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Olaparib (AZD2281)

Name: Olaparib (AZD2281)
Brand: Selleck Chemicals
SKU: S1060
Rating: 5 (815 reviews)

Catalog No.S1060 Synonyms: Ku-0059436

For research use only.

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. Olaparib induces significant autophagy that is associated with mitophagy in cells with BRCA mutations.

CAS No. 763113-22-0

Selleck's Olaparib (AZD2281) has been cited by 815 publications

Purity & Quality Control

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PARP Signaling Pathway Map

Biological Activity

Description

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

Hep3B	MXnGeY5kfGmxbjDBd5NigQ>?	MnTNOFAh\|ryP	MUeyOEBp	NUDLT4hWTE2VTx?=	NYHPNpYxUW6mdXPld{BTV1NicILv[JVkfGmxbjD3bZRpKESKTVXR	NVntNVdXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwO\|I4PTJpPkK1NFczPzV{PD;hQi=>
Huh7	NF3SdFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MXW0NEDPxE1?	M2rOOFczKGh?	NIH2dGhFVVOR	Mk\SV5lv\XKpaYP0bYNidGy7IHnubIljcXS\|IHPlcIwh\3Kxd4ToJJdqfGhiRFjNSXE>	NEPFTpI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC3Nlc2Oid-MkWwO\|I4PTJ:L3G+
Hep3B	M4\T[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MnXYOFAh\|ryP	NVPwdHFNPzJiaB?=	M1jXUGROW09?	NYW4e2E2W3mwZYLnbZN1cWOjbHz5JIlvcGmkaYTzJINmdGxiZ4Lve5RpKHerdHigSGhOTVF?	MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB5Mke1Nkc,OjVyN{K3OVI9N2F-
TE-6	NH7JbXBHfW6ldHnvckBCe3OjeR?=	M4DkUlUh\|ryP	M4frNVI1KGh?	NH\qUHZFVVOR	M1PWWGlv[3KnYYPld{BqdiCmb4XicIUhe3S{YX7kJIJz\WGtczCoSHNDeyl?	NYXpPJNHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyNVkyPjRpPkK0NlE6OTZ2PD;hQi=>
TE-6	M1zRPGZ2dmO2aX;uJGF{e2G7	NXnJVYVXPSEQvF2=	Ml65NVIhcA>?	NE\NR5VFVVOR	MYDJcoR2[2W\|IFeyM20h[XK{ZYP0	NF7ifZA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEKxPVE3PCd-MkSyNVkyPjR:L3G+
HT29	MmXtSpVv[3Srb36gRZN{[Xl?	NXjn[4dDOTBibl2=	M4KxTFEzKGh?	M1HuSmROW09?	MkLVTY5kemWjc3XzJGRPSSCmb4XicIUue3S{YX7kJIJz\WGtczDpcoR2[2WmIHL5JHNPNTN6	Mn\ZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3N{e5OFEoRjJ2NUe3PVQyRC:jPh?=
HCT116	MkS0SpVv[3Srb36gRZN{[Xl?	NEHWU2gyOCCwTR?=	NYnmPYJnOTJiaB?=	NGLIenVFVVOR	MWrJcoNz\WG\|ZYOgSG5CKGSxdXLs[U1{fHKjbnSgZpJm[Wu\|IHnu[JVk\WRiYomgV24uOzh?	MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV5N{m0NUc,OjR3N{e5OFE9N2F-
RKO	NX;IPWtvT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NUfze2xxOTByIN88US=>	M4fxblQ5KGh?	MYHEUXNQ	Ml:2VI91\W62aXH0[ZMhW05vM{igZ5l1d3SxeHnjbZR6	MmXxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3N{e5OFEoRjJ2NUe3PVQyRC:jPh?=
C-1	M3P6OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NX\xeIx3OTByIN88US=>	NHH1THc1QCCq	M{faPWROW09?	MoSwVI91\W62aXH0[ZMhW05vM{igZ5l1d3SxeHnjbZR6	M{LxdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NUe3PVQyLz5{NEW3O\|k1OTxxYU6=
SW48	MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MnT3NVAxKM7:TR?=	MWC0PEBp	MmDrSG1UVw>?	MY\Qc5RmdnSrYYTld{BUVi1\|ODDjfZRwfG:6aXPpeJk>	MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV5N{m0NUc,OjR3N{e5OFE9N2F-
LoVo	M1facmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MWixNFAh\|ryP	NVToc2liPDhiaB?=	NHjMVmxFVVOR	MoC5VI91\W62aXH0[ZMhW05vM{igZ5l1d3SxeHnjbZR6	MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV5N{m0NUc,OjR3N{e5OFE9N2F-
HT29	MnjzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NYX2SoZCOTByIN88US=>	MYq0PEBp	MoW0SG1UVw>?	M1\rNnBwfGWwdHnheIV{KFOQLUO4JIN6fG:2b4jpZ4l1gQ>?	MlmxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3N{e5OFEoRjJ2NUe3PVQyRC:jPh?=
SW1116	M3q4Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M{LofFExOCEQvF2=	M1rJcFQ5KGh?	NWPjTFBSTE2VTx?=	MlnEVI91\W62aXH0[ZMhW05vM{igZ5l1d3SxeHnjbZR6	NH;NXIs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW3O\|k1OSd-MkS1O\|c6PDF:L3G+
HCT116	Mn3US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NY\j[mZ6OTByIN88US=>	MVi0PEBp	MVHEUXNQ	NWDld4pvWG:2ZX70bYF1\XNiU16tN\|gh[3m2b4TvfIlkcXS7	M1PnU\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NUe3PVQyLz5{NEW3O\|k1OTxxYU6=
RKO	MmTVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M2\wOVExOCEQvF2=	MXi0PEBp	NH;ndI1FVVOR	NVfzVZJqUUN3ME21Mlkh\|ryP	M3q3eFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NUe3PVQyLz5{NEW3O\|k1OTxxYU6=
C-1	NV7RXZNST3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MoXRNVAxKM7:TR?=	NWXtS\|BHPDhiaB?=	M{PXfGROW09?	MXrJR\|UxRTdwNjFOwG0>	NF73eFI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW3O\|k1OSd-MkS1O\|c6PDF:L3G+
SW48	NH\TfVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NEftfHAyODBizszN	NFHFeoo1QCCq	MlXNSG1UVw>?	NHPrVnVKSzVyPUmuOUDPxE1?	NYHBdZRHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1O\|c6PDFpPkK0OVc4QTRzPD;hQi=>
HCT-15	MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MXGxNFAh\|ryP	NGT3TII1QCCq	M4PLcGROW09?	NF[4e45KSzVyPUGwJO69VQ>?	MlGzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3N{e5OFEoRjJ2NUe3PVQyRC:jPh?=
LoVo	NEjDWnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M4PJUlExOCEQvF2=	NIjrTmc1QCCq	NUjy[nZRTE2VTx?=	M2i3fGlEPTB;MUOuOEDPxE1?	M1;YN\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NUe3PVQyLz5{NEW3O\|k1OTxxYU6=
HT29	NXryTndPT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MVyxNFAh\|ryP	NITUblM1QCCq	NF;5cW1FVVOR	MnXZTWM2OD1zND63JO69VQ>?	Mn7NQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3N{e5OFEoRjJ2NUe3PVQyRC:jPh?=
SW1116	MmTjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M4jQbFExOCEQvF2=	MofrOFghcA>?	Mn7MSG1UVw>?	NUH2WJpDUUN3ME2xNFAh\|ryP	NFrDZ\|I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW3O\|k1OSd-MkS1O\|c6PDF:L3G+
HCT116	M1TBSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NV\ObJh7OTByIN88US=>	MoHMOFghcA>?	M3PUSGROW09?	NETE[GFKSzVyPUKuOUDPxE1?	MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV5N{m0NUc,OjR3N{e5OFE9N2F-
T47D	M2ryfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		M3T2ZlUh\GG7		NGHMRWhKSzVyPUmuOkDPxE1?	MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd4MES5Okc,OjN5NkC0PVY9N2F-
MCF7	Mn\JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NX;m[nZQPSCmYYm=		NXPq[4N1UUN3ME21Mlgh\|ryP	M2jSbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|N{[wOFk3Lz5{M{e2NFQ6PjxxYU6=
CAMA1	MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		M{P4UVUh\GG7		MUDJR\|UxRTF3Lkig{txO	Mn73QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5NkC0PVYoRjJ\|N{[wOFk3RC:jPh?=
SUM159	Mo\jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MkW4OUBl[Xl?		MmjGTWM2OD12LkKg{txO	NU[yT\|JWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3OlA1QTZpPkKzO\|YxPDl4PD;hQi=>
SKBR3	MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NUW0TYQ2PSCmYYm=		NXHLWotDUUN3ME2xNU4yKM7:TR?=	Ml;jQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5NkC0PVYoRjJ\|N{[wOFk3RC:jPh?=
JIMT1	MlPmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MUm1JIRigQ>?		M3jkR2lEPTB;Nz63JO69VQ>?	M37EUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|N{[wOFk3Lz5{M{e2NFQ6PjxxYU6=
BT474	M3Xi[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MXm1JIRigQ>?		NYTKR2Q{UUN3ME2xPU45KM7:TR?=	NG[0OoI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{e2NFQ6Pid-MkO3OlA1QTZ:L3G+
Hs578t(si)	M1OyWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NWnuPGw4PSCmYYm=		M4K1OWlEPTB;Nz61JO69VQ>?	MoXkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5NkC0PVYoRjJ\|N{[wOFk3RC:jPh?=
Hs578t	NEXNdZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MnzTOUBl[Xl?		M2XjPGlEPTB;NT62JO69VQ>?	MlLSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5NkC0PVYoRjJ\|N{[wOFk3RC:jPh?=
HCC1937	NYjpXmdsT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MmrHOUBl[Xl?		NF7oNGZKSzVyPUGyMlYh\|ryP	NHvaWIg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{e2NFQ6Pid-MkO3OlA1QTZ:L3G+
HCC1143	NV;VWmF5T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NGXVVY02KGSjeR?=		MlryTWM2OD1zMT6xJO69VQ>?	M{i2OlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|N{[wOFk3Lz5{M{e2NFQ6PjxxYU6=
BT20	NIC4RoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NWPqR5k4PSCmYYm=		MVvJR\|UxRTdwNzFOwG0>	MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd4MES5Okc,OjN5NkC0PVY9N2F-
MDA-MB-468	NYPDN5JRT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NVTsOWtuPSCmYYm=		NETUd41KSzVyPUWuNEDPxE1?	MmryQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5NkC0PVYoRjJ\|N{[wOFk3RC:jPh?=
MDA-MB-231	NV70RZViT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NGDuZ3c2KGSjeR?=		M4\CcWlEPTB;Nj65JO69VQ>?	MmnvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5NkC0PVYoRjJ\|N{[wOFk3RC:jPh?=
PC-9PTEN−	MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	Mm\nNlAh\|ryP	MWSxOFQhcA>?		NYrhNWVFUUN3ME22MlUzKM7:TR?=	MmH6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN{M{m4NFkoRjJ\|MkO5PFA6RC:jPh?=
PC-9	Mn:3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M3yzWVIxKM7:TR?=	NGLzcWsyPDRiaB?=		MVzJR\|UxRTVwOEig{txO	M4LWcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|MkO5PFA6Lz5{M{KzPVgxQTxxYU6=
H1650PTEN+	NVXFRYFlT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MmDVNlAh\|ryP	M4LSV\|E1PCCq		NYjncWMxUUN3ME21NE45OyEQvF2=	NYTzcW5RRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOyN\|k5ODlpPkKzNlM6QDB7PD;hQi=>
H1650	MmfuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MmrnNlAh\|ryP	NFvSSIYyPDRiaB?=		MlrOTWM2OD1zNT60O{DPxE1?	NYnTc2t[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOyN\|k5ODlpPkKzNlM6QDB7PD;hQi=>
Mouse ATM−/− ES Cells	MV3DfZRwfG:6aXOgRZN{[Xl?	M4PWPFIvPSEQvF2=	MlvaNlAhcA>?		MYXTbYdvcW[rY3HueIx6KGmwaHnibZR{KGOnbHygd5Vzfmm4YXy=	NInSbpg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O1OVQ5QSd-MkOzOVU1QDl:L3G+
Mouse H2AX−/− ES Cells	NH;pXolEgXSxdH;4bYMhSXO\|YYm=	NYT5NGdTOi53IN88US=>	NIfIbWgzOCCq		MVvTbYdvcW[rY3HueIx6KGmwaHnibZR{KGOnbHygd5Vzfmm4YXy=	MkW3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN\|NUW0PFkoRjJ\|M{W1OFg6RC:jPh?=
VCaP	MknGTY53[XOrdnWgRZN{[Xl?	MW[yOUDPxE1?	NIDkOGo1QCCq	NWXHN4VbTE2VTx?=	M{XhOXNq\26rZnnjZY51dHlicnXkeYNmeyCHUlet[JJqfmWwIHPlcIwhcW64YYPpc44>	MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTV5NUi2OUc,OjF3N{W4OlU9N2F-
RWPE	NX;nUWN7UW64YYPpeoUhSXO\|YYm=	NEDrNVQzPSEQvF2=	NGWzeVU1QCCq	M{K4UmROW09?	M{iwTnNq\26rZnnjZY51dHlicnXkeYNmeyCHUlet[JJqfmWwIHPlcIwhcW64YYPpc44>	M4XjOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNUe1PFY2Lz5{MUW3OVg3PTxxYU6=
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BB30-HNC	NYjnN\|hyT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				MkfsTWM2OD12OD6zNFczKM7:TR?=	NH;nZlE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2OjF4OE[vK\|5USU6JRWK8M4E,
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MEG-01	MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				MVHJR\|UxRTR7Lke0NVEh\|ryP	NW\scngzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTJzNki2M{c,W0GQR1XSQE9iRg>?
WM-115	MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				M1LHeGlEPTB;NEmuPVIzOiEQvF2=	MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1NlE3QDZxJ{7TRW5ITVJ:L3G+

Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID

Western Blot	DR5/CHOP ; γH2AX/H2AX ; pATM ; 53BP1 ; NF-kB ; pS6/S6	25531448 22933245 27686740 24831086
Immunofluorescence	DNA damage ; γH2AX	27686740 28069876
Growth inhibition assay	Cell viability	25531448
ELISA	IL-8 ; GLP-1	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 (from reference)

Kinase Assay: ^[1]	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]	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]	Animal Models: Brca1^-/-;p53^-/- mammary tumors are generated in K14cre;Brca1^F/F;p53^F/F mice. Dosages: 50 mg/kg Administration: Administered via i.p. injection at 10 μL/g of body weight (Only for Reference)

References

[4] Weston VJ, et al, Blood, 2010, 116(22), 4578-4587.

+ Expand

Solubility (25°C)

In vitro	DMSO	86 mg/mL (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. Click to purchase: PEG300	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	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	C1CC1C(=O)N2CCN(CC2)C(=O)C3=C(C=CC(=C3)CC4=NNC(=O)C5=CC=CC=C54)F

Download Olaparib (AZD2281) SDF

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Dilution Calculator Molecular Weight Calculator

Clinical Trial Information

NCT Number	Recruitment	Interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05153603	Not yet recruiting	Drug: Olaparib mono-maintenance therapy	Ovarian Neoplasms	Sun Yat-Sen Memorial Hospital of Sun Yat-Sen University	April 2022	--
NCT05128734	Not yet recruiting	Drug: Temozolomide\|Drug: Olaparib	Breast Cancer Triple Negative	AHS Cancer Control Alberta	April 1 2022	Phase 2
NCT04644289	Not yet recruiting	Drug: olaparib\|Drug: durvalumab	Epithelial Ovarian Cancer	AGO Research GmbH	January 2022	Phase 2
NCT05078671	Not yet recruiting	Drug: Olaparib\|Drug: Cobicistat	Cancer	Radboud University	October 15 2021	Phase 4

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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

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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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