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 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnqbnk1KGR? NUjRcpE1UUN3ME21MlcxPSBizszNJC=> MkDTNVg2PTl4MUO=
KP6.3 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH70PYM1KGR? NIrIdGRKSzVyPUGwMlQzQCEQvF2g NGjibW4yQDV3OU[xNy=>
KP7.7 NHPuV41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1O2OlQh\A>? M2HS[WlEPTB;NUegcm0h M4XlZlE5PTV7NkGz
KB2P3.4 NXztfGVNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HSV|Qh\A>? MUjJR|UxRTF{NDDNJC=> Mnu5NVg2PTl4MUO=
KB2P1.21 NG\Z[WdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUS0JIQ> NV73SFR6UUN3ME24PVA4KG6PIB?= NGTIRmgyQDV3OU[xNy=>
U373-MG NFLL[XhEgXSxdH;4bYMhSXO|YYm= M1nYUFEh|ryPIB?= NEPlb5IzPCCq NGDmeIpKdmO{ZXHz[ZMhemGmaXH0bY9vKHOnboPpeIl3cXS7 NULLN48zOTh7NUS3NVI>
T98G NXf0XlFtS3m2b4TvfIlkKEG|c3H5 Mmq1NUDPxE1i MlHZNlQhcA>? NVTvb|gyUW6lcnXhd4V{KHKjZHnheIlwdiC|ZX7zbZRqfmm2eR?= NIfINm8yQDl3NEexNi=>
U87-MG M2XMT2N6fG:2b4jpZ{BCe3OjeR?= NWXPcGtSOSEQvF2g NF;yNpozPCCq MmOwTY5kemWjc3XzJJJi\GmjdHnvckB{\W6|aYTpeol1gQ>? NVz4dFRZOTh7NUS3NVI>
UVW MYjDfZRwfG:6aXOgRZN{[Xl? M1HQXVUxOCCwTR?= NUDERYo4OjRiaB?= NHPjS3ZKdmO{ZXHz[ZMhemGmaXH0bY9vKHOnboPpeIl3cXS7 MYixPFk2PDdzMh?=
HeLa MoPvSpVv[3Srb36gRZN{[Xl? NWTjWIZ{PTByIH7N NIrOPY81KGh? NWDOOHNyS2G3c3XzJIEhdW:mZYP0JIRmdGG7IHnuJJJmcm:rbnnu[{Bw\iC{YXTpZZRqd25vaX7keYNm\CCGTlGgZpJm[Wu| NGmyO40yQDl3NEexNi=>
HeLa NYjDPIFCTnWwY4Tpc44hSXO|YYm= M{iwRVEh|ryPIB?= MWeyOEBp M1z3b2VvcGGwY3XzJJJi\GmjdHnvck1qdmS3Y3XkJHMueGijc3WgZZJz\XO2 MWGxPFk2PDdzMh?=
T98G M3fnZ2Z2dmO2aX;uJGF{e2G7 NGDWeGgyKM7:TTC= Mn3nNlQhcA>? NUTIRm03TW6qYX7j[ZMhemGmaXH0bY9vNWmwZIXj[YQhWy2yaHHz[UBienKnc4S= MoXMNVg6PTR5MUK=
L3 MXjDfZRwfG:6aXOgRZN{[Xl? NFrWdFQ2KM7:TTC= NFLK[m06PiCq MlPKSG1UVw>? MVzTbYdvcW[rY3HueIx6KGmwaHnibZR{KGOnbHygd5Vzfmm4YXy= NYPnOVNTOjBzMkS0OVk>
Granta-519 M3H3e2N6fG:2b4jpZ{BCe3OjeR?= NEiyfGU2KM7:TTC= MmXMPVYhcA>? MYTEUXNQ NFzzUIZUdGmpaITsfUBqdmirYnn0d{Bk\WyuIIP1dpZqfmGu NEjWRYkzODF{NES1PS=>
BT MXnDfZRwfG:6aXOgRZN{[Xl? M3PrRVUh|ryPIB?= NHm5eG06PiCq NXvRNIw6TE2VTx?= MYTTcIlocHSueTDpcohq[mm2czDj[YxtKHO3co\peoFt M2[3R|IxOTJ2NEW5
UPN2 MofZR5l1d3SxeHnjJGF{e2G7 NUjEVWpYPSEQvF2g M3\EfFk3KGh? NX7ueVlYTE2VTx?= MWrTcIlocHSueTDpcohq[mm2czDj[YxtKHO3co\peoFt NGXVdFkzODF{NES1PS=>
HBL-2 NWLJfYNrS3m2b4TvfIlkKEG|c3H5 MXi1JO69VSB? MnXQPVYhcA>? NGTZSZNFVVOR NFy2eWxUdGmpaITsfUBqdmirYnn0d{Bk\WyuIIP1dpZqfmGu MkXENlAyOjR2NUm=
JVM-2 MYDDfZRwfG:6aXOgRZN{[Xl? MmPlOUDPxE1i NFu4fWg6PiCq Mon0SG1UVw>? MmnFV4xq\2i2bImgbY5pcWKrdIOgZ4VtdCC|dYL2bZZidA>? M1fiVVIxOTJ2NEW5
Z138 NFXQOFJEgXSxdH;4bYMhSXO|YYm= NGq5[|Q2KM7:TTC= MUW5OkBp Mm\OSG1UVw>? MVXTcIlocHSueTDpcohq[mm2czDj[YxtKHO3co\peoFt MnTINlAyOjR2NUm=
RWPE MX7JcpZie2m4ZTDBd5NigQ>? MV2yOUDPxE1? MmDLOFghcA>? MkTrSG1UVw>? MoPuV4lodmmoaXPhcpRtgSC{ZXT1Z4V{KEWURz3kdol3\W5iY3XscEBqdn[jc3nvci=> M1jCZ|IyPTd3OE[1
VCaP M3jiOmlvfmG|aY\lJGF{e2G7 NVnD[49WOjVizszN M3\jV|Q5KGh? NXTxN2NSTE2VTx?= NHHFNnBUcWewaX\pZ4FvfGy7IILl[JVk\XNiRWLHMYRzcX[nbjDj[YxtKGmwdnHzbY9v MmjINlE2PzV6NkW=
Mouse H2AX−/− ES Cells M2nlWWN6fG:2b4jpZ{BCe3OjeR?= NUfJfVRMOi53IN88US=> M2W3TlIxKGh? M{nwOXNq\26rZnnjZY51dHliaX7obYJqfHNiY3XscEB{fXK4aY\hcC=> M{nDZVI{OzV3NEi5
Mouse ATM−/− ES Cells NULJbmExS3m2b4TvfIlkKEG|c3H5 MUeyMlUh|ryP NV;DcI9yOjBiaB?= MVnTbYdvcW[rY3HueIx6KGmwaHnibZR{KGOnbHygd5Vzfmm4YXy= M12xVVI{OzV3NEi5
H1650 NIrwdWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW[yNEDPxE1? NGW1THcyPDRiaB?= MUnJR|UxRTF3LkS3JO69VQ>? MmrnNlMzOzl6MEm=
H1650PTEN+ M2DSUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXWyNEDPxE1? NInmWW4yPDRiaB?= M2fU[2lEPTB;NUCuPFMh|ryP NFjIVI8zOzJ|OUiwPS=>
PC-9 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYL3WmdiOjBizszN NH;afJAyPDRiaB?= NFzZSXVKSzVyPUWuPFgh|ryP NYnyVGZUOjN{M{m4NFk>
PC-9PTEN− MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVmyNEDPxE1? MkDxNVQ1KGh? MXnJR|UxRTZwNUKg{txO M3\oZVI{OjN7OEC5
MDA-MB-231 M2KwcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M36yeVUh\GG7 MX;JR|UxRTZwOTFOwG0> NYLF[G4zOjN5NkC0PVY>
MDA-MB-468 NVyyPZBYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2POUVUh\GG7 M{LCZWlEPTB;NT6wJO69VQ>? MWmyN|c3ODR7Nh?=
BT20 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4C1WFUh\GG7 NUXve3RQUUN3ME23Mlch|ryP NE[0R|gzOzd4MES5Oi=>
HCC1143 MmLqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;zNJZVPSCmYYm= NYHGWY9FUUN3ME2xNU4yKM7:TR?= NVrYfHYyOjN5NkC0PVY>
HCC1937 NW\sb|hxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2X0XlUh\GG7 Mn3FTWM2OD1zMj62JO69VQ>? MmrINlM4PjB2OU[=
Hs578t MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUK1JIRigQ>? M1y4emlEPTB;NT62JO69VQ>? M3nJVlI{PzZyNEm2
Hs578t(si) NIe5O3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2niW|Uh\GG7 MYPJR|UxRTdwNTFOwG0> MnPxNlM4PjB2OU[=
BT474 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fyOVUh\GG7 NET2eI5KSzVyPUG5Mlgh|ryP M4rqXFI{PzZyNEm2
JIMT1 NHmw[I9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrpdVg2KGSjeR?= MluwTWM2OD15Lkeg{txO NGWwZ|czOzd4MES5Oi=>
SKBR3 MnHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLt[VBLPSCmYYm= MWLJR|UxRTFzLkGg{txO NUjRfmtUOjN5NkC0PVY>
SUM159 M4XxN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV[1JIRigQ>? Mke0TWM2OD12LkKg{txO MmTlNlM4PjB2OU[=
CAMA1 MlOwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmfFOUBl[Xl? NVPuZWVvUUN3ME2xOU45KM7:TR?= MXuyN|c3ODR7Nh?=
MCF7 M1zMXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTLOUBl[Xl? M{HBZWlEPTB;NT64JO69VQ>? NELZSZAzOzd4MES5Oi=>
T47D MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmHKOUBl[Xl? M362N2lEPTB;OT62JO69VQ>? M{fqfVI{PzZyNEm2
HCT116 NWTlRYVjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\R[FExOCEQvF2= M4n5ZVQ5KGh? MX\EUXNQ MXTJR|UxRTJwNTFOwG0h NX7DS3FVOjR3N{e5OFE>
SW1116 M4S3fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjvPGhpOTByIN88US=> NVTxNVFHPDhiaB?= NYTV[4tbTE2VTx?= NUHVeJd4UUN3ME2xNFAh|ryP MWiyOFU4Pzl2MR?=
HT29 MojVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnLUNVAxKM7:TR?= MUG0PEBp M{LBc2ROW09? MmTiTWM2OD1zND63JO69VQ>? NVLzSpgxOjR3N{e5OFE>
LoVo NVPEdZJHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\UNVExOCEQvF2= NVjLbVh7PDhiaB?= MVXEUXNQ M4PKO2lEPTB;MUOuOEDPxE1? NED3T5MzPDV5N{m0NS=>
HCT-15 NWq3NXk2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{nNZlExOCEQvF2= Mk\sOFghcA>? NW\acFF{TE2VTx?= NETkbY5KSzVyPUGwJO69VQ>? NI[zRpIzPDV5N{m0NS=>
SW48 NVn5bmVuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTDOG0yODBizszN NWHz[ooxPDhiaB?= M3fiT2ROW09? MoD1TWM2OD17LkWg{txO M4DRRlI1PTd5OUSx
C-1 Ml7ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\DNY0yODBizszN NYHwOo13PDhiaB?= M13qSmROW09? M{jXdmlEPTB;Nz62JO69VQ>? Mn;5NlQ2Pzd7NEG=
RKO NX;2UXJbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\sSlExOCEQvF2= M2HnSVQ5KGh? MnW0SG1UVw>? MWTJR|UxRTVwOTFOwG0> NUDuU25JOjR3N{e5OFE>
HCT116 NWjwPFRGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYixNFAh|ryP NEX0XpU1QCCq NVK1RplITE2VTx?= NH3HdnRRd3SnboTpZZRmeyCVTj2zPEBkgXSxdH;4bYNqfHli NVvJdWl5OjR3N{e5OFE>
SW1116 NVm4T3ZQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI[wO|EyODBizszN M{XiS|Q5KGh? M{Dud2ROW09? M1PMbnBwfGWwdHnheIV{KFOQLUO4JIN6fG:2b4jpZ4l1gSB? NYe0WlI4OjR3N{e5OFE>
HT29 M33Id2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;DPGoyODBizszN MYC0PEBp MnjiSG1UVw>? M2noPHBwfGWwdHnheIV{KFOQLUO4JIN6fG:2b4jpZ4l1gSB? MVyyOFU4Pzl2MR?=
LoVo MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVexNFAh|ryP M1\2OVQ5KGh? NFq0fWhFVVOR NIfib5BRd3SnboTpZZRmeyCVTj2zPEBkgXSxdH;4bYNqfHli M2fvTFI1PTd5OUSx
SW48 NVTiRYpzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3MNVAxKM7:TR?= MmOwOFghcA>? NXrNfHQ{TE2VTx?= M2DpU3BwfGWwdHnheIV{KFOQLUO4JIN6fG:2b4jpZ4l1gSB? NHjDflUzPDV5N{m0NS=>
C-1 M{XqSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX[zRXQ2OTByIN88US=> Mn;oOFghcA>? MmDaSG1UVw>? M1;kfnBwfGWwdHnheIV{KFOQLUO4JIN6fG:2b4jpZ4l1gSB? NH3ONmMzPDV5N{m0NS=>
RKO NXTIXJZ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUOxNFAh|ryP NGHPSJg1QCCq MX3EUXNQ M1\pUHBwfGWwdHnheIV{KFOQLUO4JIN6fG:2b4jpZ4l1gSB? NEfIZ4QzPDV5N{m0NS=>
HCT116 M3fmOGZ2dmO2aX;uJGF{e2G7 M4XiclExKG6P M2n4TVEzKGh? NFXyVYNFVVOR NIO1WZZKdmO{ZXHz[ZMhTE6DIHTveYJt\S2|dILhcoQh[nKnYXvzJIlv\HWlZXSgZpkhW05vM{i= MlXINlQ2Pzd7NEG=
HT29 M3LUdWZ2dmO2aX;uJGF{e2G7 MlTaNVAhdk1? MWmxNkBp NGn5PG9FVVOR MlPETY5kemWjc3XzJGRPSSCmb4XicIUue3S{YX7kJIJz\WGtczDpcoR2[2WmIHL5JHNPNTN6 NWPMNlFkOjR3N{e5OFE>
TE-6 MnrJSpVv[3Srb36gRZN{[Xl? NGjHbZM2KM7:TTC= NXTOR3dwOTJiaB?= NVnxRnZJTE2VTx?= MmC0TY5lfWOnczDHNk9OKGG{cnXzeC=> MUiyOFIyQTF4NB?=
TE-6 NWnvVW9jTnWwY4Tpc44hSXO|YYm= NHjaRo82KM7:TTC= M4DaOlI1KGh? NILNPXFFVVOR MnPLTY5kemWjc3XzJIlvKGSxdXLs[UB{fHKjbnSgZpJm[Wu|IDjEV2J{MQ>? MVmyOFIyQTF4NB?=
Hep3B MlP1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYL4bnpxPDBizszNJC=> NV;xcHZ2PzJiaB?= NUHOeo1yTE2VTx?= MWXTfY5memerc4TpZ4FtdHliaX7obYJqfHNiY3XscEBoem:5dHige4l1cCCGSF3FVS=> MWWyOVA4Ojd3Mh?=
Huh7 MlXWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXpS2w1OCEQvF2g Mli1O|IhcA>? MlPiSG1UVw>? M4TifHN6dmW{Z3nzeIlk[WyueTDpcohq[mm2czDj[YxtKGe{b4f0bEB4cXSqIFTIUWVS NEfqUGszPTB5Mke1Ni=>
Hep3B MUnGeY5kfGmxbjDBd5NigQ>? NVHCXFYxPDBizszNJC=> NYLHcWNNOjRiaB?= NF7SOHhFVVOR NE\hOmpKdmS3Y3XzJHJQWyCycn;keYN1cW:wIIfpeIghTEiPRWG= M4SxWVI2ODd{N{Wy
Huh7 M1fTW2Z2dmO2aX;uJGF{e2G7 M3vOUFQxKM7:TTC= MYGyOEBp NFW4SWlFVVOR M{C1Rmlv\HWlZYOgVm9UKHC{b3T1Z5Rqd25id3n0bEBFUE2HUR?= NGDZVmwzPTB5Mke1Ni=>
Hep3B NI[xNYhHfW6ldHnvckBCe3OjeR?= NUPIPVN1PDBizszNJC=> NIDP[GIzPCCq MnW4SG1UVw>? MXjJcoR2[2W|IHPlcIwh[XW2b4DoZYd6KHerdHigSGhOTVF? Mm[zNlUxPzJ5NUK=
Huh7 MX\GeY5kfGmxbjDBd5NigQ>? NXfLcGVbPDBizszNJC=> MWWyOEBp NYK4eFJCTE2VTx?= M3L4VWlv\HWlZYOgZ4VtdCCjdYTvdIhi\3lid3n0bEBFUE2HUR?= M134UVI2ODd{N{Wy
SGC-7901 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jJXVMxyqEQvF2= NXW4WG0zPDhiaB?= NWLUR|dOTE2VTx?= NUnGS5l{SmyxY3ugc5hidGmybHH0bY4ucW6mdXPl[EBk\WyuIHTlZZRp MXqyOVc3PzB5Nh?=
COLO-800 M1n2V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVLHeVRDUUN3ME2wMlQ1OTZ2IN88US=> M2WzfXNCVkeHUh?=
EoL-1- M4XPNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTBwNU[0OFYh|ryP MojVV2FPT0WU
NCI-H209 NYH5Zo56T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{PXeGlEPTB;MD65NVU2PiEQvF2= MV3TRW5ITVJ?
ES1 NHrFcIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NILOXHdKSzVyPUGuNVE1ODhizszN Mn3nV2FPT0WU
NKM-1 M3y3Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPKfHBRUUN3ME2xMlI2OzR5IN88US=> MkK1V2FPT0WU
NTERA-S-cl-D1 Ml3mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mom4TWM2OD1zLkOzN|QyKM7:TR?= M1rlVnNCVkeHUh?=
MHH-ES-1 MkGwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTaWlVuUUN3ME2xMlYzODZ5IN88US=> MkH0V2FPT0WU
ES8 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DpcGlEPTB;MT63NlQyPCEQvF2= M{i0VXNCVkeHUh?=
NCI-H720 M2HIRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HRTWlEPTB;Mj6yNFY6QSEQvF2= NIPnZopUSU6JRWK=
EW-3 M2TsdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHTWYpKSzVyPUKuNlc2OzRizszN NFLzcnhUSU6JRWK=
D-566MG M3fqc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY[0TlBWUUN3ME2yMlQ1PTZ6IN88US=> MoPLV2FPT0WU
697 M1zjcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjBb5BsUUN3ME2yMlg1OTd|IN88US=> M{KwVHNCVkeHUh?=
ES5 NXi4RWVpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEH1NI5KSzVyPUKuPFgyQDlizszN MXPTRW5ITVJ?
COLO-684 MmGyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLpTYROUUN3ME2zMlUyPjl4IN88US=> M3m1TnNCVkeHUh?=
ML-2 M2e0dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\1NmlEPTB;Mz62NFA2QCEQvF2= MlvpV2FPT0WU
MC-IXC MnjaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4ntfGlEPTB;Mz62N|M6OyEQvF2= NH7xZ4dUSU6JRWK=
DB NIrWWIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPWfINKSzVyPUOuOlU1PDhizszN NYHSRnF4W0GQR1XS
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KG-1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXLJR|UxRTR|LkO5OEDPxE1? MUDTRW5ITVJ?
GP5d MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUi0VWUzUUN3ME20OE4xPjZ4IN88US=> M{D0OnNCVkeHUh?=
MFM-223 M2L5Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{PsN2lEPTB;NESuNVIzQCEQvF2= NXTYOlkyW0GQR1XS
OAW-42 M{HNfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1faN2lEPTB;NESuNlY1OyEQvF2= M2e5NXNCVkeHUh?=
C8166 NU\CNIM6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTR3LkC4NlIh|ryP NXXq[pVoW0GQR1XS
LU-99A M1XNUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLPTWM2OD12Nj6xN|IzKM7:TR?= MUPTRW5ITVJ?
NCI-H23 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfvS3NKSzVyPUS2MlE4QDVizszN NHLrdoNUSU6JRWK=
HO-1-N-1 MlLrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTR5LkC5PVgh|ryP M1jXeHNCVkeHUh?=
A3-KAW M2O5e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHUXpk2UUN3ME20O{4yODB5IN88US=> M37wXHNCVkeHUh?=
CGTH-W-1 NGLyT2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTR5LkWwOlkh|ryP Mnj4V2FPT0WU
DJM-1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTR5LkW0NVMh|ryP NWXu[FFTW0GQR1XS
A101D M2HsUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmK5TWM2OD12Nz62N|U4KM7:TR?= MX\TRW5ITVJ?
BB30-HNC NH3PVHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofLTWM2OD12OD6zNFczKM7:TR?= MUPTRW5ITVJ?
T98G Mn\HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4fWdGlEPTB;NEiuOFY{OyEQvF2= M1fTc3NCVkeHUh?=
NCI-H1573 M4n3W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4PIeGlEPTB;NEmuOFQ3OiEQvF2= MoL3V2FPT0WU
MEG-01 M{\1Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFrpU4tKSzVyPUS5Mlc1OTFizszN M176bXNCVkeHUh?=
WM-115 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTR7LkmyNlIh|ryP M3THNnNCVkeHUh?=

... 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)

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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

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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.

selleck catalog

PARP Signaling Pathway Map

PARP Inhibitors with Unique Features

  • Selective PARP Inhibitors

    AG-14361 : PARP1-selective, Ki<5 nM.

  • Selective PARP Inhibitors

    UPF 1069 : PARP2-selective, IC50=0.3 μM.

  • Most Potent PARP Inhibitor

    MK-4827 (Niraparib) : PARP1, IC50=3.8 nM; PARP2, IC50=2.1 nM.

  • PARP Inhibitor in Clinical Trial

    Iniparib (BSI-201) : Phase III for solid tumors.

  • Newest PARP Inhibitor

    BMN 673 : Novel PARP inhibitor with IC50 of 0.58 nM. Also a potent inhibitor of PARP-2, but does not inhibit PARG and highly sensitive to PTEN mutation.

Related PARP Products

  • G007-LK New

    G007-LK is a potent and selective tankyrase inhibitor with IC50 of 46 nM and 25 nM for TNKS1/2, respectively.

  • NU1025 New

    NU1025 is a potent PARP inhibitor with IC50 of 400 nM.

  • SCR7 New

    SCR7 is a specific DNA Ligase IV inhibitor, which blocks nonhomologous end-joining (NHEJ). It increases the efficiency of HDR-mediated genome editing up to 19-fold using CRISPR/Cas9 in mammalian cells and mouse embryos.

  • Veliparib (ABT-888)

    Veliparib (ABT-888) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM in cell-free assays, respectively. It is inactive to SIRT2. Phase 3.

    Features:Increases the efficacy of common cancer therapies such as radiation and alkylating agents.

  • Rucaparib (AG-014699) phosphate

    Rucaparib (AG-014699, PF-01367338) is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains. Phase 3.

    Features:The first PARP inhibitor used in clinical trials combined with temozolomide.

  • Talazoparib (BMN 673)

    Talazoparib (BMN 673) is a novel PARP inhibitor with IC50 of 0.57 nM for PARP1 in a cell-free assay. It is also a potent inhibitor of PARP-2, but does not inhibit PARG and is highly sensitive to PTEN mutation. Phase 3.

    Features:Most potent and selective PARPi reported thus far.

  • Iniparib (BSI-201)

    Iniparib (BSI-201) is a PARP1 inhibitor with demonstrated effectiveness in triple-negative breast cancer (TNBC). Phase 3.

  • PJ34 HCl

    PJ34 HCl is the hydrochloride salt of PJ34, which is a PARP inhibitor with EC50 of 20 nM and is equally potent to PARP1/2.

    Features:Water-soluble PARP1/2 inhibitor with >10,000-fold potentcy vs. 3-aminobenzamide (prototypical PARP inhibitor). Potential uses in cardiovascular diseases (stroke, cerebral ischemia, & myocardial ischemia).

  • AG-14361

    AG14361 is a potent inhibitor of PARP1 with Ki of <5 nM in a cell-free assay. It is at least 1000-fold more potent than the benzamides.

    Features:The 1st high-potency PARP-1 inhibitor with the specificity & in vivo activity to enhance chemotherapy and radiation therapy of human cancers.

  • A-966492

    A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively.

    Features:A promising, structurally diverse benzimidazole analogue that is being further characterized preclinically.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID