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 187 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 MojsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmLaOEBl Ml7CTWM2OD13LkewOUAh|ryPIB?= NF;aZVcyQDV3OU[xNy=>
KP6.3 MlnJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml70OEBl NF7EdHpKSzVyPUGwMlQzQCEQvF2g MmP4NVg2PTl4MUO=
KP7.7 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnTZOEBl NGG0N3VKSzVyPUW3JI5OKA>? NHK1d3cyQDV3OU[xNy=>
KB2P3.4 NVLKT2Y6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3O4eVQh\A>? M3H3T2lEPTB;MUK0JG0h MWWxPFU2QTZzMx?=
KB2P1.21 NX\EU|RTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXMOEBl MXnJR|UxRTh7MEegcm0h NVzUVVUzOTh3NUm2NVM>
U373-MG NYKyO45iS3m2b4TvfIlkKEG|c3H5 MX2xJO69VSB? MVOyOEBp NHLFclRKdmO{ZXHz[ZMhemGmaXH0bY9vKHOnboPpeIl3cXS7 NX:2NoRJOTh7NUS3NVI>
T98G M2HMOGN6fG:2b4jpZ{BCe3OjeR?= NXXvb|BZOSEQvF2g MX:yOEBp NW\RTWxyUW6lcnXhd4V{KHKjZHnheIlwdiC|ZX7zbZRqfmm2eR?= M2fuTVE5QTV2N{Gy
U87-MG M1zNT2N6fG:2b4jpZ{BCe3OjeR?= NWr0XXE4OSEQvF2g Ml;tNlQhcA>? M3vqTmlv[3KnYYPld{Bz[WSrYYTpc44he2Wwc3n0bZZqfHl? M1XPO|E5QTV2N{Gy
UVW NVS4WlFvS3m2b4TvfIlkKEG|c3H5 NWLKTGN5PTByIH7N MYiyOEBp MVTJcoNz\WG|ZYOgdoFlcWG2aX;uJJNmdnOrdHn2bZR6 NWDtU2FiOTh7NUS3NVI>
HeLa NH3NVllHfW6ldHnvckBCe3OjeR?= NE\lSIY2ODBibl2= Ml;lOEBp NYD6SnVxS2G3c3XzJIEhdW:mZYP0JIRmdGG7IHnuJJJmcm:rbnnu[{Bw\iC{YXTpZZRqd25vaX7keYNm\CCGTlGgZpJm[Wu| NWfrdYdLOTh7NUS3NVI>
HeLa NYHiWmpqTnWwY4Tpc44hSXO|YYm= MXOxJO69VSB? M3ewUFI1KGh? MoXwSY5p[W6lZYOgdoFlcWG2aX;uMYlv\HWlZXSgV{1xcGG|ZTDhdpJme3R? M3\1XlE5QTV2N{Gy
T98G MlfMSpVv[3Srb36gRZN{[Xl? NHzEc5YyKM7:TTC= NHn6TmkzPCCq MXHFcohidmOnczDyZYRq[XSrb36tbY5lfWOnZDDTMZBp[XOnIHHydoV{fA>? NIHvRWgyQDl3NEexNi=>
L3 NEXVXGVEgXSxdH;4bYMhSXO|YYm= MVG1JO69VSB? MU[5OkBp NUnwW5NkTE2VTx?= NIDPc|BUcWewaX\pZ4FvfGy7IHnubIljcXS|IHPlcIwhe3W{dnn2ZYw> MlKyNlAyOjR2NUm=
Granta-519 NIr1OpBEgXSxdH;4bYMhSXO|YYm= M1\rWVUh|ryPIB?= MVO5OkBp NGX5bIlFVVOR M1XYdHNtcWeqdHz5JIlvcGmkaYTzJINmdGxic4Xyeol3[Wx? MX6yNFEzPDR3OR?=
BT NFiyN2VEgXSxdH;4bYMhSXO|YYm= NX;DOYRlPSEQvF2g Mk\CPVYhcA>? MoC1SG1UVw>? MULTcIlocHSueTDpcohq[mm2czDj[YxtKHO3co\peoFt MWmyNFEzPDR3OR?=
UPN2 NVrQZ3JXS3m2b4TvfIlkKEG|c3H5 Mlm0OUDPxE1i NFjHOYU6PiCq MnPQSG1UVw>? Ml7xV4xq\2i2bImgbY5pcWKrdIOgZ4VtdCC|dYL2bZZidA>? NHL4cJczODF{NES1PS=>
HBL-2 MW\DfZRwfG:6aXOgRZN{[Xl? MVq1JO69VSB? NWLXeZd3QTZiaB?= NV:yfYI2TE2VTx?= MnLnV4xq\2i2bImgbY5pcWKrdIOgZ4VtdCC|dYL2bZZidA>? NVvhWo9kOjBzMkS0OVk>
JVM-2 NGr4WZBEgXSxdH;4bYMhSXO|YYm= NFvvSG42KM7:TTC= Mn:5PVYhcA>? NYTlb5h6TE2VTx?= Mnf4V4xq\2i2bImgbY5pcWKrdIOgZ4VtdCC|dYL2bZZidA>? NYO5[HF4OjBzMkS0OVk>
Z138 M4PNfGN6fG:2b4jpZ{BCe3OjeR?= NYrnWJZUPSEQvF2g MXq5OkBp M4\BO2ROW09? MlX6V4xq\2i2bImgbY5pcWKrdIOgZ4VtdCC|dYL2bZZidA>? NX\qb5B3OjBzMkS0OVk>
RWPE NGXkd3hKdn[jc3n2[UBCe3OjeR?= M4n1[VI2KM7:TR?= MVO0PEBp MoLYSG1UVw>? MUnTbYdvcW[rY3HueIx6KHKnZIXj[ZMhTVKJLXTybZZmdiClZXzsJIlvfmG|aX;u NILpeG0zOTV5NUi2OS=>
VCaP NXy1PXdJUW64YYPpeoUhSXO|YYm= NYm1S45YOjVizszN NVHzPVc2PDhiaB?= MX;EUXNQ NX\pWnQ{W2mpbnnmbYNidnSueTDy[YR2[2W|IFXSS{1lemm4ZX6gZ4VtdCCrbo\hd4lwdg>? NHz5dYQzOTV5NUi2OS=>
Mouse H2AX−/− ES Cells M3fMbmN6fG:2b4jpZ{BCe3OjeR?= M1PKXFIvPSEQvF2= NGHBeGozOCCq M4TYUXNq\26rZnnjZY51dHliaX7obYJqfHNiY3XscEB{fXK4aY\hcC=> M1;CO|I{OzV3NEi5
Mouse ATM−/− ES Cells NFnX[HNEgXSxdH;4bYMhSXO|YYm= NFjRWIUzNjVizszN M2K4d|IxKGh? NF;0fnRUcWewaX\pZ4FvfGy7IHnubIljcXS|IHPlcIwhe3W{dnn2ZYw> MXGyN|M2PTR6OR?=
H1650 NFz6VJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mor2NlAh|ryP NIjXdVYyPDRiaB?= MlfsTWM2OD1zNT60O{DPxE1? NFzOS|AzOzJ|OUiwPS=>
H1650PTEN+ NVr6eI5HT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXSNlAh|ryP NHzMR2gyPDRiaB?= Mn\kTWM2OD13MD64N{DPxE1? M3:zV|I{OjN7OEC5
PC-9 MkjUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW[yNEDPxE1? M3rOOFE1PCCq MmnJTWM2OD13Lki4JO69VQ>? NXy4XVJyOjN{M{m4NFk>
PC-9PTEN− M4rxV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVuzc4JmOjBizszN MoKxNVQ1KGh? NVTLPHh6UUN3ME22MlUzKM7:TR?= MVyyN|I{QThyOR?=
MDA-MB-231 NEXzWIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWC1JIRigQ>? NWfCb5hPUUN3ME22Mlkh|ryP M2rmdFI{PzZyNEm2
MDA-MB-468 NHzYSHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLvfmVrPSCmYYm= MYXJR|UxRTVwMDFOwG0> NUfNPIlwOjN5NkC0PVY>
BT20 NU\GcJlZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHf4emc2KGSjeR?= NYXqPWJ1UUN3ME23Mlch|ryP NVn5NHA5OjN5NkC0PVY>
HCC1143 NHO3UZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\mN5Y2KGSjeR?= MUnJR|UxRTFzLkGg{txO M3faeFI{PzZyNEm2
HCC1937 NEj4No9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnrwOUBl[Xl? Moe1TWM2OD1zMj62JO69VQ>? M33w[lI{PzZyNEm2
Hs578t MlLqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1X0c|Uh\GG7 NG\JSXhKSzVyPUWuOkDPxE1? NFTP[XIzOzd4MES5Oi=>
Hs578t(si) NF3mR5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLocmc2KGSjeR?= NYfvSmZEUUN3ME23MlUh|ryP MlPvNlM4PjB2OU[=
BT474 NH7neJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXm1JIRigQ>? NV3lS5l[UUN3ME2xPU45KM7:TR?= M2ixdlI{PzZyNEm2
JIMT1 MmrPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnToOUBl[Xl? NV7vbVQ5UUN3ME23Mlch|ryP NUTYNWJqOjN5NkC0PVY>
SKBR3 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUi1JIRigQ>? M2PjdGlEPTB;MUGuNUDPxE1? NFW2V2EzOzd4MES5Oi=>
SUM159 MlX5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYK1JIRigQ>? M4nMZ2lEPTB;ND6yJO69VQ>? NIPqW4UzOzd4MES5Oi=>
CAMA1 M37veGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjSOUBl[Xl? MUHJR|UxRTF3Lkig{txO NWHK[GFmOjN5NkC0PVY>
MCF7 NUm2U2xpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLoOVU2KGSjeR?= MoXXTWM2OD13Lkig{txO NH7PdGYzOzd4MES5Oi=>
T47D NX7BUlQ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY[1JIRigQ>? NX60cZh5UUN3ME25MlYh|ryP NF25O|QzOzd4MES5Oi=>
HCT116 MkfXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVuxNFAh|ryP M4\wclQ5KGh? NY\m[o86TE2VTx?= NHfxXWlKSzVyPUKuOUDPxE1i MUCyOFU4Pzl2MR?=
SW1116 NGHHbI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NILTPFQyODBizszN NX;wV5g{PDhiaB?= MVnEUXNQ NHTkclhKSzVyPUGwNEDPxE1? MVuyOFU4Pzl2MR?=
HT29 M1\PNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV6xNFAh|ryP Mnv1OFghcA>? MmPNSG1UVw>? NELSSWFKSzVyPUG0Mlch|ryP M17IblI1PTd5OUSx
LoVo NYqw[GFxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXsd4oyODBizszN Mn\jOFghcA>? M1nsT2ROW09? M2nSR2lEPTB;MUOuOEDPxE1? NHHz[GUzPDV5N{m0NS=>
HCT-15 NFrLXIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHvWWGgyODBizszN MX60PEBp M{LiemROW09? M1XBSGlEPTB;MUCg{txO NETzWFkzPDV5N{m0NS=>
SW48 NFvCZ41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\nUI0yODBizszN MkXzOFghcA>? NEO1N|hFVVOR Mk\TTWM2OD17LkWg{txO MnjpNlQ2Pzd7NEG=
C-1 NWOwXHJxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGnXdXMyODBizszN NUPMRoxkPDhiaB?= M4jETmROW09? NWfiUIN[UUN3ME23MlYh|ryP MmjzNlQ2Pzd7NEG=
RKO NYHJT4dRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUGxNFAh|ryP MljxOFghcA>? NHzGboxFVVOR NXTjendYUUN3ME21Mlkh|ryP Mk\ZNlQ2Pzd7NEG=
HCT116 NG\BfVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXflPYl[OTByIN88US=> NEjXNow1QCCq NIfJfHhFVVOR M2XjNnBwfGWwdHnheIV{KFOQLUO4JIN6fG:2b4jpZ4l1gSB? MmfPNlQ2Pzd7NEG=
SW1116 MlyyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLB[3YyODBizszN M{HBZ|Q5KGh? MUnEUXNQ MlywVI91\W62aXH0[ZMhW05vM{igZ5l1d3SxeHnjbZR6KA>? MX2yOFU4Pzl2MR?=
HT29 MlLwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4fXeVExOCEQvF2= NYDGSIRRPDhiaB?= NGC5UYhFVVOR NFvUcIJRd3SnboTpZZRmeyCVTj2zPEBkgXSxdH;4bYNqfHli NFrrUIgzPDV5N{m0NS=>
LoVo M1K4Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPXNVAxKM7:TR?= NYLPd3FnPDhiaB?= MWDEUXNQ M1XWdnBwfGWwdHnheIV{KFOQLUO4JIN6fG:2b4jpZ4l1gSB? NYHBfZNZOjR3N{e5OFE>
SW48 Mn3TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV6xNFAh|ryP MVi0PEBp NHTZRWZFVVOR NGPxTnBRd3SnboTpZZRmeyCVTj2zPEBkgXSxdH;4bYNqfHli MVWyOFU4Pzl2MR?=
C-1 MnrvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXexNFAh|ryP MmrWOFghcA>? NEixPHNFVVOR MUHQc5RmdnSrYYTld{BUVi1|ODDjfZRwfG:6aXPpeJkh MUGyOFU4Pzl2MR?=
RKO NEj1[XJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWWxNFAh|ryP MUm0PEBp NUm3WVdDTE2VTx?= M1mzUnBwfGWwdHnheIV{KFOQLUO4JIN6fG:2b4jpZ4l1gSB? NVvC[VY4OjR3N{e5OFE>
HCT116 MXjGeY5kfGmxbjDBd5NigQ>? NXTKfZl5OTBibl2= MYexNkBp NXnScpRnTE2VTx?= NG\LXW1KdmO{ZXHz[ZMhTE6DIHTveYJt\S2|dILhcoQh[nKnYXvzJIlv\HWlZXSgZpkhW05vM{i= NU\FZZdJOjR3N{e5OFE>
HT29 MXXGeY5kfGmxbjDBd5NigQ>? NYi1RXE1OTBibl2= NEfEe2EyOiCq MYLEUXNQ NF\UW4VKdmO{ZXHz[ZMhTE6DIHTveYJt\S2|dILhcoQh[nKnYXvzJIlv\HWlZXSgZpkhW05vM{i= MkTYNlQ2Pzd7NEG=
TE-6 NYjDSZpWTnWwY4Tpc44hSXO|YYm= NEK4bWc2KM7:TTC= Mk\BNVIhcA>? NXTxZ21UTE2VTx?= MXPJcoR2[2W|IFeyM20h[XK{ZYP0 MVGyOFIyQTF4NB?=
TE-6 MX7GeY5kfGmxbjDBd5NigQ>? MYO1JO69VSB? MWSyOEBp M2WyW2ROW09? NVe3foV{UW6lcnXhd4V{KGmwIHTveYJt\SC|dILhcoQh[nKnYXvzJEhFW0K|KR?= NXG5[IRYOjR{MUmxOlQ>
Hep3B MkXUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUe0NEDPxE1i MVy3NkBp MVnEUXNQ MULTfY5memerc4TpZ4FtdHliaX7obYJqfHNiY3XscEBoem:5dHige4l1cCCGSF3FVS=> NHvEe44zPTB5Mke1Ni=>
Huh7 NXzu[o1xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV20NEDPxE1i NV3LW3d1PzJiaB?= NWfzTm82TE2VTx?= NYq5TY9kW3mwZYLnbZN1cWOjbHz5JIlvcGmkaYTzJINmdGxiZ4Lve5RpKHerdHigSGhOTVF? M2\0dVI2ODd{N{Wy
Hep3B M3rv[WZ2dmO2aX;uJGF{e2G7 Mn\VOFAh|ryPIB?= NU\mSpB7OjRiaB?= NXnyc|dNTE2VTx?= NXjhW3RtUW6mdXPld{BTV1NicILv[JVkfGmxbjD3bZRpKESKTVXR MkSwNlUxPzJ5NUK=
Huh7 NEfje49HfW6ldHnvckBCe3OjeR?= M3;rOVQxKM7:TTC= NX61dHJnOjRiaB?= MX;EUXNQ M{PLSmlv\HWlZYOgVm9UKHC{b3T1Z5Rqd25id3n0bEBFUE2HUR?= NFG2Wm8zPTB5Mke1Ni=>
Hep3B NFXCfXlHfW6ldHnvckBCe3OjeR?= NUO0ZlFIPDBizszNJC=> NVzXc3ZPOjRiaB?= NYfTfYtyTE2VTx?= NEjnTpJKdmS3Y3XzJINmdGxiYYX0c5Bp[We7IIfpeIghTEiPRWG= Mnu2NlUxPzJ5NUK=
Huh7 NIrM[YJHfW6ldHnvckBCe3OjeR?= MnzlOFAh|ryPIB?= M3qxZlI1KGh? MVPEUXNQ MUTJcoR2[2W|IHPlcIwh[XW2b4DoZYd6KHerdHigSGhOTVF? NUXRNI52OjVyN{K3OVI>
SGC-7901 M3X3Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV33fI5nOzEEoN88US=> M3jre|Q5KGh? MVLEUXNQ MYPCcI9kcyCxeHHsbZBt[XSrbj3pcoR2[2WmIHPlcIwh\GWjdHi= M{L3ZVI2PzZ5MEe2
COLO-800 M1HGSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofxTWM2OD1yLkS0NVY1KM7:TR?= NVzsWlEyW0GQR1XS
EoL-1- NHTpWYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTBwNU[0OFYh|ryP MY\TRW5ITVJ?
NCI-H209 NITER4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnTU5M2UUN3ME2wMlkyPTV4IN88US=> MVXTRW5ITVJ?
ES1 MoTxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLxN4dKSzVyPUGuNVE1ODhizszN MXvTRW5ITVJ?
NKM-1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmHUTWM2OD1zLkK1N|Q4KM7:TR?= MXXTRW5ITVJ?
NTERA-S-cl-D1 NEfZNZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnH2TWM2OD1zLkOzN|QyKM7:TR?= NXPnfY1IW0GQR1XS
MHH-ES-1 M{X2dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLOTWM2OD1zLk[yNFY4KM7:TR?= MVHTRW5ITVJ?
ES8 NFzub5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHSTWM2OD1zLkeyOFE1KM7:TR?= M1vMSnNCVkeHUh?=
NCI-H720 NEjaZo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\jTWM2OD1{LkKwOlk6KM7:TR?= NIH6PWRUSU6JRWK=
EW-3 NUPHN2pXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLacXhJUUN3ME2yMlI4PTN2IN88US=> NXLSdodlW0GQR1XS
D-566MG MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTJwNES1Olgh|ryP MYjTRW5ITVJ?
697 NF\DXopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTJwOESxO|Mh|ryP NFHlSHFUSU6JRWK=
ES5 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInB[YZKSzVyPUKuPFgyQDlizszN MVfTRW5ITVJ?
COLO-684 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3LN4lKSzVyPUOuOVE3QTZizszN MXzTRW5ITVJ?
ML-2 M4\oUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWm2U|hRUUN3ME2zMlYxODV6IN88US=> MorIV2FPT0WU
MC-IXC NHK4cIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTNwNkOzPVMh|ryP M4HibXNCVkeHUh?=
DB NXjZR3A3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUTQWJFoUUN3ME2zMlY2PDR6IN88US=> M{OwPXNCVkeHUh?=
HCC2218 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYO3S4lGUUN3ME2zMlc{OTB|IN88US=> MmnmV2FPT0WU
NCI-H510A MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTNwOEK3NlQh|ryP MX7TRW5ITVJ?
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OAW-42 M3TGfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHtN2ptUUN3ME20OE4zPjR|IN88US=> MnLKV2FPT0WU
C8166 NInCfVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHGzWlhKSzVyPUS1MlA5OjJizszN M3fH[3NCVkeHUh?=
LU-99A NUj3TFFjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTR4LkGzNlIh|ryP NXXtO5lYW0GQR1XS
NCI-H23 NGLtXYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnI[oMxUUN3ME20Ok4yPzh3IN88US=> NECzc3NUSU6JRWK=
HO-1-N-1 MonmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXsWWlKSzVyPUS3MlA6QThizszN NVLuWmNPW0GQR1XS
A3-KAW MlqyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIr3RY5KSzVyPUS3MlExODdizszN MUjTRW5ITVJ?
CGTH-W-1 M2O1RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NETuUIZKSzVyPUS3MlUxPjlizszN NXv1OFM1W0GQR1XS
DJM-1 M1\MSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1T6cmlEPTB;NEeuOVQyOyEQvF2= Ml\OV2FPT0WU
A101D NYnyfGl[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDtSHNKSzVyPUS3MlY{PTdizszN NEnKNWtUSU6JRWK=
BB30-HNC MnfJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHETWM2OD12OD6zNFczKM7:TR?= NX3WPGZkW0GQR1XS
T98G NFHETIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXrQV5RKUUN3ME20PE41PjN|IN88US=> MUHTRW5ITVJ?
NCI-H1573 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoLaTWM2OD12OT60OFYzKM7:TR?= NHXGdmdUSU6JRWK=
MEG-01 Mnu5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33FeGlEPTB;NEmuO|QyOSEQvF2= NEHld25USU6JRWK=
WM-115 NVPsO|IxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvETWM2OD12OT65NlIzKM7:TR?= M{XKWnNCVkeHUh?=

... 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 (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

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

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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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)
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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.

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID