Olaparib (AZD2281)

目录号:S1060 别名: Ku-0059436 中文名称:奥拉帕尼

仅限科研使用

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。在BRCA突变的细胞中,Olaparib可以显著地诱导线粒体自噬相关的细胞自噬。

Olaparib (AZD2281) Chemical Structure

CAS: 763113-22-0

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 745.41 现货
RMB 794.43 现货
RMB 1219.52 现货
RMB 3019.32 现货
大包装 有超大折扣

今日订购,明日送达 全国免运费 分装免费 分装成小规格产品(单支最小为1mg)
如1支10mg产品可分装为10支1mg产品

全国免费电话:400-668-6834   |   Email:info@selleck.cn

客户使用Selleck生产的Olaparib (AZD2281)发表文献878篇:

产品安全说明书

PARP抑制剂选择性比较

相关PARP产品

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。在BRCA突变的细胞中,Olaparib可以显著地诱导线粒体自噬相关的细胞自噬。
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
Hep3B MVTGeY5kfGmxbjDBd5NigQ>? NE\u[mk1OCEQvF2= M{nwbVI1KGh? NVzaXJdrTE2VTx?= M1PNbWlv\HWlZYOgVm9UKHC{b3T1Z5Rqd25id3n0bEBFUE2HUR?= MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB5Mke1Nkc,OjVyN{K3OVI9N2F-
Huh7 MmPaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV60NEDPxE1? MYO3NkBp NV23bmZtTE2VTx?= M37TfHN6dmW{Z3nzeIlk[WyueTDpcohq[mm2czDj[YxtKGe{b4f0bEB4cXSqIFTIUWVS MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB5Mke1Nkc,OjVyN{K3OVI9N2F-
Hep3B MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTmOFAh|ryP MmryO|IhcA>? Ml\XSG1UVw>? NVfwZohFW3mwZYLnbZN1cWOjbHz5JIlvcGmkaYTzJINmdGxiZ4Lve5RpKHerdHigSGhOTVF? MlfNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyN{K3OVIoRjJ3MEeyO|UzRC:jPh?=
TE-6 MWjGeY5kfGmxbjDBd5NigQ>? NVvCT3NIPSEQvF2= NXjwc3UxOjRiaB?= NWDuTGlqTE2VTx?= NHnQOYhKdmO{ZXHz[ZMhcW5iZH;1ZoxmKHO2cnHu[EBjemWja4OgLGRUSnNr M1LxfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MkG5NVY1Lz5{NEKxPVE3PDxxYU6=
TE-6 NYn4UnpNTnWwY4Tpc44hSXO|YYm= NUjtb4dUPSEQvF2= M335blEzKGh? NV3FVWt4TE2VTx?= MonFTY5lfWOnczDHNk9OKGG{cnXzeC=> NUexemkxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyNVkyPjRpPkK0NlE6OTZ2PD;hQi=>
HT29 NXfzboo4TnWwY4Tpc44hSXO|YYm= NV\Yem4{OTBibl2= M37zcFEzKGh? NHm0OWxFVVOR MkHtTY5kemWjc3XzJGRPSSCmb4XicIUue3S{YX7kJIJz\WGtczDpcoR2[2WmIHL5JHNPNTN6 MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV5N{m0NUc,OjR3N{e5OFE9N2F-
HCT116 M1;QWWZ2dmO2aX;uJGF{e2G7 MYOxNEBvVQ>? MmDDNVIhcA>? M3v1RmROW09? M2HVS2lv[3KnYYPld{BFVkFiZH;1ZoxmNXO2cnHu[EBjemWja4OgbY5lfWOnZDDifUBUVi1|OB?= MkDUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3N{e5OFEoRjJ2NUe3PVQyRC:jPh?=
RKO MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljSNVAxKM7:TR?= M{TCeFQ5KGh? MljqSG1UVw>? Mn3mVI91\W62aXH0[ZMhW05vM{igZ5l1d3SxeHnjbZR6 M4DjN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NUe3PVQyLz5{NEW3O|k1OTxxYU6=
C-1 MlnlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX[xNFAh|ryP NITqXJo1QCCq NXjUNW9NTE2VTx?= M1zTNHBwfGWwdHnheIV{KFOQLUO4JIN6fG:2b4jpZ4l1gQ>? NGf1TIc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW3O|k1OSd-MkS1O|c6PDF:L3G+
SW48 NHPySVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jDcFExOCEQvF2= MmrFOFghcA>? MlruSG1UVw>? M4nUNHBwfGWwdHnheIV{KFOQLUO4JIN6fG:2b4jpZ4l1gQ>? NHPuSnI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW3O|k1OSd-MkS1O|c6PDF:L3G+
LoVo NF\1WZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXixNFAh|ryP MojQOFghcA>? M1fwUmROW09? MUnQc5RmdnSrYYTld{BUVi1|ODDjfZRwfG:6aXPpeJk> MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV5N{m0NUc,OjR3N{e5OFE9N2F-
HT29 NGLCRpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfH[HVYOTByIN88US=> M4TofFQ5KGh? NEDId3lFVVOR MkPIVI91\W62aXH0[ZMhW05vM{igZ5l1d3SxeHnjbZR6 M1rSe|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NUe3PVQyLz5{NEW3O|k1OTxxYU6=
SW1116 M37uT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rOU|ExOCEQvF2= MUO0PEBp Mnv3SG1UVw>? MWDQc5RmdnSrYYTld{BUVi1|ODDjfZRwfG:6aXPpeJk> MonoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3N{e5OFEoRjJ2NUe3PVQyRC:jPh?=
HCT116 M{\ZeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjqSHAyODBizszN NHPzToo1QCCq NWLQeVJKTE2VTx?= MW\Qc5RmdnSrYYTld{BUVi1|ODDjfZRwfG:6aXPpeJk> MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV5N{m0NUc,OjR3N{e5OFE9N2F-
RKO NUj5NJNmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUTpXGJDOTByIN88US=> M2nQdlQ5KGh? NVrnNWwyTE2VTx?= M3;kVmlEPTB;NT65JO69VQ>? MoTkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3N{e5OFEoRjJ2NUe3PVQyRC:jPh?=
C-1 NFHHd5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVzydZlDOTByIN88US=> MljzOFghcA>? NI\m[WlFVVOR MVnJR|UxRTdwNjFOwG0> MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV5N{m0NUc,OjR3N{e5OFE9N2F-
SW48 NH\TSXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXm1Vo5qOTByIN88US=> MX20PEBp NE\xeHZFVVOR NXjiWmEyUUN3ME25MlUh|ryP MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV5N{m0NUc,OjR3N{e5OFE9N2F-
HCT-15 MorBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXSxNFAh|ryP M2DwRVQ5KGh? MXvEUXNQ M2XlPGlEPTB;MUCg{txO M{mwXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NUe3PVQyLz5{NEW3O|k1OTxxYU6=
LoVo MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXixNFAh|ryP NXvQSYxjPDhiaB?= MlXxSG1UVw>? MlfWTWM2OD1zMz60JO69VQ>? NVXqV3M5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1O|c6PDFpPkK0OVc4QTRzPD;hQi=>
HT29 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\0TJEyODBizszN MV60PEBp Mm[xSG1UVw>? M1HyXWlEPTB;MUSuO{DPxE1? M{TFVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NUe3PVQyLz5{NEW3O|k1OTxxYU6=
SW1116 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXPqeVlXOTByIN88US=> MVK0PEBp M2K5T2ROW09? M2nMR2lEPTB;MUCwJO69VQ>? MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV5N{m0NUc,OjR3N{e5OFE9N2F-
HCT116 NHfpNYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\LNVAxKM7:TR?= NGPrVZI1QCCq M13ITGROW09? M3j1N2lEPTB;Mj61JO69VQ>? NHnhWJM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW3O|k1OSd-MkS1O|c6PDF:L3G+
T47D M3uxZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYC1JIRigQ>? MlPuTWM2OD17Lk[g{txO Mn7EQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5NkC0PVYoRjJ|N{[wOFk3RC:jPh?=
MCF7 MoTGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnzXOUBl[Xl? NUXBVmFSUUN3ME21Mlgh|ryP NYPJfFVGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3OlA1QTZpPkKzO|YxPDl4PD;hQi=>
CAMA1 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjVOUBl[Xl? M33ub2lEPTB;MUWuPEDPxE1? MnHWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5NkC0PVYoRjJ|N{[wOFk3RC:jPh?=
SUM159 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYq1JIRigQ>? NFLiT3ZKSzVyPUSuNkDPxE1? MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd4MES5Okc,OjN5NkC0PVY9N2F-
SKBR3 NXfJd5I5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rWWlUh\GG7 NX7pV|BQUUN3ME2xNU4yKM7:TR?= Mn3NQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5NkC0PVYoRjJ|N{[wOFk3RC:jPh?=
JIMT1 M33DXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jvd|Uh\GG7 NIT5R4VKSzVyPUeuO{DPxE1? M3z6fVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{[wOFk3Lz5{M{e2NFQ6PjxxYU6=
BT474 Mn7TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGf5T4Y2KGSjeR?= MlHsTWM2OD1zOT64JO69VQ>? NFKzXXY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{e2NFQ6Pid-MkO3OlA1QTZ:L3G+
Hs578t(si) Mn72S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWO1JIRigQ>? M{DlWGlEPTB;Nz61JO69VQ>? MlzrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5NkC0PVYoRjJ|N{[wOFk3RC:jPh?=
Hs578t M4K2b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HGelUh\GG7 Ml;oTWM2OD13Lk[g{txO NGi5N|U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{e2NFQ6Pid-MkO3OlA1QTZ:L3G+
HCC1937 MlzmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7jOUBl[Xl? MV;JR|UxRTF{Lk[g{txO MnPHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5NkC0PVYoRjJ|N{[wOFk3RC:jPh?=
HCC1143 NFzaPXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWfzVldyPSCmYYm= MUjJR|UxRTFzLkGg{txO MmrxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5NkC0PVYoRjJ|N{[wOFk3RC:jPh?=
BT20 M4LMcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjGOUBl[Xl? MoLzTWM2OD15Lkeg{txO NXLvVXJ6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3OlA1QTZpPkKzO|YxPDl4PD;hQi=>
MDA-MB-468 MnjLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\jeFUh\GG7 M{W5[WlEPTB;NT6wJO69VQ>? M1q0V|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{[wOFk3Lz5{M{e2NFQ6PjxxYU6=
MDA-MB-231 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvFTYE2KGSjeR?= M2SyWWlEPTB;Nj65JO69VQ>? MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd4MES5Okc,OjN5NkC0PVY9N2F-
PC-9PTEN− MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvXNlAh|ryP MmXpNVQ1KGh? MWrJR|UxRTZwNUKg{txO NECwdGk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{KzPVgxQSd-MkOyN|k5ODl:L3G+
PC-9 NG\PcHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4n1OFIxKM7:TR?= M4TBe|E1PCCq NG\ZXm9KSzVyPUWuPFgh|ryP MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzJ|OUiwPUc,OjN{M{m4NFk9N2F-
H1650PTEN+ NH;3fVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVL3[WV5OjBizszN MorlNVQ1KGh? MnK0TWM2OD13MD64N{DPxE1? NGrHbIM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{KzPVgxQSd-MkOyN|k5ODl:L3G+
H1650 NH7Ufm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX2yNEDPxE1? Mn\XNVQ1KGh? M3jpfWlEPTB;MUWuOFch|ryP M{D4VVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MkO5PFA6Lz5{M{KzPVgxQTxxYU6=
Mouse ATM−/− ES Cells MUDDfZRwfG:6aXOgRZN{[Xl? NUnhbHN7Oi53IN88US=> MlmyNlAhcA>? NX65TIFGW2mpbnnmbYNidnSueTDpcohq[mm2czDj[YxtKHO3co\peoFt NEDOUYk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O1OVQ5QSd-MkOzOVU1QDl:L3G+
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BB30-HNC NXvVWIhpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVf6XpBtUUN3ME20PE4{ODd{IN88US=> NUTlbVNPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTJzNki2M{c,W0GQR1XSQE9iRg>?
T98G MnHIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTR6LkS2N|Mh|ryP MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1NlE3QDZxJ{7TRW5ITVJ:L3G+
NCI-H1573 NF7Re4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml32TWM2OD12OT60OFYzKM7:TR?= NU\neFdTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTJzNki2M{c,W0GQR1XSQE9iRg>?
MEG-01 NVzHZpJDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLvU2FKSzVyPUS5Mlc1OTFizszN NIH6bpA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2OjF4OE[vK|5USU6JRWK8M4E,
WM-115 NF35PIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEWwW|NKSzVyPUS5MlkzOjJizszN M17KO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFUzOTZ6Nj:nQnNCVkeHUkyvZV4>
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
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]

  • 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]

  • 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。

动物实验:

[3]

  • Animal Models: 携带Brca1-/-;p53-/-乳腺癌的 K14cre;Brca1F/F;p53F/F
  • Dosages: 50 mg/kg
  • Administration: 按10 μL/g剂量腹腔注射

溶解度(25°C)

体外

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 3年 -20°C 粉状
2年 -80°C 溶于溶剂

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

摩尔浓度计算器

质量 浓度 体积 分子量

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05128734 Not yet recruiting Drug: Temozolomide|Drug: Olaparib Breast Cancer Triple Negative AHS Cancer Control Alberta December 1 2022 Phase 2
NCT05358639 Not yet recruiting Drug: Olaparib tablet|Drug: Navitoclax High Grade Serous Carcinoma|Triple Negative Breast Cancer|Ovarian Cancer Sunnybrook Health Sciences Centre|Exactis Innovation|Centre hospitalier de l''Université de Montréal (CHUM)|Princess Margaret Hospital Canada June 15 2022 Phase 1
NCT04644289 Recruiting Drug: olaparib|Drug: durvalumab Epithelial Ovarian Cancer AGO Research GmbH May 5 2022 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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.