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 349 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 NXLmU4hRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm[wOEBl NEn5XmdKSzVyPUWuO|A2KCEQvF2g MmXaNVg2PTl4MUO=
KP6.3 MkXSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4PZUlQh\A>? MU\JR|UxRTFyLkSyPEDPxE1i NVnuPHVSOTh3NUm2NVM>
KP7.7 NXLmcHJpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfa[YM1KGR? NHOyW5JKSzVyPUW3JI5OKA>? M4PxclE5PTV7NkGz
KB2P3.4 MofmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUO0JIQ> NWLFfZQzUUN3ME2xNlQhVSB? M4HRPFE5PTV7NkGz
KB2P1.21 MmTYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWj6XFRiPCCm NVH6SJhIUUN3ME24PVA4KG6PIB?= MoizNVg2PTl4MUO=
U373-MG NF;WWFVEgXSxdH;4bYMhSXO|YYm= MnzhNUDPxE1i MVKyOEBp NH7EWoVKdmO{ZXHz[ZMhemGmaXH0bY9vKHOnboPpeIl3cXS7 NVnZU5k5OTh7NUS3NVI>
T98G MlfrR5l1d3SxeHnjJGF{e2G7 MX[xJO69VSB? NFnNPI0zPCCq NV;kdI4yUW6lcnXhd4V{KHKjZHnheIlwdiC|ZX7zbZRqfmm2eR?= MnK1NVg6PTR5MUK=
U87-MG NYexSFM6S3m2b4TvfIlkKEG|c3H5 NX3aWoFDOSEQvF2g NGm2O4szPCCq M2TtWWlv[3KnYYPld{Bz[WSrYYTpc44he2Wwc3n0bZZqfHl? MX[xPFk2PDdzMh?=
UVW NWHK[GJGS3m2b4TvfIlkKEG|c3H5 MWG1NFAhdk1? MoP4NlQhcA>? NFXvRmdKdmO{ZXHz[ZMhemGmaXH0bY9vKHOnboPpeIl3cXS7 NHPrU40yQDl3NEexNi=>
HeLa M1u0TGZ2dmO2aX;uJGF{e2G7 M1TXRVUxOCCwTR?= MoXjOEBp NVWxVHFCS2G3c3XzJIEhdW:mZYP0JIRmdGG7IHnuJJJmcm:rbnnu[{Bw\iC{YXTpZZRqd25vaX7keYNm\CCGTlGgZpJm[Wu| M2j2NFE5QTV2N{Gy
HeLa MXjGeY5kfGmxbjDBd5NigQ>? MorVNUDPxE1i NEe2epgzPCCq NIXiboxGdmijbnPld{Bz[WSrYYTpc44ucW6mdXPl[EBUNXCqYYPlJIFzemW|dB?= NX6weY1oOTh7NUS3NVI>
T98G M2fSWGZ2dmO2aX;uJGF{e2G7 M4C3cFEh|ryPIB?= NU\HOVlmOjRiaB?= MV;FcohidmOnczDyZYRq[XSrb36tbY5lfWOnZDDTMZBp[XOnIHHydoV{fA>? NEDrN3oyQDl3NEexNi=>
L3 NYDkXIVnS3m2b4TvfIlkKEG|c3H5 MV[1JO69VSB? MWG5OkBp M3vUc2ROW09? MWfTbYdvcW[rY3HueIx6KGmwaHnibZR{KGOnbHygd5Vzfmm4YXy= NIfESWszODF{NES1PS=>
Granta-519 MXzDfZRwfG:6aXOgRZN{[Xl? NI\pe3o2KM7:TTC= NYDGNWN3QTZiaB?= NUnp[pZXTE2VTx?= NITz[29UdGmpaITsfUBqdmirYnn0d{Bk\WyuIIP1dpZqfmGu M3XhRVIxOTJ2NEW5
BT NIPvcoJEgXSxdH;4bYMhSXO|YYm= Mn;2OUDPxE1i MVO5OkBp NHfHOWtFVVOR NGWyU4hUdGmpaITsfUBqdmirYnn0d{Bk\WyuIIP1dpZqfmGu MV:yNFEzPDR3OR?=
UPN2 NYfCeGJVS3m2b4TvfIlkKEG|c3H5 NV\QUI94PSEQvF2g M3zBflk3KGh? NEDCNFlFVVOR M4jlcnNtcWeqdHz5JIlvcGmkaYTzJINmdGxic4Xyeol3[Wx? M4L1bFIxOTJ2NEW5
HBL-2 MUjDfZRwfG:6aXOgRZN{[Xl? MnjCOUDPxE1i MnvrPVYhcA>? NG\sToFFVVOR NYHIZYJrW2yrZ3j0cJkhcW6qaXLpeJMh[2WubDDzeZJ3cX[jbB?= M17TSVIxOTJ2NEW5
JVM-2 NH7ZdIJEgXSxdH;4bYMhSXO|YYm= MlPaOUDPxE1i NVPhb3ZKQTZiaB?= NXvXPIMxTE2VTx?= MlLjV4xq\2i2bImgbY5pcWKrdIOgZ4VtdCC|dYL2bZZidA>? M3fxRVIxOTJ2NEW5
Z138 MW\DfZRwfG:6aXOgRZN{[Xl? NXrEOmtxPSEQvF2g MkPGPVYhcA>? M1fBWWROW09? Mo\zV4xq\2i2bImgbY5pcWKrdIOgZ4VtdCC|dYL2bZZidA>? M4n3cFIxOTJ2NEW5
RWPE MW\JcpZie2m4ZTDBd5NigQ>? M4DYWlI2KM7:TR?= M1L1PFQ5KGh? MkXGSG1UVw>? MmTBV4lodmmoaXPhcpRtgSC{ZXT1Z4V{KEWURz3kdol3\W5iY3XscEBqdn[jc3nvci=> M1PUZlIyPTd3OE[1
VCaP NXzHd2ZHUW64YYPpeoUhSXO|YYm= NVe2cnd{OjVizszN NYfHTHl{PDhiaB?= MkfpSG1UVw>? Moe1V4lodmmoaXPhcpRtgSC{ZXT1Z4V{KEWURz3kdol3\W5iY3XscEBqdn[jc3nvci=> NUnw[VFWOjF3N{W4OlU>
Mouse H2AX−/− ES Cells Mon0R5l1d3SxeHnjJGF{e2G7 M37Wb|IvPSEQvF2= NFiyUY0zOCCq NEjnfWxUcWewaX\pZ4FvfGy7IHnubIljcXS|IHPlcIwhe3W{dnn2ZYw> NYXJSXEzOjN|NUW0PFk>
Mouse ATM−/− ES Cells NIOyVWFEgXSxdH;4bYMhSXO|YYm= MoniNk42KM7:TR?= M2jPclIxKGh? NGG1TnRUcWewaX\pZ4FvfGy7IHnubIljcXS|IHPlcIwhe3W{dnn2ZYw> MYWyN|M2PTR6OR?=
H1650 M1XCSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWGyNEDPxE1? MVuxOFQhcA>? MUjJR|UxRTF3LkS3JO69VQ>? MWmyN|I{QThyOR?=
H1650PTEN+ NWrlNZRHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFeyOIEzOCEQvF2= NFHIeGYyPDRiaB?= NUnSZpV{UUN3ME21NE45OyEQvF2= MkexNlMzOzl6MEm=
PC-9 NID4T4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzJe3MzOCEQvF2= MmXlNVQ1KGh? M331R2lEPTB;NT64PEDPxE1? Ml;HNlMzOzl6MEm=
PC-9PTEN− NH7W[ZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\QNJUzOCEQvF2= NUfJWGFXOTR2IHi= MUDJR|UxRTZwNUKg{txO MoXQNlMzOzl6MEm=
MDA-MB-231 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYO1JIRigQ>? MnjLTWM2OD14Lkmg{txO MWOyN|c3ODR7Nh?=
MDA-MB-468 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV76OGF3PSCmYYm= MWXJR|UxRTVwMDFOwG0> M{TrTVI{PzZyNEm2
BT20 MkflS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3VOUBl[Xl? NEHtW5VKSzVyPUeuO{DPxE1? Ml7INlM4PjB2OU[=
HCC1143 NI\ZNnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvmT3RRPSCmYYm= NHvi[opKSzVyPUGxMlEh|ryP NUPOcVVbOjN5NkC0PVY>
HCC1937 MoP0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnSO5J6PSCmYYm= NIrUb|VKSzVyPUGyMlYh|ryP NHnmRVYzOzd4MES5Oi=>
Hs578t Mm\3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDMUGE2KGSjeR?= MUDJR|UxRTVwNjFOwG0> MnnCNlM4PjB2OU[=
Hs578t(si) MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW[1JIRigQ>? M2fkOWlEPTB;Nz61JO69VQ>? Ml\5NlM4PjB2OU[=
BT474 NYjMR5lPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWK1JIRigQ>? NH3zPIxKSzVyPUG5Mlgh|ryP NFjQ[mwzOzd4MES5Oi=>
JIMT1 MorrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4DIU|Uh\GG7 MYfJR|UxRTdwNzFOwG0> NI\3W3UzOzd4MES5Oi=>
SKBR3 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV:1JIRigQ>? MnfvTWM2OD1zMT6xJO69VQ>? NYjoWlM1OjN5NkC0PVY>
SUM159 NVTTXZg5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIi0SI42KGSjeR?= NYXDeVdNUUN3ME20MlIh|ryP M3;vOlI{PzZyNEm2
CAMA1 NVGy[2VDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVOxb5pTPSCmYYm= M2fITWlEPTB;MUWuPEDPxE1? M1riOVI{PzZyNEm2
MCF7 NFPNZ5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;mV|Uh\GG7 MoK5TWM2OD13Lkig{txO M3jNXFI{PzZyNEm2
T47D NY[3[5h1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmLmOUBl[Xl? NULKXIptUUN3ME25MlYh|ryP Mn7MNlM4PjB2OU[=
HCT116 NXrsO4toT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYCxXVVyOTByIN88US=> MnTEOFghcA>? M4XaVWROW09? MV3JR|UxRTJwNTFOwG0h M1nWRVI1PTd5OUSx
SW1116 NV\zbmZNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjHeoIyODBizszN NGnncJY1QCCq MkPBSG1UVw>? NUPoU5g6UUN3ME2xNFAh|ryP MXqyOFU4Pzl2MR?=
HT29 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWC1XHJnOTByIN88US=> NVjlfGlkPDhiaB?= NWrH[|VpTE2VTx?= MVXJR|UxRTF2Lkeg{txO M{PTRlI1PTd5OUSx
LoVo MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTvNVAxKM7:TR?= M1u2[FQ5KGh? MVrEUXNQ M{XheWlEPTB;MUOuOEDPxE1? NXW2WXd6OjR3N{e5OFE>
HCT-15 Mn3rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vPV|ExOCEQvF2= M3KydVQ5KGh? MlfESG1UVw>? NEjifnJKSzVyPUGwJO69VQ>? NYPBemN7OjR3N{e5OFE>
SW48 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXr2SI9EOTByIN88US=> NXzySo9wPDhiaB?= MlnuSG1UVw>? NW[3S2M{UUN3ME25MlUh|ryP MlmwNlQ2Pzd7NEG=
C-1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVSxNFAh|ryP NXzFW4R4PDhiaB?= MYDEUXNQ MX3JR|UxRTdwNjFOwG0> NYX0NpRjOjR3N{e5OFE>
RKO NYGzcVB[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVjnUXZXOTByIN88US=> M4TQWFQ5KGh? M1\KPGROW09? NFuwZ|NKSzVyPUWuPUDPxE1? NXLGb5RKOjR3N{e5OFE>
HCT116 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzse41EOTByIN88US=> NUPZV5BuPDhiaB?= M3z0[GROW09? MoPYVI91\W62aXH0[ZMhW05vM{igZ5l1d3SxeHnjbZR6KA>? NHLjO5gzPDV5N{m0NS=>
SW1116 NI\CfWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1GyblExOCEQvF2= NYXmNpZKPDhiaB?= M3fkdGROW09? Mnq2VI91\W62aXH0[ZMhW05vM{igZ5l1d3SxeHnjbZR6KA>? MljKNlQ2Pzd7NEG=
HT29 NX;peodbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXtNJRoOTByIN88US=> NEW2eHk1QCCq MnLiSG1UVw>? NXfDOVcxWG:2ZX70bYF1\XNiU16tN|gh[3m2b4TvfIlkcXS7IB?= NFuwW5YzPDV5N{m0NS=>
LoVo M{jOZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGLSNVMyODBizszN MkG4OFghcA>? NF[3SIpFVVOR M1rtcHBwfGWwdHnheIV{KFOQLUO4JIN6fG:2b4jpZ4l1gSB? NIjzOIQzPDV5N{m0NS=>
SW48 M1nDU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfZNVAxKM7:TR?= Mln4OFghcA>? M3vqd2ROW09? NYjrdopFWG:2ZX70bYF1\XNiU16tN|gh[3m2b4TvfIlkcXS7IB?= NEjFRXAzPDV5N{m0NS=>
C-1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPDcVJXOTByIN88US=> M2HOc|Q5KGh? MmDPSG1UVw>? M2nxSHBwfGWwdHnheIV{KFOQLUO4JIN6fG:2b4jpZ4l1gSB? MViyOFU4Pzl2MR?=
RKO NF3wNFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXWUlcyODBizszN NGPXNFY1QCCq NFqye4pFVVOR M2D2cnBwfGWwdHnheIV{KFOQLUO4JIN6fG:2b4jpZ4l1gSB? M4jmfFI1PTd5OUSx
HCT116 MoPHSpVv[3Srb36gRZN{[Xl? MmXkNVAhdk1? Mle3NVIhcA>? NHn2VI9FVVOR MV7JcoNz\WG|ZYOgSG5CKGSxdXLs[U1{fHKjbnSgZpJm[Wu|IHnu[JVk\WRiYomgV24uOzh? Mmm5NlQ2Pzd7NEG=
HT29 NYf0N2NoTnWwY4Tpc44hSXO|YYm= NGnSWG8yOCCwTR?= MnLjNVIhcA>? NVv4NJdJTE2VTx?= M4rH[Wlv[3KnYYPld{BFVkFiZH;1ZoxmNXO2cnHu[EBjemWja4OgbY5lfWOnZDDifUBUVi1|OB?= MU[yOFU4Pzl2MR?=
TE-6 MUXGeY5kfGmxbjDBd5NigQ>? NH;wdpY2KM7:TTC= NGPPNm0yOiCq NGrXVlZFVVOR NVLWXJhLUW6mdXPld{BIOi:PIHHydoV{fA>? M{fLelI1OjF7MU[0
TE-6 NHfGUJpHfW6ldHnvckBCe3OjeR?= M{nme|Uh|ryPIB?= NGGxOY4zPCCq MnH6SG1UVw>? M1;Lcmlv[3KnYYPld{BqdiCmb4XicIUhe3S{YX7kJIJz\WGtczCoSHNDeyl? MYKyOFIyQTF4NB?=
Hep3B M4G3eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2f0RVQxKM7:TTC= NXThe|doPzJiaB?= NVrtdIs2TE2VTx?= M4DX[3N6dmW{Z3nzeIlk[WyueTDpcohq[mm2czDj[YxtKGe{b4f0bEB4cXSqIFTIUWVS MV2yOVA4Ojd3Mh?=
Huh7 M4C2T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXS0NEDPxE1i NH3HO4I4OiCq MWXEUXNQ MUPTfY5memerc4TpZ4FtdHliaX7obYJqfHNiY3XscEBoem:5dHige4l1cCCGSF3FVS=> MmK3NlUxPzJ5NUK=
Hep3B NIXhTlNHfW6ldHnvckBCe3OjeR?= MV20NEDPxE1i NFzEPG4zPCCq MlzTSG1UVw>? NV:xeVM3UW6mdXPld{BTV1NicILv[JVkfGmxbjD3bZRpKESKTVXR MViyOVA4Ojd3Mh?=
Huh7 NVHKVpNjTnWwY4Tpc44hSXO|YYm= M1KwWVQxKM7:TTC= M1qyO|I1KGh? MUfEUXNQ NWjISm9DUW6mdXPld{BTV1NicILv[JVkfGmxbjD3bZRpKESKTVXR NW\h[G1TOjVyN{K3OVI>
Hep3B M1\wWGZ2dmO2aX;uJGF{e2G7 MXW0NEDPxE1i MnLENlQhcA>? NIXVcG1FVVOR MXXJcoR2[2W|IHPlcIwh[XW2b4DoZYd6KHerdHigSGhOTVF? M{LLZlI2ODd{N{Wy
Huh7 NVLs[I5CTnWwY4Tpc44hSXO|YYm= MYG0NEDPxE1i Mlz4NlQhcA>? NVW4fll4TE2VTx?= NYPXdIlsUW6mdXPld{Bk\WyuIHH1eI9xcGGpeTD3bZRpKESKTVXR NWm1cYZ[OjVyN{K3OVI>
SGC-7901 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVHWSo9[OzEEoN88US=> NUTiTXlHPDhiaB?= M375W2ROW09? NVzLWnJiSmyxY3ugc5hidGmybHH0bY4ucW6mdXPl[EBk\WyuIHTlZZRp MYmyOVc3PzB5Nh?=
COLO-800 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjBTWM2OD1yLkS0NVY1KM7:TR?= MofyV2FPT0WU
EoL-1- NEmyWHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlrmTWM2OD1yLkW2OFQ3KM7:TR?= M3W5e3NCVkeHUh?=
NCI-H209 NHn5PXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHROGRKSzVyPUCuPVE2PTZizszN M3\0cHNCVkeHUh?=
ES1 MkDXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7hTWM2OD1zLkGxOFA5KM7:TR?= NEPWPVJUSU6JRWK=
NKM-1 NGf1V2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjKR4ZRUUN3ME2xMlI2OzR5IN88US=> NUfZXnZ4W0GQR1XS
NTERA-S-cl-D1 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTFwM{OzOFEh|ryP MWDTRW5ITVJ?
MHH-ES-1 M4Xrb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTFwNkKwOlch|ryP MoXTV2FPT0WU
ES8 NEjDRVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUP3UIRXUUN3ME2xMlczPDF2IN88US=> NYjM[mRDW0GQR1XS
NCI-H720 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTJwMkC2PVkh|ryP NG\KW2tUSU6JRWK=
EW-3 M4TIXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTJwMke1N|Qh|ryP MXXTRW5ITVJ?
D-566MG M3vxT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTJwNES1Olgh|ryP NULteHN{W0GQR1XS
697 NFT0SpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYrpboM2UUN3ME2yMlg1OTd|IN88US=> MlrQV2FPT0WU
ES5 NHfQN3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWT2WWg{UUN3ME2yMlg5OTh7IN88US=> Mn32V2FPT0WU
COLO-684 M2CyZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTNwNUG2PVYh|ryP MWTTRW5ITVJ?
ML-2 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEP1coZKSzVyPUOuOlAxPThizszN NUPueGQ5W0GQR1XS
MC-IXC M3y2dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknjTWM2OD1|Lk[zN|k{KM7:TR?= NGXXbnJUSU6JRWK=
DB Mln0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWToS4diUUN3ME2zMlY2PDR6IN88US=> M{CyN3NCVkeHUh?=
HCC2218 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDyTWM2OD1|LkezNVA{KM7:TR?= NVO5[IVMW0GQR1XS
NCI-H510A MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4GwbmlEPTB;Mz64NlczPCEQvF2= M2LvNXNCVkeHUh?=
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MFM-223 MofMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jNeWlEPTB;NESuNVIzQCEQvF2= MnHCV2FPT0WU
OAW-42 NWnENZFwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlTUTWM2OD12ND6yOlQ{KM7:TR?= M2jr[3NCVkeHUh?=
C8166 M17ONGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NID2UZlKSzVyPUS1MlA5OjJizszN NXHqNmx6W0GQR1XS
LU-99A NFrEUXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;XPWlEPTB;NE[uNVMzOiEQvF2= M{TBXXNCVkeHUh?=
NCI-H23 M2DJOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DaVWlEPTB;NE[uNVc5PSEQvF2= MkPJV2FPT0WU
HO-1-N-1 M37ubGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXDSWNKSzVyPUS3MlA6QThizszN M4rqTnNCVkeHUh?=
A3-KAW NHe2WmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rhR2lEPTB;NEeuNVAxPyEQvF2= MWTTRW5ITVJ?
CGTH-W-1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\4fItKSzVyPUS3MlUxPjlizszN MmD2V2FPT0WU
DJM-1 MmXSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3XTWM2OD12Nz61OFE{KM7:TR?= NU[ydnZ{W0GQR1XS
A101D MkT5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTR5Lk[zOVch|ryP MULTRW5ITVJ?
BB30-HNC NGfTcVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETkO2FKSzVyPUS4MlMxPzJizszN MkD6V2FPT0WU
T98G NGXQTGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\TRpJKSzVyPUS4MlQ3OzNizszN NXnBWYZJW0GQR1XS
NCI-H1573 MknES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmfKTWM2OD12OT60OFYzKM7:TR?= NUW3VXVIW0GQR1XS
MEG-01 NWjtU4FUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzhWnFlUUN3ME20PU44PDFzIN88US=> NVzwWll4W0GQR1XS
WM-115 M1nyWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnq3TWM2OD12OT65NlIzKM7:TR?= MVXTRW5ITVJ?

... 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 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:

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.

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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