Olaparib (AZD2281)

For research use only. Not for use in humans.

目录号:S1060 别名: Ku-0059436

Olaparib (AZD2281) Chemical Structure

Molecular Weight(MW): 434.46

Olaparib (AZD2281, KU0059436)是选择性的PARP1/2抑制剂,IC50为5 nM/1 nM,其对PARP1/2的作用比对Tankyrase-1效果高300倍。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 745.41 现货
RMB 571.54 现货
RMB 1219.52 现货
RMB 3019.32 现货
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客户使用Selleck生产的Olaparib (AZD2281)发表文献453篇:

产品安全说明书

PARP抑制剂选择性比较

生物活性

产品描述 Olaparib (AZD2281, KU0059436)是选择性的PARP1/2抑制剂,IC50为5 nM/1 nM,其对PARP1/2的作用比对Tankyrase-1效果高300倍。
特性 Olaparib是第一批PARP抑制剂之一。
靶点
PARP2 [1]
(Cell-free assay)
PARP1 [1]
(Cell-free assay)
1 nM 5 nM
体外研究

Olaparib是PARP抑制剂,也作用于BRCA1或BRCA2突变。Olaparib对端锚(聚合)酶-1作用效果不大,IC50值大于。Olaparib浓度为30-100 nM作用于SW620细胞,使PARP-1失活。与BRCA1和BRCA2充足细胞系(Hs578T,MDA-MB-231,T47D)相比,BRCA1缺陷细胞系(MDA-MB-463和HCC1937)对Olaparib过分敏感[1] Olaparib抑制PARP,阻断碱基切除修复,导致KB2P细胞对Olaparib强烈敏感。结果导致在DNA复制时由单链断裂转变为双链断裂,由此激活BRCA2依赖的重组途径。[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
KP3.33 NYHZVIM2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYO0JIQ> NWTIfY51UUN3ME21MlcxPSBizszNJC=> MnTnNVg2PTl4MUO=
KP6.3 NF7kR2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfNOEBl MV\JR|UxRTFyLkSyPEDPxE1i NWf4TZdQOTh3NUm2NVM>
KP7.7 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHUW4lzPCCm M2LOUWlEPTB;NUegcm0h NV\V[Wp1OTh3NUm2NVM>
KB2P3.4 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LzPVQh\A>? MWPJR|UxRTF{NDDNJC=> MmDZNVg2PTl4MUO=
KB2P1.21 NGGzXmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVS0JIQ> M1L1T2lEPTB;OEmwO{BvVSB? NHzYblIyQDV3OU[xNy=>
U373-MG M3\DUmN6fG:2b4jpZ{BCe3OjeR?= NHPBZYgyKM7:TTC= M4XrTlI1KGh? M3vqUGlv[3KnYYPld{Bz[WSrYYTpc44he2Wwc3n0bZZqfHl? M3r5R|E5QTV2N{Gy
T98G M3[zfWN6fG:2b4jpZ{BCe3OjeR?= NVLXXWI6OSEQvF2g NXTSVHZ[OjRiaB?= NFzIcIdKdmO{ZXHz[ZMhemGmaXH0bY9vKHOnboPpeIl3cXS7 NXy0V|ZLOTh7NUS3NVI>
U87-MG NGGwdZhEgXSxdH;4bYMhSXO|YYm= M1v3NlEh|ryPIB?= M17VbFI1KGh? NIP0eoRKdmO{ZXHz[ZMhemGmaXH0bY9vKHOnboPpeIl3cXS7 M173Z|E5QTV2N{Gy
UVW NWnydo5YS3m2b4TvfIlkKEG|c3H5 NEPJOlU2ODBibl2= M2mzelI1KGh? NVjNOGxSUW6lcnXhd4V{KHKjZHnheIlwdiC|ZX7zbZRqfmm2eR?= NGnSTHkyQDl3NEexNi=>
HeLa NU[5SY9zTnWwY4Tpc44hSXO|YYm= MWO1NFAhdk1? NEPpeJQ1KGh? NHWyNllE[XW|ZYOgZUBud2Snc4Sg[IVt[XliaX6gdoVrd2mwaX7nJI9nKHKjZHnheIlwdi2rbnT1Z4VlKESQQTDidoVic3N? MlXXNVg6PTR5MUK=
HeLa NHvKUIxHfW6ldHnvckBCe3OjeR?= MoXwNUDPxE1i NWT3NVZ3OjRiaB?= NGTLN4NGdmijbnPld{Bz[WSrYYTpc44ucW6mdXPl[EBUNXCqYYPlJIFzemW|dB?= NVT1eIoyOTh7NUS3NVI>
T98G NInWRotHfW6ldHnvckBCe3OjeR?= MX:xJO69VSB? NFT4SXgzPCCq MU\FcohidmOnczDyZYRq[XSrb36tbY5lfWOnZDDTMZBp[XOnIHHydoV{fA>? Ml22NVg6PTR5MUK=
L3 NHzZfpZEgXSxdH;4bYMhSXO|YYm= MoPpOUDPxE1i MVi5OkBp NILmSYxFVVOR NU\KT3JGW2mpbnnmbYNidnSueTDpcohq[mm2czDj[YxtKHO3co\peoFt MlTINlAyOjR2NUm=
Granta-519 NUCzcnVjS3m2b4TvfIlkKEG|c3H5 NWnvRmpuPSEQvF2g NFT6T4s6PiCq NGnne5JFVVOR NXPVfWNFW2yrZ3j0cJkhcW6qaXLpeJMh[2WubDDzeZJ3cX[jbB?= MV6yNFEzPDR3OR?=
BT NGPacnVEgXSxdH;4bYMhSXO|YYm= MVu1JO69VSB? M4PwUFk3KGh? M3XwfmROW09? Mk\3V4xq\2i2bImgbY5pcWKrdIOgZ4VtdCC|dYL2bZZidA>? NFSzOYgzODF{NES1PS=>
UPN2 NX;lOndnS3m2b4TvfIlkKEG|c3H5 M3LMbVUh|ryPIB?= M4nie|k3KGh? M1jpTWROW09? M2XPTXNtcWeqdHz5JIlvcGmkaYTzJINmdGxic4Xyeol3[Wx? MVOyNFEzPDR3OR?=
HBL-2 M1uwVWN6fG:2b4jpZ{BCe3OjeR?= M3nzXVUh|ryPIB?= NVrtfZV5QTZiaB?= NHvKdmpFVVOR M2fDWnNtcWeqdHz5JIlvcGmkaYTzJINmdGxic4Xyeol3[Wx? NFj0TGczODF{NES1PS=>
JVM-2 MlvzR5l1d3SxeHnjJGF{e2G7 NUPEfVlrPSEQvF2g NGfDUYQ6PiCq MkXYSG1UVw>? MYLTcIlocHSueTDpcohq[mm2czDj[YxtKHO3co\peoFt NF:4[5UzODF{NES1PS=>
Z138 NY\JXo5ZS3m2b4TvfIlkKEG|c3H5 NH73S3U2KM7:TTC= NFfoflg6PiCq NFnReotFVVOR M3\Yc3NtcWeqdHz5JIlvcGmkaYTzJINmdGxic4Xyeol3[Wx? M3XRdVIxOTJ2NEW5
RWPE M3K3XmlvfmG|aY\lJGF{e2G7 M4jlclI2KM7:TR?= NFrwS3E1QCCq MYPEUXNQ MnLpV4lodmmoaXPhcpRtgSC{ZXT1Z4V{KEWURz3kdol3\W5iY3XscEBqdn[jc3nvci=> NFzBXoszOTV5NUi2OS=>
VCaP MYrJcpZie2m4ZTDBd5NigQ>? MVmyOUDPxE1? NYXBclhnPDhiaB?= MULEUXNQ MnTNV4lodmmoaXPhcpRtgSC{ZXT1Z4V{KEWURz3kdol3\W5iY3XscEBqdn[jc3nvci=> NX\MN5JVOjF3N{W4OlU>
Mouse H2AX−/− ES Cells NXXLTIlNS3m2b4TvfIlkKEG|c3H5 NEDtNpYzNjVizszN NYDFd3Z5OjBiaB?= NFLD[3ZUcWewaX\pZ4FvfGy7IHnubIljcXS|IHPlcIwhe3W{dnn2ZYw> Ml3HNlM{PTV2OEm=
Mouse ATM−/− ES Cells Mo\MR5l1d3SxeHnjJGF{e2G7 NHTJWW8zNjVizszN NXPB[VVDOjBiaB?= MnT0V4lodmmoaXPhcpRtgSCrbnjpZol1eyClZXzsJJN2en[rdnHs MX[yN|M2PTR6OR?=
H1650 NWiwRnYxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHaSmJxOjBizszN NVrKcWZkOTR2IHi= MkHRTWM2OD1zNT60O{DPxE1? MWWyN|I{QThyOR?=
H1650PTEN+ M4r6TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDh[JYzOCEQvF2= MYGxOFQhcA>? NHPXfJdKSzVyPUWwMlg{KM7:TR?= NYnCZWRbOjN{M{m4NFk>
PC-9 NV;LXYoxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3S3[lIxKM7:TR?= NEHoN2EyPDRiaB?= NEPKT4JKSzVyPUWuPFgh|ryP NHLER5YzOzJ|OUiwPS=>
PC-9PTEN− NYHWOmRET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU[yNEDPxE1? M2fxR|E1PCCq M3:zVmlEPTB;Nj61NkDPxE1? NYDjNpVkOjN{M{m4NFk>
MDA-MB-231 NFnxUmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{LWOVUh\GG7 M37zUWlEPTB;Nj65JO69VQ>? MlPJNlM4PjB2OU[=
MDA-MB-468 MlX0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVi1JIRigQ>? NUO4b5BTUUN3ME21MlAh|ryP NIWycowzOzd4MES5Oi=>
BT20 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUe1JIRigQ>? MXfJR|UxRTdwNzFOwG0> NUL3U2NDOjN5NkC0PVY>
HCC1143 M4PjcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fZXlUh\GG7 MkCyTWM2OD1zMT6xJO69VQ>? NX62W2NGOjN5NkC0PVY>
HCC1937 M2DmZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M323WFUh\GG7 NVPUeXQ6UUN3ME2xNk43KM7:TR?= NF3EUYozOzd4MES5Oi=>
Hs578t MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2TES|Uh\GG7 M{T3W2lEPTB;NT62JO69VQ>? MVGyN|c3ODR7Nh?=
Hs578t(si) M3q4Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3:4VVUh\GG7 MVzJR|UxRTdwNTFOwG0> NEPLWYszOzd4MES5Oi=>
BT474 M4\YWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fZeVUh\GG7 MVjJR|UxRTF7Lkig{txO NX7PVGtVOjN5NkC0PVY>
JIMT1 NVK0WJA2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zJd|Uh\GG7 MmX3TWM2OD15Lkeg{txO M3zxTVI{PzZyNEm2
SKBR3 NH\SW|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkHsOUBl[Xl? M{njUmlEPTB;MUGuNUDPxE1? NGHKNmYzOzd4MES5Oi=>
SUM159 M3jDemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TmfVUh\GG7 NGfvSZlKSzVyPUSuNkDPxE1? NHXoeHYzOzd4MES5Oi=>
CAMA1 NGjU[5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;Yc2g2KGSjeR?= MYrJR|UxRTF3Lkig{txO Mk\HNlM4PjB2OU[=
MCF7 NULvVnJJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfxOUBl[Xl? NG\CRZFKSzVyPUWuPEDPxE1? MV:yN|c3ODR7Nh?=
T47D MoG1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX[1JIRigQ>? MVvJR|UxRTlwNjFOwG0> MY[yN|c3ODR7Nh?=
HCT116 M{\rUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPYNVAxKM7:TR?= NW[wU|NUPDhiaB?= MVXEUXNQ M2DnbWlEPTB;Mj61JO69VSB? MonoNlQ2Pzd7NEG=
SW1116 M17YXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1PvR|ExOCEQvF2= Mn;qOFghcA>? MVXEUXNQ MV\JR|UxRTFyMDFOwG0> NGXaR3kzPDV5N{m0NS=>
HT29 MkjkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\0UVU{OTByIN88US=> Mo\XOFghcA>? NEjvUZpFVVOR NH3IVIRKSzVyPUG0Mlch|ryP MnTnNlQ2Pzd7NEG=
LoVo MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLGW5gyODBizszN Mnz6OFghcA>? M37PZWROW09? NYO3SIs{UUN3ME2xN{41KM7:TR?= Mn;3NlQ2Pzd7NEG=
HCT-15 MnH2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nQTVExOCEQvF2= MUe0PEBp MVjEUXNQ NHO4bYlKSzVyPUGwJO69VQ>? M3jxSFI1PTd5OUSx
SW48 M1rM[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NES1PJYyODBizszN NVmxPFFZPDhiaB?= M1H0ZWROW09? NWHNdnltUUN3ME25MlUh|ryP MUmyOFU4Pzl2MR?=
C-1 NFvzUWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknRNVAxKM7:TR?= NXjXUlFPPDhiaB?= NHjlcWdFVVOR M{f6dGlEPTB;Nz62JO69VQ>? NXzRbIRROjR3N{e5OFE>
RKO MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnvONVAxKM7:TR?= MmPyOFghcA>? NUmx[Vd4TE2VTx?= MXzJR|UxRTVwOTFOwG0> NHLOWZkzPDV5N{m0NS=>
HCT116 NXj5PVJbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4j6c|ExOCEQvF2= NXvkeJR[PDhiaB?= M1HvPWROW09? MVfQc5RmdnSrYYTld{BUVi1|ODDjfZRwfG:6aXPpeJkh NXPIWZN[OjR3N{e5OFE>
SW1116 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHXSNJYyODBizszN MmWwOFghcA>? NE\IXIJFVVOR NHnqbYhRd3SnboTpZZRmeyCVTj2zPEBkgXSxdH;4bYNqfHli NFG2fJQzPDV5N{m0NS=>
HT29 M37odmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vFVVExOCEQvF2= NVjsfpFtPDhiaB?= NWLGRW1ITE2VTx?= M{L0[HBwfGWwdHnheIV{KFOQLUO4JIN6fG:2b4jpZ4l1gSB? MoK4NlQ2Pzd7NEG=
LoVo M1GzN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWL5Zod5OTByIN88US=> NFjZTVY1QCCq M2PXSmROW09? NXy2bmd5WG:2ZX70bYF1\XNiU16tN|gh[3m2b4TvfIlkcXS7IB?= NFjrdoMzPDV5N{m0NS=>
SW48 NWPlOlFNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfIUJhtOTByIN88US=> M4P3PVQ5KGh? NX60WpI2TE2VTx?= NXu4dmVOWG:2ZX70bYF1\XNiU16tN|gh[3m2b4TvfIlkcXS7IB?= MkDNNlQ2Pzd7NEG=
C-1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXMd4YyODBizszN M3TlW|Q5KGh? NWHG[GZvTE2VTx?= MV7Qc5RmdnSrYYTld{BUVi1|ODDjfZRwfG:6aXPpeJkh MXqyOFU4Pzl2MR?=
RKO NUTNU4VDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYWxNFAh|ryP MYC0PEBp MXnEUXNQ M2fCRnBwfGWwdHnheIV{KFOQLUO4JIN6fG:2b4jpZ4l1gSB? MV:yOFU4Pzl2MR?=
HCT116 NYjON3lYTnWwY4Tpc44hSXO|YYm= M1vxOVExKG6P M1[4e|EzKGh? MX\EUXNQ NIjpWW1KdmO{ZXHz[ZMhTE6DIHTveYJt\S2|dILhcoQh[nKnYXvzJIlv\HWlZXSgZpkhW05vM{i= NHjQeoczPDV5N{m0NS=>
HT29 NX;UUZlSTnWwY4Tpc44hSXO|YYm= M{jhZ|ExKG6P Mor1NVIhcA>? NXLWbnBETE2VTx?= M1LnSmlv[3KnYYPld{BFVkFiZH;1ZoxmNXO2cnHu[EBjemWja4OgbY5lfWOnZDDifUBUVi1|OB?= M37sVFI1PTd5OUSx
TE-6 M2nJXWZ2dmO2aX;uJGF{e2G7 M1rLWFUh|ryPIB?= NWPSOVFjOTJiaB?= NWDlelF5TE2VTx?= M3nBcmlv\HWlZYOgS|IwVSCjcoLld5Q> MViyOFIyQTF4NB?=
TE-6 NEn4[JJHfW6ldHnvckBCe3OjeR?= MXS1JO69VSB? NVT2fXBUOjRiaB?= MUjEUXNQ M2ewTmlv[3KnYYPld{BqdiCmb4XicIUhe3S{YX7kJIJz\WGtczCoSHNDeyl? NVvqXG5SOjR{MUmxOlQ>
Hep3B NVPHRXFjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVW0NEDPxE1i NYrzPGdTPzJiaB?= MkfMSG1UVw>? M2DBW3N6dmW{Z3nzeIlk[WyueTDpcohq[mm2czDj[YxtKGe{b4f0bEB4cXSqIFTIUWVS NUXMRXZMOjVyN{K3OVI>
Huh7 MofCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTZOFAh|ryPIB?= MoP3O|IhcA>? NWDqOlBiTE2VTx?= NXHKfGZlW3mwZYLnbZN1cWOjbHz5JIlvcGmkaYTzJINmdGxiZ4Lve5RpKHerdHigSGhOTVF? MUCyOVA4Ojd3Mh?=
Hep3B M3T3[GZ2dmO2aX;uJGF{e2G7 MWe0NEDPxE1i NIHB[XgzPCCq NHfsTmpFVVOR MkXyTY5lfWOnczDSU3MheHKxZIXjeIlwdiC5aYToJGRJVUWT NIXLTFczPTB5Mke1Ni=>
Huh7 NEXUTYdHfW6ldHnvckBCe3OjeR?= M37JXVQxKM7:TTC= NU\lPYNqOjRiaB?= M1n1PWROW09? NHLhfXVKdmS3Y3XzJHJQWyCycn;keYN1cW:wIIfpeIghTEiPRWG= NFKyXHozPTB5Mke1Ni=>
Hep3B NGfZcmpHfW6ldHnvckBCe3OjeR?= MX[0NEDPxE1i NHnzU|QzPCCq NIHOeGtFVVOR NXLE[|RkUW6mdXPld{Bk\WyuIHH1eI9xcGGpeTD3bZRpKESKTVXR M{nvblI2ODd{N{Wy
Huh7 NV72UIxbTnWwY4Tpc44hSXO|YYm= NIKzbnI1OCEQvF2g Ml2xNlQhcA>? MYHEUXNQ Ml[wTY5lfWOnczDj[YxtKGG3dH;wbIFogSC5aYToJGRJVUWT M2rLclI2ODd{N{Wy
SGC-7901 MlL2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkOzN|DDqM7:TR?= MWe0PEBp M{TMeGROW09? NHHyZWdDdG:lazDvfIFtcXCuYYTpck1qdmS3Y3XkJINmdGxiZHXheIg> M{W2b|I2PzZ5MEe2
COLO-800 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DRbGlEPTB;MD60OFE3PCEQvF2= MU\TRW5ITVJ?
EoL-1- MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mof1TWM2OD1yLkW2OFQ3KM7:TR?= NV7qXJh1W0GQR1XS
NCI-H209 Mn7jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnOSIdnUUN3ME2wMlkyPTV4IN88US=> NYLadVBVW0GQR1XS
ES1 NUT0W2FZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4Xy[2lEPTB;MT6xNVQxQCEQvF2= M4G0PXNCVkeHUh?=
NKM-1 NIm3XWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXDZWlsUUN3ME2xMlI2OzR5IN88US=> NEHx[m5USU6JRWK=
NTERA-S-cl-D1 NY\JcodOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFrxU3BKSzVyPUGuN|M{PDFizszN NV;PcJl4W0GQR1XS
MHH-ES-1 M{XzZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XiTGlEPTB;MT62NlA3PyEQvF2= NYPpN4xNW0GQR1XS
ES8 Mny2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{P3cGlEPTB;MT63NlQyPCEQvF2= NYTafWdUW0GQR1XS
NCI-H720 M2LYWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTJwMkC2PVkh|ryP NUXZeHVGW0GQR1XS
EW-3 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|UxRTJwMke1N|Qh|ryP NFm2[VVUSU6JRWK=
D-566MG NEPsUI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TVTGlEPTB;Mj60OFU3QCEQvF2= NWL6WFZqW0GQR1XS
697 Mn;RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7aZpZjUUN3ME2yMlg1OTd|IN88US=> NEXabFRUSU6JRWK=
ES5 M2Dqemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTJwOEixPFkh|ryP M{TOWnNCVkeHUh?=
COLO-684 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmq2TWM2OD1|LkWxOlk3KM7:TR?= MULTRW5ITVJ?
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BALL-1 NHPHVGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTN7LkKxNlkh|ryP MX;TRW5ITVJ?
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GI-1 MmK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV35ephCUUN3ME2zPU45PjR5IN88US=> MWrTRW5ITVJ?
GOTO MofYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3zCXWlEPTB;M{muPVE{QSEQvF2= M3\V[nNCVkeHUh?=
A673 NIPjd3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7qTWM2OD12MT6wN|Q{KM7:TR?= MYXTRW5ITVJ?
KG-1 MlPXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTR|LkO5OEDPxE1? MXPTRW5ITVJ?
GP5d NXjYOHlST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vlXmlEPTB;NESuNFY3PiEQvF2= MkXKV2FPT0WU
MFM-223 NVzqV2JLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmK3TWM2OD12ND6xNlI5KM7:TR?= NHn4ZY9USU6JRWK=
OAW-42 NFraVXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmDUTWM2OD12ND6yOlQ{KM7:TR?= M4rxN3NCVkeHUh?=
C8166 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlzNTWM2OD12NT6wPFIzKM7:TR?= NITZW4VUSU6JRWK=
LU-99A MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\0cWlEPTB;NE[uNVMzOiEQvF2= NInmbmlUSU6JRWK=
NCI-H23 NYnL[Xo1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlvjTWM2OD12Nj6xO|g2KM7:TR?= NUnBSmRUW0GQR1XS
HO-1-N-1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTR5LkC5PVgh|ryP MoPnV2FPT0WU
A3-KAW NVLsN3lXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPIOJRQUUN3ME20O{4yODB5IN88US=> M4\tfHNCVkeHUh?=
CGTH-W-1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\pTWM2OD12Nz61NFY6KM7:TR?= NVz3bo9CW0GQR1XS
DJM-1 MlO1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTR5LkW0NVMh|ryP MUjTRW5ITVJ?
A101D MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfmSXFKSzVyPUS3MlY{PTdizszN NVrkUFY1W0GQR1XS
BB30-HNC NFzUN4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfiSpM2UUN3ME20PE4{ODd{IN88US=> NYrLe4NJW0GQR1XS
T98G M2G0Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjTTWM2OD12OD60OlM{KM7:TR?= MnnYV2FPT0WU
NCI-H1573 NV;UPFdtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXQSmZEUUN3ME20PU41PDZ{IN88US=> NX7jOo5NW0GQR1XS
MEG-01 M13aXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjGTWM2OD12OT63OFEyKM7:TR?= MYrTRW5ITVJ?
WM-115 NVrH[YNXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUC0dnF[UUN3ME20PU46OjJ{IN88US=> M1v2fXNCVkeHUh?=

... 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
体内研究 Olaparib有效作用于Brca1-/-;p53-/- 乳腺肿瘤 (每天按50 mg/kg剂量腹腔注射),但是对 HR缺陷的Ecad-/-;p53-/-乳腺肿瘤没有效果。Olaparib作用于携带肿瘤的鼠没有剂量限制毒性。[3] Olaparib已经用于治疗BRCA突变的肿瘤, 比如卵巢癌,胸腺癌,前列腺癌。此外,Olaparib抑制ATM缺陷的肿瘤细胞具有选择性,说明Olaparib可作为治疗ATM突变的淋巴肿瘤的潜在试剂。[4]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:

[1]

- 合并

体外独立酶实验:

通过PARP-1实验测定PARP-2抑制活性,实验在96孔板上进行,PARP-2特定抗体与重组PARP-2蛋白结合。加入3H-NAD+DNA测定PARP-2活性。 冲洗后,加入闪烁剂测定3H-渗透的核糖基化。通过AlphaScreen实验测定端锚聚合酶-1, 实验中HIS标签重组TANK-1蛋白和生物素化的NAD+ 在384孔Proxi板上温育。 加入Alpha 磁珠,与HIS和生物素化的标签结合,产生邻近信号,测定信号消失的比例来计算TANK-1抑制活性。
细胞实验:

[1]

- 合并
  • Cell lines: 胸腺癌细胞系SW620结肠, A2780卵巢,HCC1937,Hs578T,MDA-MB-231,MDA-MB-436,和T47D
  • Concentrations: 1到300 nM
  • Incubation Time: 7-14天
  • Method:

    通过成株实验测定Olaparib毒性。Olaparib溶于DMSO中,用培养基稀释。细胞接种在六孔板上,过夜使粘附。然后加入不同浓度Olaparib,温育7-14天。计算存活菌落,测定IC50值。


    (Only for Reference)
动物实验:

[3]

- 合并
  • Animal Models: 携带Brca1-/-;p53-/-乳腺癌的 K14cre;Brca1F/F;p53F/F
  • Formulation: 50 mg/mL储存在含10% 2-羟丙基-β-环糊精/PBS的DMSO中
  • Dosages: 50 mg/kg
  • Administration: 按10 μL/g剂量腹腔注射
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 86 mg/mL warmed (197.94 mM)
Water 0.002 mg/mL (0.0 mM)
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
4% DMSO+30% PEG 300+ddH2O
5mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 434.46
化学式

C24H23FN4O3

CAS号 763113-22-0
储存条件 粉状
溶于溶剂
别名 Ku-0059436

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

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

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1:

    How to prepare the solution of the compound (S1060) for in vivo study?

  • 回答:

    We recommend the following formulation: 4% DMSO+30% PEG300+ 66%H2O. It is a clear solution and can be used for IP injection.

  • 问题 2:

    I saw that the solubility of the compound for in vivo on the website had been changed, why the change has been made?

  • 回答:

    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.

  • 问题 3:

    How long can the chemical compound be stable in DMEM at 4 °C?

  • 回答:

    The compound is stable in DMEM at 4 degree for one week.

PARP Signaling Pathway Map

PARP Inhibitors with Unique Features

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