Olaparib (AZD2281)

For research use only. Not for use in humans.

Catalog No.S1060 Synonyms: Ku-0059436

453 publications

Olaparib (AZD2281) 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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Selleck's Olaparib (AZD2281) has been cited by 453 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 M1:zTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\6OEBl NHza[4JKSzVyPUWuO|A2KCEQvF2g MoW0NVg2PTl4MUO=
KP6.3 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH:1Vm81KGR? M3juXWlEPTB;MUCuOFI5KM7:TTC= NGrZVGoyQDV3OU[xNy=>
KP7.7 MlnnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXy0JIQ> MUDJR|UxRTV5IH7NJC=> NG\2cVgyQDV3OU[xNy=>
KB2P3.4 NYjUcXdRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXK0JIQ> MX7JR|UxRTF{NDDNJC=> NULkNFM4OTh3NUm2NVM>
KB2P1.21 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY[0JIQ> NUDEWnpsUUN3ME24PVA4KG6PIB?= MoCwNVg2PTl4MUO=
U373-MG NHHafWREgXSxdH;4bYMhSXO|YYm= MVGxJO69VSB? MoKxNlQhcA>? NYLBZlBSUW6lcnXhd4V{KHKjZHnheIlwdiC|ZX7zbZRqfmm2eR?= MUixPFk2PDdzMh?=
T98G MmrxR5l1d3SxeHnjJGF{e2G7 M3KyRVEh|ryPIB?= NGDqb3UzPCCq MVLJcoNz\WG|ZYOgdoFlcWG2aX;uJJNmdnOrdHn2bZR6 M3niRVE5QTV2N{Gy
U87-MG NILMOGxEgXSxdH;4bYMhSXO|YYm= NXL6fJpmOSEQvF2g MWiyOEBp MX\JcoNz\WG|ZYOgdoFlcWG2aX;uJJNmdnOrdHn2bZR6 NYGz[Gt[OTh7NUS3NVI>
UVW M{XxdmN6fG:2b4jpZ{BCe3OjeR?= MUW1NFAhdk1? M{nuRlI1KGh? M1yzW2lv[3KnYYPld{Bz[WSrYYTpc44he2Wwc3n0bZZqfHl? M3SxWVE5QTV2N{Gy
HeLa M3rj[mZ2dmO2aX;uJGF{e2G7 Ml3LOVAxKG6P NIrIV2I1KGh? NXvo[VgyS2G3c3XzJIEhdW:mZYP0JIRmdGG7IHnuJJJmcm:rbnnu[{Bw\iC{YXTpZZRqd25vaX7keYNm\CCGTlGgZpJm[Wu| NHzYZW0yQDl3NEexNi=>
HeLa NWrib3RxTnWwY4Tpc44hSXO|YYm= M1TCPVEh|ryPIB?= MlfXNlQhcA>? M{K2cGVvcGGwY3XzJJJi\GmjdHnvck1qdmS3Y3XkJHMueGijc3WgZZJz\XO2 MmrCNVg6PTR5MUK=
T98G MXHGeY5kfGmxbjDBd5NigQ>? NFO1XWoyKM7:TTC= NXv2XZJvOjRiaB?= MYXFcohidmOnczDyZYRq[XSrb36tbY5lfWOnZDDTMZBp[XOnIHHydoV{fA>? NXrDdGVsOTh7NUS3NVI>
L3 MmLtR5l1d3SxeHnjJGF{e2G7 NUTS[m1jPSEQvF2g MUi5OkBp M{PPOGROW09? MV3TbYdvcW[rY3HueIx6KGmwaHnibZR{KGOnbHygd5Vzfmm4YXy= MmnVNlAyOjR2NUm=
Granta-519 NVvZd4V4S3m2b4TvfIlkKEG|c3H5 M4TWW|Uh|ryPIB?= M{DoNlk3KGh? MYrEUXNQ NELTdJZUdGmpaITsfUBqdmirYnn0d{Bk\WyuIIP1dpZqfmGu M1WyXFIxOTJ2NEW5
BT NXr1WWliS3m2b4TvfIlkKEG|c3H5 NED1OWM2KM7:TTC= NXS0eY4yQTZiaB?= NWi2bnlnTE2VTx?= MV\TcIlocHSueTDpcohq[mm2czDj[YxtKHO3co\peoFt NEDNe|QzODF{NES1PS=>
UPN2 MorqR5l1d3SxeHnjJGF{e2G7 NHPwfHo2KM7:TTC= MYW5OkBp NYDL[pZsTE2VTx?= M37ZN3NtcWeqdHz5JIlvcGmkaYTzJINmdGxic4Xyeol3[Wx? MkXuNlAyOjR2NUm=
HBL-2 M{nIeWN6fG:2b4jpZ{BCe3OjeR?= MUW1JO69VSB? NX;rSo9QQTZiaB?= NFvzbGdFVVOR M4T2PHNtcWeqdHz5JIlvcGmkaYTzJINmdGxic4Xyeol3[Wx? M37uXlIxOTJ2NEW5
JVM-2 NVHD[otDS3m2b4TvfIlkKEG|c3H5 NWn0OpA4PSEQvF2g M{DqbVk3KGh? NGHtS|lFVVOR MmfrV4xq\2i2bImgbY5pcWKrdIOgZ4VtdCC|dYL2bZZidA>? M2XS[VIxOTJ2NEW5
Z138 MW\DfZRwfG:6aXOgRZN{[Xl? M4\nR|Uh|ryPIB?= M{HhSFk3KGh? NXPOXY9RTE2VTx?= M1rNW3NtcWeqdHz5JIlvcGmkaYTzJINmdGxic4Xyeol3[Wx? M3\icVIxOTJ2NEW5
RWPE MnqyTY53[XOrdnWgRZN{[Xl? MlnTNlUh|ryP M2fXXFQ5KGh? M3K5RWROW09? M3[4S3Nq\26rZnnjZY51dHlicnXkeYNmeyCHUlet[JJqfmWwIHPlcIwhcW64YYPpc44> NXHsNoZwOjF3N{W4OlU>
VCaP MmC0TY53[XOrdnWgRZN{[Xl? M{LNW|I2KM7:TR?= M4nuelQ5KGh? MkTmSG1UVw>? M2O2fnNq\26rZnnjZY51dHlicnXkeYNmeyCHUlet[JJqfmWwIHPlcIwhcW64YYPpc44> NYPwcndPOjF3N{W4OlU>
Mouse H2AX−/− ES Cells NH3iNG9EgXSxdH;4bYMhSXO|YYm= MWSyMlUh|ryP NFvDNGozOCCq MlPrV4lodmmoaXPhcpRtgSCrbnjpZol1eyClZXzsJJN2en[rdnHs NUPHZYlFOjN|NUW0PFk>
Mouse ATM−/− ES Cells NGHr[GdEgXSxdH;4bYMhSXO|YYm= NWDxeGdwOi53IN88US=> M3WzbFIxKGh? MVTTbYdvcW[rY3HueIx6KGmwaHnibZR{KGOnbHygd5Vzfmm4YXy= MW[yN|M2PTR6OR?=
H1650 MnnkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYeyNEDPxE1? MlPyNVQ1KGh? M2nFZmlEPTB;MUWuOFch|ryP MVuyN|I{QThyOR?=
H1650PTEN+ MmHFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;wdlIxKM7:TR?= MYSxOFQhcA>? MmTVTWM2OD13MD64N{DPxE1? M3\SN|I{OjN7OEC5
PC-9 NYThc2k6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWOyNEDPxE1? MonVNVQ1KGh? MkP6TWM2OD13Lki4JO69VQ>? NHWxSVYzOzJ|OUiwPS=>
PC-9PTEN− NGLkSpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2CxeVIxKM7:TR?= MYixOFQhcA>? NGnMfGpKSzVyPU[uOVIh|ryP M1PGWlI{OjN7OEC5
MDA-MB-231 M{PnUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV3lTI54PSCmYYm= NFftN5hKSzVyPU[uPUDPxE1? MnTrNlM4PjB2OU[=
MDA-MB-468 NVjtTFZ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXK1JIRigQ>? MUTJR|UxRTVwMDFOwG0> MXWyN|c3ODR7Nh?=
BT20 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PnZlUh\GG7 NGS5UohKSzVyPUeuO{DPxE1? NXnMOHhlOjN5NkC0PVY>
HCC1143 NH\he|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYK1JIRigQ>? MYHJR|UxRTFzLkGg{txO M4jZfVI{PzZyNEm2
HCC1937 NYLBfIlTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3PQNVUh\GG7 NGDMOnBKSzVyPUGyMlYh|ryP NFvqV3ozOzd4MES5Oi=>
Hs578t NH:zbVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTBOUBl[Xl? MWXJR|UxRTVwNjFOwG0> NHHaT3czOzd4MES5Oi=>
Hs578t(si) MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXG1JIRigQ>? NYTHT3RpUUN3ME23MlUh|ryP MnTNNlM4PjB2OU[=
BT474 NVrTXG9nT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3r3VFUh\GG7 Mki5TWM2OD1zOT64JO69VQ>? Ml7yNlM4PjB2OU[=
JIMT1 M{LrNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV:1JIRigQ>? MlPVTWM2OD15Lkeg{txO MnTwNlM4PjB2OU[=
SKBR3 M3rSeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIj2dIs2KGSjeR?= MWfJR|UxRTFzLkGg{txO MU[yN|c3ODR7Nh?=
SUM159 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWK1JIRigQ>? Ml6zTWM2OD12LkKg{txO NFfvd20zOzd4MES5Oi=>
CAMA1 Ml;JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn64OUBl[Xl? Mkn2TWM2OD1zNT64JO69VQ>? NX[4cHVzOjN5NkC0PVY>
MCF7 NELVXHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYW1JIRigQ>? NEnEbXJKSzVyPUWuPEDPxE1? M3ryflI{PzZyNEm2
T47D MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jyWFUh\GG7 NIq3[GJKSzVyPUmuOkDPxE1? MmfyNlM4PjB2OU[=
HCT116 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;Ccot7OTByIN88US=> MWO0PEBp NIjubFlFVVOR NU\q[mRnUUN3ME2yMlUh|ryPIB?= NVHpTWpYOjR3N{e5OFE>
SW1116 NX3FU2hTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{K3S|ExOCEQvF2= NVe2Omk1PDhiaB?= MnrQSG1UVw>? M{e1RWlEPTB;MUCwJO69VQ>? MXyyOFU4Pzl2MR?=
HT29 NE\BVmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzUO48yODBizszN MnH4OFghcA>? MWrEUXNQ M1fzS2lEPTB;MUSuO{DPxE1? MnPKNlQ2Pzd7NEG=
LoVo NXrOW4tIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHO4NHUyODBizszN NGnrd441QCCq NWDoOFh{TE2VTx?= NYLzWVVNUUN3ME2xN{41KM7:TR?= NVTydWdjOjR3N{e5OFE>
HCT-15 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX[xNFAh|ryP NIHMR2o1QCCq NUXpPVIyTE2VTx?= M13BbmlEPTB;MUCg{txO MoqyNlQ2Pzd7NEG=
SW48 MnHDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4C0PFExOCEQvF2= NFHt[mU1QCCq NYjPRpN2TE2VTx?= NGi3dmFKSzVyPUmuOUDPxE1? MlXPNlQ2Pzd7NEG=
C-1 MmfSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYKxNFAh|ryP MlzwOFghcA>? MWrEUXNQ Moi4TWM2OD15Lk[g{txO NW\5fYFvOjR3N{e5OFE>
RKO MoPGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3UXIl1OTByIN88US=> NIHQO4U1QCCq NHixe|ZFVVOR M2jXWGlEPTB;NT65JO69VQ>? MkLBNlQ2Pzd7NEG=
HCT116 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXrCOI8xOTByIN88US=> MXq0PEBp MXfEUXNQ MXPQc5RmdnSrYYTld{BUVi1|ODDjfZRwfG:6aXPpeJkh M4P4TVI1PTd5OUSx
SW1116 NVXSN4Z1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTp[3l2OTByIN88US=> MUO0PEBp NH\YOY5FVVOR MXXQc5RmdnSrYYTld{BUVi1|ODDjfZRwfG:6aXPpeJkh NYLTPGZGOjR3N{e5OFE>
HT29 MnmzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXGxNFAh|ryP NYnPTmdiPDhiaB?= NG\PT3NFVVOR NYPDR4I2WG:2ZX70bYF1\XNiU16tN|gh[3m2b4TvfIlkcXS7IB?= Mo\INlQ2Pzd7NEG=
LoVo NH21e4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mkn5NVAxKM7:TR?= MX:0PEBp NF7HfJBFVVOR M1fVd3BwfGWwdHnheIV{KFOQLUO4JIN6fG:2b4jpZ4l1gSB? M33ibFI1PTd5OUSx
SW48 MmrpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvkWJNyOTByIN88US=> NGTwVFE1QCCq MXvEUXNQ MlTGVI91\W62aXH0[ZMhW05vM{igZ5l1d3SxeHnjbZR6KA>? NYXWOpJSOjR3N{e5OFE>
C-1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUSyW5lxOTByIN88US=> Mle4OFghcA>? M2jkfWROW09? NHL6NmlRd3SnboTpZZRmeyCVTj2zPEBkgXSxdH;4bYNqfHli MmnyNlQ2Pzd7NEG=
RKO M{fERmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVixNFAh|ryP M4[wS|Q5KGh? MYDEUXNQ MkjsVI91\W62aXH0[ZMhW05vM{igZ5l1d3SxeHnjbZR6KA>? MXSyOFU4Pzl2MR?=
HCT116 NGn3OnRHfW6ldHnvckBCe3OjeR?= Mk\4NVAhdk1? NIjBNZgyOiCq MVvEUXNQ MWjJcoNz\WG|ZYOgSG5CKGSxdXLs[U1{fHKjbnSgZpJm[Wu|IHnu[JVk\WRiYomgV24uOzh? M1jxWVI1PTd5OUSx
HT29 MXnGeY5kfGmxbjDBd5NigQ>? NE\EUGEyOCCwTR?= NHHldGUyOiCq Ml7vSG1UVw>? MV;JcoNz\WG|ZYOgSG5CKGSxdXLs[U1{fHKjbnSgZpJm[Wu|IHnu[JVk\WRiYomgV24uOzh? MWSyOFU4Pzl2MR?=
TE-6 MVHGeY5kfGmxbjDBd5NigQ>? NEn6fm42KM7:TTC= NEXiOHUyOiCq MUfEUXNQ NWK5Zo1jUW6mdXPld{BIOi:PIHHydoV{fA>? NXTXVWtSOjR{MUmxOlQ>
TE-6 NYDYOGE3TnWwY4Tpc44hSXO|YYm= MnrIOUDPxE1i M2XGdVI1KGh? NWDCUmduTE2VTx?= M4XXcGlv[3KnYYPld{BqdiCmb4XicIUhe3S{YX7kJIJz\WGtczCoSHNDeyl? MUiyOFIyQTF4NB?=
Hep3B Ml6yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M372c|QxKM7:TTC= NHf2WHo4OiCq MVvEUXNQ NWjEWHBxW3mwZYLnbZN1cWOjbHz5JIlvcGmkaYTzJINmdGxiZ4Lve5RpKHerdHigSGhOTVF? M{TYXlI2ODd{N{Wy
Huh7 M2m2TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkXmOFAh|ryPIB?= NX\q[mNYPzJiaB?= MknhSG1UVw>? M{j6dHN6dmW{Z3nzeIlk[WyueTDpcohq[mm2czDj[YxtKGe{b4f0bEB4cXSqIFTIUWVS NXL3SnNkOjVyN{K3OVI>
Hep3B NWrrOGdHTnWwY4Tpc44hSXO|YYm= M1nlW|QxKM7:TTC= M2\pc|I1KGh? MWnEUXNQ MUPJcoR2[2W|IGLPV{Bxem:mdXP0bY9vKHerdHigSGhOTVF? NHnQSHkzPTB5Mke1Ni=>
Huh7 Mm\6SpVv[3Srb36gRZN{[Xl? NHvpdWU1OCEQvF2g M4fxRVI1KGh? MU\EUXNQ NWO3SlR3UW6mdXPld{BTV1NicILv[JVkfGmxbjD3bZRpKESKTVXR NXXFXXlQOjVyN{K3OVI>
Hep3B MYjGeY5kfGmxbjDBd5NigQ>? NGHxdlI1OCEQvF2g MmrJNlQhcA>? M2DNT2ROW09? Mlu1TY5lfWOnczDj[YxtKGG3dH;wbIFogSC5aYToJGRJVUWT NWDXeIxKOjVyN{K3OVI>
Huh7 MmDqSpVv[3Srb36gRZN{[Xl? MVu0NEDPxE1i NVnHeG9lOjRiaB?= M1[zVGROW09? MmfNTY5lfWOnczDj[YxtKGG3dH;wbIFogSC5aYToJGRJVUWT MkfoNlUxPzJ5NUK=
SGC-7901 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVKzNOKh|ryP MknQOFghcA>? NEHpNJFFVVOR Mo\JRoxw[2tib4jhcIlxdGG2aX6tbY5lfWOnZDDj[YxtKGSnYYTo MonONlU4PjdyN{[=
COLO-800 M1W5Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XxN2lEPTB;MD60OFE3PCEQvF2= M{m1PXNCVkeHUh?=
EoL-1- NYjidIx3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPvPIdKSzVyPUCuOVY1PDZizszN M3TFU3NCVkeHUh?=
NCI-H209 NV[xdZhJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTBwOUG1OVYh|ryP NYnYNWdMW0GQR1XS
ES1 MlTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmW0TWM2OD1zLkGxOFA5KM7:TR?= NGCwWlBUSU6JRWK=
NKM-1 M2juRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnWTWM2OD1zLkK1N|Q4KM7:TR?= NXH2co9nW0GQR1XS
NTERA-S-cl-D1 Mn60S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFS0XFlKSzVyPUGuN|M{PDFizszN Mn7EV2FPT0WU
MHH-ES-1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXyfoZKSzVyPUGuOlIxPjdizszN MU\TRW5ITVJ?
ES8 NH3ScmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPVTWM2OD1zLkeyOFE1KM7:TR?= M4rROXNCVkeHUh?=
NCI-H720 MmLQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPUcHV{UUN3ME2yMlIxPjl7IN88US=> NY\qbnROW0GQR1XS
EW-3 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jRVWlEPTB;Mj6yO|U{PCEQvF2= MoDyV2FPT0WU
D-566MG NUXINIt{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTJwNES1Olgh|ryP M3rNbnNCVkeHUh?=
697 M{O4e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrjNZd6UUN3ME2yMlg1OTd|IN88US=> NYPGeFdEW0GQR1XS
ES5 NXmxWll3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTJwOEixPFkh|ryP MYjTRW5ITVJ?
COLO-684 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnqd2RKSzVyPUOuOVE3QTZizszN NHK2XZhUSU6JRWK=
ML-2 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjCTlBKSzVyPUOuOlAxPThizszN NX3YS|ExW0GQR1XS
MC-IXC MojVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTNwNkOzPVMh|ryP MmLpV2FPT0WU
DB NUXrTmo3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7JVplKSzVyPUOuOlU1PDhizszN M4XacHNCVkeHUh?=
HCC2218 M1nUU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTNwN{OxNFMh|ryP NYX0d4lpW0GQR1XS
NCI-H510A MkXmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmj1TWM2OD1|LkiyO|I1KM7:TR?= MkTVV2FPT0WU
NCI-H526 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvuepFiUUN3ME2zMlg3QTV6IN88US=> MWLTRW5ITVJ?
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LU-139 MmDUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWLRT|Q3UUN3ME20Mlc2QDJ7IN88US=> MWTTRW5ITVJ?
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NCI-H1048 Ml\WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HnUWlEPTB;NT65O|I4OyEQvF2= M2KzcXNCVkeHUh?=
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DU-4475 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4rvZ2lEPTB;MkSuN|M{PyEQvF2= NFv4W3ZUSU6JRWK=
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Ramos-2G6-4C10 M13vTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\lVZlKSzVyPUO1MlI1OjVizszN MVPTRW5ITVJ?
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MFM-223 Mmr1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mki5TWM2OD12ND6xNlI5KM7:TR?= M2XRVnNCVkeHUh?=
OAW-42 NVHaOpl6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkWxTWM2OD12ND6yOlQ{KM7:TR?= NVXxfmpMW0GQR1XS
C8166 NGq0ZotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLjTWM2OD12NT6wPFIzKM7:TR?= NI\QOpNUSU6JRWK=
LU-99A NWqwcpJQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLVdZVsUUN3ME20Ok4yOzJ{IN88US=> MXXTRW5ITVJ?
NCI-H23 NF7G[ZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHG4VY1KSzVyPUS2MlE4QDVizszN M3q4NnNCVkeHUh?=
HO-1-N-1 NIn1cmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX2yTJB2UUN3ME20O{4xQTl6IN88US=> MnT3V2FPT0WU
A3-KAW Mlm4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13P[2lEPTB;NEeuNVAxPyEQvF2= M164VXNCVkeHUh?=
CGTH-W-1 M4HKNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrRc3dNUUN3ME20O{42ODZ7IN88US=> NX;BVmpYW0GQR1XS
DJM-1 Mlu4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWT4Z4RxUUN3ME20O{42PDF|IN88US=> Mkj2V2FPT0WU
A101D MnG1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTR5Lk[zOVch|ryP M1rLXXNCVkeHUh?=
BB30-HNC NXnZZWtoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rNSWlEPTB;NEiuN|A4OiEQvF2= NFTUVFdUSU6JRWK=
T98G M3PXdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;DNVVPUUN3ME20PE41PjN|IN88US=> NIC4NWhUSU6JRWK=
NCI-H1573 M2WzVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NETNZY1KSzVyPUS5MlQ1PjJizszN M1:4eHNCVkeHUh?=
MEG-01 NEftVHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTR7Lke0NVEh|ryP NH3kc3NUSU6JRWK=
WM-115 NEX3bJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTR7LkmyNlIh|ryP NEPjSWJUSU6JRWK=

... 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.
  • 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 Ku-0059436
Smiles FC1=C(C=C(CC2=NNC(=O)C3=C2C=CC=C3)C=C1)C(=O)N4CCN(CC4)C(=O)C5CC5

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
    Concentration
    Volume
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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 interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04024254 Not yet recruiting Drug: Folic Acid Tablet Ovarian Cancer|Breast Cancer|Folic Acid Deficiency Rush University Medical Center August 2019 Phase 2|Phase 3
NCT04005690 Recruiting Drug: Cobimetinib|Drug: Olaparib Resectable Pancreatic Ductal Adenocarcinoma|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|Stage III Pancreatic Cancer AJCC v8 OHSU Knight Cancer Institute|National Cancer Institute (NCI) August 1 2019 Phase 2
NCT03786796 Recruiting Drug: Olaparib Renal Cell Carcinoma|Metastatic Renal Cell Carcinoma|Kidney Cancer|Renal Carcinoma|Kidney Cancer Metastatic Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins|AstraZeneca June 3 2019 Phase 2
NCT03745950 Not yet recruiting Drug: Olaparib Oral Capsule|Drug: Placebo oral capsule Endometrial Carcinoma ARCAGY/ GINECO GROUP February 1 2019 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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID