ|N{[wOFk3RC:jPh?=
Hs578t NYOwb|JrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2O0UVUh\GG7 MlLHTWM2OD13Lk[g{txO MoDTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5NkC0PVYoRjJ|N{[wOFk3RC:jPh?=
HCC1937 M2T2R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI\OXFA2KGSjeR?= MX7JR|UxRTF{Lk[g{txO NYjLfWc4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3OlA1QTZpPkKzO|YxPDl4PD;hQi=>
HCC1143 M{XTTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGnMVHE2KGSjeR?= MXTJR|UxRTFzLkGg{txO MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd4MES5Okc,OjN5NkC0PVY9N2F-
BT20 NIG0SZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUX1XpprPSCmYYm= NV\mWIpKUUN3ME23Mlch|ryP NUHQR3ZGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3OlA1QTZpPkKzO|YxPDl4PD;hQi=>
MDA-MB-468 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4rVSVUh\GG7 MUfJR|UxRTVwMDFOwG0> M1HzWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{[wOFk3Lz5{M{e2NFQ6PjxxYU6=
MDA-MB-231 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TRT|Uh\GG7 M3v5S2lEPTB;Nj65JO69VQ>? NWjJV2JIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3OlA1QTZpPkKzO|YxPDl4PD;hQi=>
PC-9PTEN− NWHnb2xFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4THSVIxKM7:TR?= MW[xOFQhcA>? MoTFTWM2OD14LkWyJO69VQ>? M1LwbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MkO5PFA6Lz5{M{KzPVgxQTxxYU6=
PC-9 NYr0b49[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjadpo5OjBizszN NW\uNohtOTR2IHi= M1vsW2lEPTB;NT64PEDPxE1? M1vDVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MkO5PFA6Lz5{M{KzPVgxQTxxYU6=
H1650PTEN+ NYPxcW9LT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLtVnczOCEQvF2= MkCzNVQ1KGh? M{\3VmlEPTB;NUCuPFMh|ryP NXHVU5dZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOyN|k5ODlpPkKzNlM6QDB7PD;hQi=>
H1650 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TX[FIxKM7:TR?= NXrG[lNTOTR2IHi= MVTJR|UxRTF3LkS3JO69VQ>? NEmwOII9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{KzPVgxQSd-MkOyN|k5ODl:L3G+
Mouse ATM−/− ES Cells MX7DfZRwfG:6aXOgRZN{[Xl? NHjIfZUzNjVizszN M17ONFIxKGh? M1OzcHNq\26rZnnjZY51dHliaX7obYJqfHNiY3XscEB{fXK4aY\hcC=> NYi4bZhURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzOVU1QDlpPkKzN|U2PDh7PD;hQi=>
Mouse H2AX−/− ES Cells NVv6T5BZS3m2b4TvfIlkKEG|c3H5 M1jQO|IvPSEQvF2= NHPDPIwzOCCq M4LVe3Nq\26rZnnjZY51dHliaX7obYJqfHNiY3XscEB{fXK4aY\hcC=> NYD2U5lFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzOVU1QDlpPkKzN|U2PDh7PD;hQi=>
VCaP MUnJcpZie2m4ZTDBd5NigQ>? MWCyOUDPxE1? NFzzbpQ1QCCq MX3EUXNQ NWLwWnlyW2mpbnnmbYNidnSueTDy[YR2[2W|IFXSS{1lemm4ZX6gZ4VtdCCrbo\hd4lwdg>? MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTV5NUi2OUc,OjF3N{W4OlU9N2F-
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BB30-HNC NHL0dFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPQO4ZKSzVyPUS4MlMxPzJizszN MoTYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVIyPjh4Lze+V2FPT0WUPD;hQi=>
T98G M2TBN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTR6LkS2N|Mh|ryP M1vTclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFUzOTZ6Nj:nQnNCVkeHUkyvZV4>
NCI-H1573 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLoTWM2OD12OT60OFYzKM7:TR?= M1nSWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFUzOTZ6Nj:nQnNCVkeHUkyvZV4>
MEG-01 NXPScotGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTR7Lke0NVEh|ryP NWrQUnJxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTJzNki2M{c,W0GQR1XSQE9iRg>?
WM-115 M{H2Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnv1TWM2OD12OT65NlIzKM7:TR?= MmXPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVIyPjh4Lze+V2FPT0WUPD;hQi=>

... 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)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

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)

  • Mass
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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 SDS / 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
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / 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
NCT04972110 Recruiting Drug: RP-3500 Advanced Solid Tumor Adult Repare Therapeutics July 21 2021 Phase 1|Phase 2
NCT04644289 Not yet recruiting Drug: olaparib|Drug: durvalumab Epithelial Ovarian Cancer AGO Research GmbH July 2021 Phase 2
NCT04884360 Recruiting Drug: Olaparib|Other: Matching placebo Ovarian Cancer AstraZeneca May 31 2021 Phase 3
NCT04858334 Recruiting Drug: Olaparib|Drug: Placebo Administration Pancreatic Acinar Cell Carcinoma|Pancreatic Adenosquamous Carcinoma|Pancreatic Carcinoma|Pancreatic Squamous Cell Carcinoma|Resectable Pancreatic Acinar Cell Carcinoma|Resectable Pancreatic Adenocarcinoma|Resectable Pancreatic Adenosquamous Carcinoma|Resectable Pancreatic Carcinoma|Stage 0 Pancreatic Cancer AJCC v8|Stage I Pancreatic Cancer AJCC v8|Stage IA Pancreatic Cancer AJCC v8|Stage IB Pancreatic Cancer AJCC v8|Stage II Pancreatic Cancer AJCC v8|Stage IIA Pancreatic Cancer AJCC v8|Stage IIB Pancreatic Cancer AJCC v8 National Cancer Institute (NCI) April 29 2021 Phase 2

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.

  • 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.

  • Blasticidin S HCl New

    Blasticidin S HCl is a nucleoside antibiotic isolated from Stretomyces girseochromogenes, and acts as a DNA and protein synthesis inhibitor, used to select transfected cells carrying bsr or BSD resistance genes.

  • 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.

  • 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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID