Olaparib (AZD2281, Ku-0059436)

Catalog No.S1060

Olaparib (AZD2281, Ku-0059436) Chemical Structure

Molecular Weight(MW): 434.46

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.

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Cited by 119 Publications

Purity & Quality Control

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.
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
KP3.33 NX7C[Ip6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUW0JIQ> NF;ScGtKSzVyPUWuO|A2KCEQvF2g Mn;2NVg2PTl4MUO=
KP6.3 M3jacmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPyOEBl M{LuZWlEPTB;MUCuOFI5KM7:TTC= Mlj5NVg2PTl4MUO=
KP7.7 NHu2[VFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnK2OEBl MWHJR|UxRTV5IH7NJC=> M4H1cVE5PTV7NkGz
KB2P3.4 NFLicJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE[yU5M1KGR? M3K3RmlEPTB;MUK0JG0h MXqxPFU2QTZzMx?=
KB2P1.21 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M160UVQh\A>? NEG0cJJKSzVyPUi5NFchdk1i M2G1NFE5PTV7NkGz
U373-MG NYLNVFlmS3m2b4TvfIlkKEG|c3H5 M4DqSFEh|ryPIB?= M{D2flI1KGh? NGjhNmVKdmO{ZXHz[ZMhemGmaXH0bY9vKHOnboPpeIl3cXS7 M{f4elE5QTV2N{Gy
T98G MkP6R5l1d3SxeHnjJGF{e2G7 M4iyWlEh|ryPIB?= NG\UVYszPCCq MX3JcoNz\WG|ZYOgdoFlcWG2aX;uJJNmdnOrdHn2bZR6 NXu2U3BTOTh7NUS3NVI>
U87-MG NVHDU5VtS3m2b4TvfIlkKEG|c3H5 M3rHfFEh|ryPIB?= NF3FbmszPCCq M4H0R2lv[3KnYYPld{Bz[WSrYYTpc44he2Wwc3n0bZZqfHl? MY[xPFk2PDdzMh?=
UVW M1;x[GN6fG:2b4jpZ{BCe3OjeR?= NFOxcoM2ODBibl2= MorXNlQhcA>? NGDDbnFKdmO{ZXHz[ZMhemGmaXH0bY9vKHOnboPpeIl3cXS7 MojLNVg6PTR5MUK=
HeLa NEDu[YtHfW6ldHnvckBCe3OjeR?= MkWxOVAxKG6P MWe0JIg> MXXDZZV{\XNiYTDtc4Rme3RiZHXsZZkhcW5icnXqc4lvcW6pIH;mJJJi\GmjdHnvck1qdmS3Y3XkJGRPSSCkcnXhb5M> MXyxPFk2PDdzMh?=
HeLa NX3UXHp7TnWwY4Tpc44hSXO|YYm= NX7lV4JEOSEQvF2g NV;WdnBIOjRiaB?= Mk[1SY5p[W6lZYOgdoFlcWG2aX;uMYlv\HWlZXSgV{1xcGG|ZTDhdpJme3R? MUmxPFk2PDdzMh?=
T98G Mlr6SpVv[3Srb36gRZN{[Xl? MmD0NUDPxE1i M4rWeFI1KGh? MlXNSY5p[W6lZYOgdoFlcWG2aX;uMYlv\HWlZXSgV{1xcGG|ZTDhdpJme3R? NVXGO2FOOTh7NUS3NVI>
L3 Mn76R5l1d3SxeHnjJGF{e2G7 Mli5OUDPxE1i MYW5OkBp NWf2WJNoTE2VTx?= MWPTbYdvcW[rY3HueIx6KGmwaHnibZR{KGOnbHygd5Vzfmm4YXy= Mk\2NlAyOjR2NUm=
Granta-519 MonUR5l1d3SxeHnjJGF{e2G7 MUG1JO69VSB? MoDaPVYhcA>? M1fWfGROW09? NWHIRW1SW2yrZ3j0cJkhcW6qaXLpeJMh[2WubDDzeZJ3cX[jbB?= MofoNlAyOjR2NUm=
BT NWj1OlljS3m2b4TvfIlkKEG|c3H5 Mon5OUDPxE1i NEjWN406PiCq NYm0UYNvTE2VTx?= NX35XWd1W2yrZ3j0cJkhcW6qaXLpeJMh[2WubDDzeZJ3cX[jbB?= M17FUFIxOTJ2NEW5
UPN2 MkPmR5l1d3SxeHnjJGF{e2G7 M{GwbVUh|ryPIB?= NGfsS2Y6PiCq NHOyWm5FVVOR NIHQU4tUdGmpaITsfUBqdmirYnn0d{Bk\WyuIIP1dpZqfmGu NGLkfIozODF{NES1PS=>
HBL-2 NXO0WVJ6S3m2b4TvfIlkKEG|c3H5 M4jpVFUh|ryPIB?= MojaPVYhcA>? MnXGSG1UVw>? NY\vSXI4W2yrZ3j0cJkhcW6qaXLpeJMh[2WubDDzeZJ3cX[jbB?= MofyNlAyOjR2NUm=
JVM-2 M3HPXmN6fG:2b4jpZ{BCe3OjeR?= NIDMZnY2KM7:TTC= NIfmSmc6PiCq NXPENJFOTE2VTx?= Mk\YV4xq\2i2bImgbY5pcWKrdIOgZ4VtdCC|dYL2bZZidA>? MUiyNFEzPDR3OR?=
Z138 NUGwSWdmS3m2b4TvfIlkKEG|c3H5 MWq1JO69VSB? MmP2PVYhcA>? M{S2bWROW09? NVO1RmhXW2yrZ3j0cJkhcW6qaXLpeJMh[2WubDDzeZJ3cX[jbB?= M4fHblIxOTJ2NEW5
RWPE M{jXd2lvfmG|aY\lJGF{e2G7 NV:zRYNGOjVizszN NIPrRpo1QCCq NF7zSWFFVVOR NYLhUnNrW2mpbnnmbYNidnSueTDy[YR2[2W|IFXSS{1lemm4ZX6gZ4VtdCCrbo\hd4lwdg>? M3H3[FIyPTd3OE[1
VCaP MkfsTY53[XOrdnWgRZN{[Xl? M2njblI2KM7:TR?= M161W|Q5KGh? NVLHe4p[TE2VTx?= NHeyS5FUcWewaX\pZ4FvfGy7IILl[JVk\XNiRWLHMYRzcX[nbjDj[YxtKGmwdnHzbY9v M2XTWFIyPTd3OE[1
Mouse H2AX−/− ES Cells MXfDfZRwfG:6aXOgRZN{[Xl? MWKyMlUh|ryP MlnuNlAhcA>? NF3UZXdUcWewaX\pZ4FvfGy7IHnubIljcXS|IHPlcIwhe3W{dnn2ZYw> NH\zbWEzOzN3NUS4PS=>
Mouse ATM−/− ES Cells NXSyXnBnS3m2b4TvfIlkKEG|c3H5 M{LLUlIvPSEQvF2= MoDZNlAhcA>? M{jrXXNq\26rZnnjZY51dHliaX7obYJqfHNiY3XscEB{fXK4aY\hcC=> M3W4S|I{OzV3NEi5
H1650 NYXPTmdzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{X5XVIxKM7:TR?= MXSxOFQhcA>? NWnN[nRiUUN3ME2xOU41PyEQvF2= M{jlcFI{OjN7OEC5
H1650PTEN+ NHXvbJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWCxc3dYOjBizszN MVuxOFQhcA>? NYHWeJJSUUN3ME21NE45OyEQvF2= Ml7qNlMzOzl6MEm=
PC-9 NIPMUHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlOzNlAh|ryP M1W1VlE1PCCq NIT0VodKSzVyPUWuPFgh|ryP MormNlMzOzl6MEm=
PC-9PTEN− NX\POoU1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHrdGtZOjBizszN NE\QW3UyPDRiaB?= MoL0TWM2OD14LkWyJO69VQ>? MW[yN|I{QThyOR?=
MDA-MB-231 Mor5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnVVVA2KGSjeR?= NE\BU21KSzVyPU[uPUDPxE1? NVzab2kzOjN5NkC0PVY>
MDA-MB-468 MkXrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33BbFUh\GG7 NHi3S2FKSzVyPUWuNEDPxE1? NFfBZYkzOzd4MES5Oi=>
BT20 M2r6NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1H4XVUh\GG7 M3yxW2lEPTB;Nz63JO69VQ>? NX;WN5U1OjN5NkC0PVY>
HCC1143 NGrZSZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfZOUBl[Xl? MmXXTWM2OD1zMT6xJO69VQ>? MVWyN|c3ODR7Nh?=
HCC1937 NVz5OnhXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLxfJI2KGSjeR?= M{jRemlEPTB;MUKuOkDPxE1? MXSyN|c3ODR7Nh?=
Hs578t M3vibWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXy1JIRigQ>? MkflTWM2OD13Lk[g{txO NVHZO4N{OjN5NkC0PVY>
Hs578t(si) Mn30S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX62U3pGPSCmYYm= MmfnTWM2OD15LkWg{txO MYeyN|c3ODR7Nh?=
BT474 NGL3PYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml;iOUBl[Xl? MkToTWM2OD1zOT64JO69VQ>? NIXxSWwzOzd4MES5Oi=>
JIMT1 MkflS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7zWVVmPSCmYYm= MVrJR|UxRTdwNzFOwG0> NIG2PJozOzd4MES5Oi=>
SKBR3 NVHLcmd1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\1OUBl[Xl? NXTXZllYUUN3ME2xNU4yKM7:TR?= MXWyN|c3ODR7Nh?=
SUM159 Mnz3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEnsNGo2KGSjeR?= M3HndmlEPTB;ND6yJO69VQ>? M2fkW|I{PzZyNEm2
CAMA1 NHzCXm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVy1JIRigQ>? NFLlVnRKSzVyPUG1Mlgh|ryP MYmyN|c3ODR7Nh?=
MCF7 NV3Gc|AxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DmT|Uh\GG7 NVjuT2pwUUN3ME21Mlgh|ryP MlrJNlM4PjB2OU[=
T47D NYrkbXZWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWq3Npg5PSCmYYm= MkL1TWM2OD17Lk[g{txO NHrCW5YzOzd4MES5Oi=>
HCT116 NHrSOlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX6xNFAh|ryP M3m3dlQ5KGh? NHXGN2VFVVOR NFm2O|BKSzVyPUKuOUDPxE1i MUiyOFU4Pzl2MR?=
SW1116 M{PuO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4THWlExOCEQvF2= M4q3NFQ5KGh? NGTKU4FFVVOR M{nZU2lEPTB;MUCwJO69VQ>? MnjLNlQ2Pzd7NEG=
HT29 MkP6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjBVmRYOTByIN88US=> NVPrNlM5PDhiaB?= M1HiUWROW09? MXHJR|UxRTF2Lkeg{txO MoPTNlQ2Pzd7NEG=
LoVo NUK1bmpbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV6xNFAh|ryP M3zwWVQ5KGh? NGnlSGZFVVOR MYLJR|UxRTF|LkSg{txO NUDMN2d7OjR3N{e5OFE>
HCT-15 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUmxNFAh|ryP Ml;KOFghcA>? NYj5T|A4TE2VTx?= NYnab5pKUUN3ME2xNEDPxE1? NXG4VlhsOjR3N{e5OFE>
SW48 MmPmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzoZ|YyODBizszN MXG0PEBp M2LCb2ROW09? NV[2blNUUUN3ME25MlUh|ryP MnHhNlQ2Pzd7NEG=
C-1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHKc4IyODBizszN M13k[lQ5KGh? NWr4bGZ4TE2VTx?= M3;BSWlEPTB;Nz62JO69VQ>? NHzqU5QzPDV5N{m0NS=>
RKO MnGzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTlNVAxKM7:TR?= NIru[HA1QCCq M1\6eGROW09? Mn\0TWM2OD13Lkmg{txO NWfwT2NkOjR3N{e5OFE>
HCT116 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUOxNFAh|ryP MW[0PEBp MXfEUXNQ NF7vdXhRd3SnboTpZZRmeyCVTj2zPEBkgXSxdH;4bYNqfHli M2nzOFI1PTd5OUSx
SW1116 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2P4[VExOCEQvF2= M3foZ|Q5KGh? MXPEUXNQ M2G4UXBwfGWwdHnheIV{KFOQLUO4JIN6fG:2b4jpZ4l1gSB? M2HoNlI1PTd5OUSx
HT29 NI\qTYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\oZlYyODBizszN M3LzUVQ5KGh? NGXETFJFVVOR MXnQc5RmdnSrYYTld{BUVi1|ODDjfZRwfG:6aXPpeJkh MX:yOFU4Pzl2MR?=
LoVo MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvPOHQyODBizszN M4LtOVQ5KGh? NH70eWxFVVOR MWHQc5RmdnSrYYTld{BUVi1|ODDjfZRwfG:6aXPpeJkh NGP6emszPDV5N{m0NS=>
SW48 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUixNFAh|ryP M2\RSVQ5KGh? NVO2S|J2TE2VTx?= MV7Qc5RmdnSrYYTld{BUVi1|ODDjfZRwfG:6aXPpeJkh M3zIeFI1PTd5OUSx
C-1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfTfo1vOTByIN88US=> NIe1WVE1QCCq MmLzSG1UVw>? MnLVVI91\W62aXH0[ZMhW05vM{igZ5l1d3SxeHnjbZR6KA>? Mlj6NlQ2Pzd7NEG=
RKO NF3VU2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M133bVExOCEQvF2= MlHLOFghcA>? Ml;qSG1UVw>? M4LONnBwfGWwdHnheIV{KFOQLUO4JIN6fG:2b4jpZ4l1gSB? Ml\TNlQ2Pzd7NEG=
HCT116 M4SzO2Z2dmO2aX;uJGF{e2G7 MnLoNVAhdk1? MV[xNkBp Mn3ZSG1UVw>? MkexTY5kemWjc3XzJGRPSSCmb4XicIUue3S{YX7kJIJz\WGtczDpcoR2[2WmIHL5JHNPNTN6 MVmyOFU4Pzl2MR?=
HT29 MoXrSpVv[3Srb36gRZN{[Xl? NYPYXVQ4OTBibl2= NEW4UHAyOiCq M3LrTWROW09? NH3oXpVKdmO{ZXHz[ZMhTE6DIHTveYJt\S2|dILhcoQh[nKnYXvzJIlv\HWlZXSgZpkhW05vM{i= NVH2dVlvOjR3N{e5OFE>
TE-6 Mny3SpVv[3Srb36gRZN{[Xl? NXvOPVU1PSEQvF2g Ml;KNVIhcA>? NYfkV5Z7TE2VTx?= MoPVTY5lfWOnczDHNk9OKGG{cnXzeC=> MoXQNlQzOTlzNkS=
TE-6 M4nOUWZ2dmO2aX;uJGF{e2G7 MkjQOUDPxE1i NVnnUJR{OjRiaB?= MYrEUXNQ NXf0OlZrUW6lcnXhd4V{KGmwIHTveYJt\SC|dILhcoQh[nKnYXvzJEhFW0K|KR?= MUmyOFIyQTF4NB?=
Hep3B M4j4cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX20NEDPxE1i NWLRVpRUPzJiaB?= MkDOSG1UVw>? M2XlZXN6dmW{Z3nzeIlk[WyueTDpcohq[mm2czDj[YxtKGe{b4f0bEB4cXSqIFTIUWVS MoTWNlUxPzJ5NUK=
Huh7 M2joe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYO0NEDPxE1i NIf6Zok4OiCq NIL0fYxFVVOR MXTTfY5memerc4TpZ4FtdHliaX7obYJqfHNiY3XscEBoem:5dHige4l1cCCGSF3FVS=> NXLXN2o3OjVyN{K3OVI>
Hep3B M3exfmZ2dmO2aX;uJGF{e2G7 M1rkZVQxKM7:TTC= NFG3e2kzPCCq NWDZOW1bTE2VTx?= NV72eHhDUW6mdXPld{BTV1NicILv[JVkfGmxbjD3bZRpKESKTVXR MlrHNlUxPzJ5NUK=
Huh7 NGPZ[XBHfW6ldHnvckBCe3OjeR?= M1nrSVQxKM7:TTC= M1rqT|I1KGh? M{PMT2ROW09? NVzvT4FDUW6mdXPld{BTV1NicILv[JVkfGmxbjD3bZRpKESKTVXR NIT5WZAzPTB5Mke1Ni=>
Hep3B M1LOcGZ2dmO2aX;uJGF{e2G7 M4nnNFQxKM7:TTC= NICz[IUzPCCq NGLmS2VFVVOR M{X6Wmlv\HWlZYOgZ4VtdCCjdYTvdIhi\3lid3n0bEBFUE2HUR?= MVWyOVA4Ojd3Mh?=
Huh7 M3Xid2Z2dmO2aX;uJGF{e2G7 MnzHOFAh|ryPIB?= MWGyOEBp M4\qS2ROW09? NXnH[4xOUW6mdXPld{Bk\WyuIHH1eI9xcGGpeTD3bZRpKESKTVXR MX6yOVA4Ojd3Mh?=
SGC-7901 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXPOOVFEOzEEoN88US=> MYq0PEBp Mo\nSG1UVw>? NGm1fVBDdG:lazDvfIFtcXCuYYTpck1qdmS3Y3XkJINmdGxiZHXheIg> MljLNlU4PjdyN{[=
COLO-800 M3qxbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPaXmtWUUN3ME2wMlQ1OTZ2IN88US=> NW\zOm9JW0GQR1XS
EoL-1- Mk\MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;NSVlKSzVyPUCuOVY1PDZizszN MVrTRW5ITVJ?
NCI-H209 MofjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTBwOUG1OVYh|ryP NWfnRYlWW0GQR1XS
ES1 M2CwN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmL0TWM2OD1zLkGxOFA5KM7:TR?= MVHTRW5ITVJ?
NKM-1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnTsTWM2OD1zLkK1N|Q4KM7:TR?= MWXTRW5ITVJ?
NTERA-S-cl-D1 NHTwOpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1rDNmlEPTB;MT6zN|M1OSEQvF2= Mk\6V2FPT0WU
MHH-ES-1 NFvUVlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13FNWlEPTB;MT62NlA3PyEQvF2= Mn7OV2FPT0WU
ES8 MmnsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnn1TWM2OD1zLkeyOFE1KM7:TR?= MkPGV2FPT0WU
NCI-H720 NVPNPW51T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTJwMkC2PVkh|ryP NGe5VnNUSU6JRWK=
EW-3 NEGwZY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTJwMke1N|Qh|ryP M3;FcnNCVkeHUh?=
D-566MG MnSyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV75bVRjUUN3ME2yMlQ1PTZ6IN88US=> MXzTRW5ITVJ?
697 NXWzUow2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTJwOESxO|Mh|ryP MUjTRW5ITVJ?
ES5 NXjvXWxvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXGOGpKSzVyPUKuPFgyQDlizszN M{Lr[nNCVkeHUh?=
COLO-684 NFfKcGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnjTWM2OD1|LkWxOlk3KM7:TR?= M{PIZXNCVkeHUh?=
ML-2 NILPc41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTNwNkCwOVgh|ryP NF[xcopUSU6JRWK=
MC-IXC NV3pUmJZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFztN2lKSzVyPUOuOlM{QTNizszN MWfTRW5ITVJ?
DB MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrETWM2OD1|Lk[1OFQ5KM7:TR?= MYTTRW5ITVJ?
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MFM-223 NYfKUlN1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\QNFBIUUN3ME20OE4yOjJ6IN88US=> NV7SPIxqW0GQR1XS
OAW-42 NUn1T3BHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;QRmlEPTB;NESuNlY1OyEQvF2= NV;2TWtFW0GQR1XS
C8166 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnqOVh7UUN3ME20OU4xQDJ{IN88US=> M3XDOHNCVkeHUh?=
LU-99A NF7ETYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\2ZpZlUUN3ME20Ok4yOzJ{IN88US=> MYnTRW5ITVJ?
NCI-H23 Mn\wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zrOWlEPTB;NE[uNVc5PSEQvF2= NVHh[mhlW0GQR1XS
HO-1-N-1 NXP2WHI4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHz1[|NKSzVyPUS3MlA6QThizszN NE\ZOFNUSU6JRWK=
A3-KAW NF;DW3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{LoVmlEPTB;NEeuNVAxPyEQvF2= NET2cXNUSU6JRWK=
CGTH-W-1 NU\h[IRTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3JR|UxRTR5LkWwOlkh|ryP MVPTRW5ITVJ?
DJM-1 M4CzO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXSTWM2OD12Nz61OFE{KM7:TR?= NV\FU5poW0GQR1XS
A101D MlTpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTR5Lk[zOVch|ryP NITpZ3FUSU6JRWK=
BB30-HNC M{f6dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLzNmUzUUN3ME20PE4{ODd{IN88US=> MX;TRW5ITVJ?
T98G MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTR6LkS2N|Mh|ryP NEjzR41USU6JRWK=
NCI-H1573 NF\tPXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\GTWM2OD12OT60OFYzKM7:TR?= MoDRV2FPT0WU
MEG-01 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\DPFFKSzVyPUS5Mlc1OTFizszN M13qU3NCVkeHUh?=
WM-115 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH31NHBKSzVyPUS5MlkzOjJizszN NF\Re3JUSU6JRWK=

... 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]

+ Expand

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]

+ Expand
  • 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]

+ Expand
  • Animal Models: Brca1-/-;p53-/- mammary tumors are generated in K14cre;Brca1F/F;p53F/F mice.
  • Formulation: 50 mg/mL stocks in DMSO with 10% 2-hydroxyl-propyl-β-cyclodextrine/PBS
  • 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 N/A

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 (g) = Concentration (mol/L) × Volume (L) × 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 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
    V1
    C2
    V2

* 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 Conditions Sponsor/Collaborators Start Date Phases
NCT03561870 Not yet recruiting Recurrent IDH|Mutant High Grade Glioma Hospices Civils de Lyon December 1 2019 Phase 2
NCT03561870 Not yet recruiting Recurrent IDH|Mutant High Grade Glioma Hospices Civils de Lyon December 1 2019 Phase 2
NCT03741426 Not yet recruiting Renal Cell Cancer CCTU- Cancer Theme|University of Cambridge|AstraZeneca|Cancer Research UK|Cambridge University Hospitals NHS Foundation Trust July 25 2019 Phase 2
NCT03741426 Not yet recruiting Renal Cell Cancer CCTU- Cancer Theme|University of Cambridge|AstraZeneca|Cancer Research UK|Cambridge University Hospitals NHS Foundation Trust July 25 2019 Phase 2
NCT03880019 Not yet recruiting Stage III Uterine Corpus Leiomyosarcoma AJCC v8|Stage IIIA Uterine Corpus Leiomyosarcoma AJCC v8|Stage IIIB Uterine Corpus Leiomyosarcoma AJCC v8|Stage IIIC Uterine Corpus Leiomyosarcoma AJCC v8|Stage IV Uterine Corpus Leiomyosarcoma AJCC v8|Stage IVA Uterine Corpus Leiomyosarcoma AJCC v8|Stage IVB Uterine Corpus Leiomyosarcoma AJCC v8 National Cancer Institute (NCI) June 7 2019 Phase 2
NCT03842228 Not yet recruiting Advanced Malignant Solid Neoplasm|ARID1A Gene Mutation|ATM Gene Mutation|ATRX Gene Mutation|BARD1 Gene Mutation|BRCA1 Gene Mutation|BRCA2 Gene Mutation|BRIP1 Gene Mutation|CDK12 Gene Mutation|CHEK1 Gene Mutation|CHEK2 Gene Mutation|FANCA Gene Mutation|FANCL Gene Mutation|Metastatic Malignant Solid Neoplasm|MRE11 Gene Mutation|MSH2 Gene Mutation|PALB2 Gene Mutation|PARP1 Gene Mutation|PIK3CA Gene Mutation|POLD1 Gene Mutation|PPP2R2A Gene Mutation|PTEN Gene Mutation|RAD51B Gene Mutation|RAD51C Gene Mutation|RAD51D Gene Mutation|RAD54L Gene Mutation|Unresectable Malignant Solid Neoplasm|XRCC2 Gene Mutation National Cancer Institute (NCI) June 10 2019 Phase 1

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.

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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.

PARP Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID