Olaparib (AZD2281)

Catalog No.S1060 Synonyms: Ku-0059436

For research use only.

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.

Olaparib (AZD2281) Chemical Structure

CAS No. 763113-22-0

Selleck's Olaparib (AZD2281) has been cited by 878 publications

Purity & Quality Control

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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 MljNSpVv[3Srb36gRZN{[Xl? M4O5TFQxKM7:TR?= NIK2eJQzPCCq NW\4[mhZTE2VTx?= MWnJcoR2[2W|IGLPV{Bxem:mdXP0bY9vKHerdHigSGhOTVF? NWm5e2d1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwO|I4PTJpPkK1NFczPzV{PD;hQi=>
Huh7 NIG4dYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;HOG41OCEQvF2= M2j5SVczKGh? MYnEUXNQ Mke1V5lv\XKpaYP0bYNidGy7IHnubIljcXS|IHPlcIwh\3Kxd4ToJJdqfGhiRFjNSXE> MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB5Mke1Nkc,OjVyN{K3OVI9N2F-
Hep3B M{fXdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7xOFAh|ryP MVe3NkBp Mn7FSG1UVw>? MWrTfY5memerc4TpZ4FtdHliaX7obYJqfHNiY3XscEBoem:5dHige4l1cCCGSF3FVS=> NVfmVGFyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwO|I4PTJpPkK1NFczPzV{PD;hQi=>
TE-6 NFi3eXdHfW6ldHnvckBCe3OjeR?= NYnINldjPSEQvF2= NHT4bXMzPCCq NW\BXZZLTE2VTx?= NVn4ToVJUW6lcnXhd4V{KGmwIHTveYJt\SC|dILhcoQh[nKnYXvzJEhFW0K|KR?= M{DuTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MkG5NVY1Lz5{NEKxPVE3PDxxYU6=
TE-6 NYHjSHhzTnWwY4Tpc44hSXO|YYm= NH6xWYs2KM7:TR?= MkS2NVIhcA>? Mkj4SG1UVw>? NHW1cWtKdmS3Y3XzJGczN01iYYLy[ZN1 MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJzOUG2OEc,OjR{MUmxOlQ9N2F-
HT29 MX;GeY5kfGmxbjDBd5NigQ>? NWjjXGQyOTBibl2= M4LPO|EzKGh? NUfGXGhGTE2VTx?= NH7hfWtKdmO{ZXHz[ZMhTE6DIHTveYJt\S2|dILhcoQh[nKnYXvzJIlv\HWlZXSgZpkhW05vM{i= NHHLbHQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW3O|k1OSd-MkS1O|c6PDF:L3G+
HCT116 MlTSSpVv[3Srb36gRZN{[Xl? NWLJbYx{OTBibl2= MoP0NVIhcA>? NVjF[XJMTE2VTx?= NIDtcWtKdmO{ZXHz[ZMhTE6DIHTveYJt\S2|dILhcoQh[nKnYXvzJIlv\HWlZXSgZpkhW05vM{i= NFTYTlM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW3O|k1OSd-MkS1O|c6PDF:L3G+
RKO NIO4dplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjGXGl{OTByIN88US=> NEnDZnc1QCCq M3vzcGROW09? M4DzfXBwfGWwdHnheIV{KFOQLUO4JIN6fG:2b4jpZ4l1gQ>? M4D0OFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NUe3PVQyLz5{NEW3O|k1OTxxYU6=
C-1 M3zB[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVixNFAh|ryP MYK0PEBp MYDEUXNQ MX7Qc5RmdnSrYYTld{BUVi1|ODDjfZRwfG:6aXPpeJk> MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV5N{m0NUc,OjR3N{e5OFE9N2F-
SW48 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\TdppQOTByIN88US=> MoHjOFghcA>? MlfZSG1UVw>? MYTQc5RmdnSrYYTld{BUVi1|ODDjfZRwfG:6aXPpeJk> NHHiSII9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW3O|k1OSd-MkS1O|c6PDF:L3G+
LoVo M3:5cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPycI9kOTByIN88US=> NIfsR3E1QCCq MWXEUXNQ MnXVVI91\W62aXH0[ZMhW05vM{igZ5l1d3SxeHnjbZR6 NH7rWpU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW3O|k1OSd-MkS1O|c6PDF:L3G+
HT29 NWrSOpVmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWDTVpJ1OTByIN88US=> MVy0PEBp NVz3e2tlTE2VTx?= NYXGbplTWG:2ZX70bYF1\XNiU16tN|gh[3m2b4TvfIlkcXS7 MlP4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3N{e5OFEoRjJ2NUe3PVQyRC:jPh?=
SW1116 NFX4VmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;hOGEyODBizszN M3zybFQ5KGh? NXn5VoRRTE2VTx?= NGfHVXlRd3SnboTpZZRmeyCVTj2zPEBkgXSxdH;4bYNqfHl? NGnMNo89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW3O|k1OSd-MkS1O|c6PDF:L3G+
HCT116 NGnMOXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;GWYlbOTByIN88US=> NFXXe5I1QCCq NYOwfIJnTE2VTx?= Moq3VI91\W62aXH0[ZMhW05vM{igZ5l1d3SxeHnjbZR6 M13KdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NUe3PVQyLz5{NEW3O|k1OTxxYU6=
RKO NX7RflNGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\SNVAxKM7:TR?= Ml\2OFghcA>? NVzle2N4TE2VTx?= NIPLXZNKSzVyPUWuPUDPxE1? MmD1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3N{e5OFEoRjJ2NUe3PVQyRC:jPh?=
C-1 Ml3uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoL6NVAxKM7:TR?= MlqxOFghcA>? M4ntcGROW09? MVjJR|UxRTdwNjFOwG0> MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV5N{m0NUc,OjR3N{e5OFE9N2F-
SW48 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjCSmM6OTByIN88US=> NUjmO2VYPDhiaB?= MX3EUXNQ NWHkbZhRUUN3ME25MlUh|ryP M2W4[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NUe3PVQyLz5{NEW3O|k1OTxxYU6=
HCT-15 NW\OSYhpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYSxNFAh|ryP M{PPWlQ5KGh? M2HvdmROW09? M3PzWmlEPTB;MUCg{txO NIjQfVM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW3O|k1OSd-MkS1O|c6PDF:L3G+
LoVo Mn33S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LWOlExOCEQvF2= MoXJOFghcA>? NIT3SHdFVVOR M3jmN2lEPTB;MUOuOEDPxE1? Moj0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3N{e5OFEoRjJ2NUe3PVQyRC:jPh?=
HT29 M4PNWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHOySZUyODBizszN NUTLVolOPDhiaB?= M3\1RmROW09? MnjkTWM2OD1zND63JO69VQ>? MoPhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3N{e5OFEoRjJ2NUe3PVQyRC:jPh?=
SW1116 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;hNVAxKM7:TR?= M4nmOFQ5KGh? M13TUWROW09? M{fKeWlEPTB;MUCwJO69VQ>? NWD5W4hLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1O|c6PDFpPkK0OVc4QTRzPD;hQi=>
HCT116 NXzVOVZVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1rMV|ExOCEQvF2= NEnMXIo1QCCq NXrONpdnTE2VTx?= NWDzVJUzUUN3ME2yMlUh|ryP NE\VUG89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW3O|k1OSd-MkS1O|c6PDF:L3G+
T47D M2XSeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nn[FUh\GG7 MXzJR|UxRTlwNjFOwG0> M4LxWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{[wOFk3Lz5{M{e2NFQ6PjxxYU6=
MCF7 M4rSOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWS1JIRigQ>? NYjwNZU2UUN3ME21Mlgh|ryP NI[3V|g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{e2NFQ6Pid-MkO3OlA1QTZ:L3G+
CAMA1 NV[zb|JQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPne3NlPSCmYYm= M3PBTGlEPTB;MUWuPEDPxE1? MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd4MES5Okc,OjN5NkC0PVY9N2F-
SUM159 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUm1JIRigQ>? MXHJR|UxRTRwMjFOwG0> M2LabFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{[wOFk3Lz5{M{e2NFQ6PjxxYU6=
SKBR3 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnO4OUBl[Xl? NIfCZ2xKSzVyPUGxMlEh|ryP NHLZbno9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{e2NFQ6Pid-MkO3OlA1QTZ:L3G+
JIMT1 NX3rcpFiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUK1JIRigQ>? MV7JR|UxRTdwNzFOwG0> NVf1dnd2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3OlA1QTZpPkKzO|YxPDl4PD;hQi=>
BT474 NWHQc5pRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4Dvb|Uh\GG7 Ml7BTWM2OD1zOT64JO69VQ>? NHHk[mY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{e2NFQ6Pid-MkO3OlA1QTZ:L3G+
Hs578t(si) M2XGPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUK1JIRigQ>? MUPJR|UxRTdwNTFOwG0> MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd4MES5Okc,OjN5NkC0PVY9N2F-
Hs578t MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVq1JIRigQ>? Mm\wTWM2OD13Lk[g{txO M{C4XVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{[wOFk3Lz5{M{e2NFQ6PjxxYU6=
HCC1937 NF:xNnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXG1JIRigQ>? NEnFOYZKSzVyPUGyMlYh|ryP NVjxTWtLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3OlA1QTZpPkKzO|YxPDl4PD;hQi=>
HCC1143 NV\2R3RWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVW1JIRigQ>? M3WzUGlEPTB;MUGuNUDPxE1? NFvQTIk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{e2NFQ6Pid-MkO3OlA1QTZ:L3G+
BT20 M4LwO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHrpOGY2KGSjeR?= NUTrbnZ6UUN3ME23Mlch|ryP MliwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5NkC0PVYoRjJ|N{[wOFk3RC:jPh?=
MDA-MB-468 NGPXTFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYmyVFVwPSCmYYm= MWHJR|UxRTVwMDFOwG0> MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd4MES5Okc,OjN5NkC0PVY9N2F-
MDA-MB-231 NGP1fm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfDOW1PPSCmYYm= MmH1TWM2OD14Lkmg{txO MkjJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5NkC0PVYoRjJ|N{[wOFk3RC:jPh?=
PC-9PTEN− MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXuyNEDPxE1? MUixOFQhcA>? MoPZTWM2OD14LkWyJO69VQ>? NGfXbIY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{KzPVgxQSd-MkOyN|k5ODl:L3G+
PC-9 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPvbWozOCEQvF2= MljnNVQ1KGh? NYfhfmg3UUN3ME21Mlg5KM7:TR?= MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzJ|OUiwPUc,OjN{M{m4NFk9N2F-
H1650PTEN+ NV\jSYx[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vSfFIxKM7:TR?= MWKxOFQhcA>? NYHMdpFYUUN3ME21NE45OyEQvF2= MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzJ|OUiwPUc,OjN{M{m4NFk9N2F-
H1650 NGPWboFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLje21NOjBizszN NUDDWY1HOTR2IHi= M{\NUmlEPTB;MUWuOFch|ryP NVPlWJZWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOyN|k5ODlpPkKzNlM6QDB7PD;hQi=>
Mouse ATM−/− ES Cells MmTCR5l1d3SxeHnjJGF{e2G7 MV:yMlUh|ryP NUH6co9[OjBiaB?= M1jPXXNq\26rZnnjZY51dHliaX7obYJqfHNiY3XscEB{fXK4aY\hcC=> MmDxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|NUW0PFkoRjJ|M{W1OFg6RC:jPh?=
Mouse H2AX−/− ES Cells MlTQR5l1d3SxeHnjJGF{e2G7 MnfXNk42KM7:TR?= MkDHNlAhcA>? NGLVNXpUcWewaX\pZ4FvfGy7IHnubIljcXS|IHPlcIwhe3W{dnn2ZYw> NEP3Nmw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O1OVQ5QSd-MkOzOVU1QDl:L3G+
VCaP NV7NPXJHUW64YYPpeoUhSXO|YYm= NYDweoYzOjVizszN MXu0PEBp NGrMcppFVVOR MnjVV4lodmmoaXPhcpRtgSC{ZXT1Z4V{KEWURz3kdol3\W5iY3XscEBqdn[jc3nvci=> NIO0WG09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3OVg3PSd-MkG1O|U5PjV:L3G+
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WM-115 NEjYcJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXHTWM2OD12OT65NlIzKM7:TR?= NEXaeno9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2OjF4OE[vK|5USU6JRWK8M4E,
Assay
Methods Test Index PMID
Western Blot DR5/CHOP ; γH2AX/H2AX ; pATM ; 53BP1 ; NF-kB ; pS6/S6 25531448 22933245 27686740 24831086
Immunofluorescence DNA damage ; γH2AX 27686740 28069876
Growth inhibition assay Cell viability 25531448
ELISA IL-8 ; GLP-1 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 (from reference)

Kinase Assay:

[1]

  • 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]

  • 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.

Animal Research:

[3]

  • 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

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 434.46
Formula

C24H23FN4O3

CAS No. 763113-22-0
Storage 3 years -20°C powder
2 years -80°C in solvent
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)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05153603 Not yet recruiting Drug: Olaparib mono-maintenance therapy Ovarian Neoplasms Sun Yat-Sen Memorial Hospital of Sun Yat-Sen University April 2022 --
NCT05128734 Not yet recruiting Drug: Temozolomide|Drug: Olaparib Breast Cancer Triple Negative AHS Cancer Control Alberta April 1 2022 Phase 2
NCT04644289 Not yet recruiting Drug: olaparib|Drug: durvalumab Epithelial Ovarian Cancer AGO Research GmbH January 2022 Phase 2
NCT05078671 Not yet recruiting Drug: Olaparib|Drug: Cobicistat Cancer Radboud University October 15 2021 Phase 4

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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

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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.

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