Talazoparib (BMN 673)

目录号:S7048 别名: LT-673

仅限科研使用

Talazoparib (BMN 673, LT-673)是一种新型的PARP抑制剂,无细胞试验中对PARP1的IC50为0.57 nM。它也是有效的PARP-2抑制剂,但不抑制PARG,对PTEN突变型高度敏感。Phase 3。

Talazoparib (BMN 673) Chemical Structure

CAS: 1207456-01-6

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 4005.46 现货
RMB 3831.14 现货
大包装 有超大折扣
大剂量询单有大折扣!

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Talazoparib (BMN 673)发表文献167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 Talazoparib (BMN 673, LT-673)是一种新型的PARP抑制剂,无细胞试验中对PARP1的IC50为0.57 nM。它也是有效的PARP-2抑制剂,但不抑制PARG,对PTEN突变型高度敏感。Phase 3。
特性 到目前为止报道的最有效的选择性PARP抑制剂。
靶点
PARP1 [1]
(Cell-free assay)
0.57 nM
体外研究

BMN-673 选择性与PARP 结合,且抑制PARP-介导的通过碱基切除修复途径的单链DNA断裂的修复。增强了DNA链断裂的积累,促进基因组不稳定性,并最终导致细胞凋亡。BMN 673选择性杀死BRCA-1或BRCA-2突变的癌细胞。BMN 673作用于BRCA-1突变 (MX-1,IC50 = 0.3 nM) 和BRCA-2 突变的细胞(Capan-1,IC50 = 5 nM),具有单药细胞毒性。相反, BMN-673 作用于MRC-5正常人类成纤维细胞和其他含野生型BRCA-1 和 BRCA-2基因的肿瘤细胞系,IC50为90 nM到1.9 μM。[1] BMN 673 作用于培养的人类癌细胞,也显著增强Temozolomide 和 SN-38的细胞毒性效果。[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BR5FVB1-Akt Mlv6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXNNE4yNTFyMDDuUS=> Ml;UNlQwPDhxN{KgbC=> NYfLN2c2cW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> NVrnS3pZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wOFc3QTdpPkK2NFQ4Pjl5PD;hQi=>
BR5FVB1-Akt NXmxcnVDSXCxcITvd4l{KEG|c3H5 MnnpNE4yNTFyMDDuUS=> MXq3NkBp M{HteYlv\HWlZYOgZZBweHSxc3nz MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjB2N{[5O{c,OjZyNEe2PVc9N2F-
Capan-1 M4PpWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\SUpFxUUN3ME2xOk4x6oDLwsJihKk2NjUkgJpCuW3DqA>? MnPlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6NkS1PVAoRjJ3OE[0OVkxRC:jPh?=
MIA PaCa-2 NWLHW3l4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjE[|hKSzVyPUW4MlI{6oDLwsJihKk5NjIkgJpCuW3DqA>? MoHEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6NkS1PVAoRjJ3OE[0OVkxRC:jPh?=
RD MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvISGFKSzVyPUiuO{BvVQ>? NWnONllFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyOlM2OzlpPkK1NlY{PTN7PD;hQi=>
Rh41 M2LSUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzWS4NKSzVyPUiuNUBvVQ>? MoG0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{NkO1N|koRjJ3Mk[zOVM6RC:jPh?=
Rh18 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHE[41KSzVyPUSuPUBvVQ>? NITm[|U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK2N|U{QSd-MkWyOlM2Ozl:L3G+
Rh30 NXjyPYx3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTNzLkGgcm0> MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ4M{WzPUc,OjV{NkO1N|k9N2F-
BT-12 M4jrVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYPLWlNkUUN3ME9ihKkyNDByMDDuUS=> MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ4M{WzPUc,OjV{NkO1N|k9N2F-
CHLA-266 M3PFSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnKfHJKSzVyPvMAjVEtODByIH7N NInJV3M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK2N|U{QSd-MkWyOlM2Ozl:L3G+
TC-71 NHWyfmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfhdndzUUN3ME2zMlchdk1? MoPIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{NkO1N|koRjJ3Mk[zOVM6RC:jPh?=
CHLA-9 NIHsW|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\aTWM2OD16LkKgcm0> NWHSRo9WRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyOlM2OzlpPkK1NlY{PTN7PD;hQi=>
CHLA-10 M2m0cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTZ5Lkigcm0> NVTHfoV2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyOlM2OzlpPkK1NlY{PTN7PD;hQi=>
CHLA-258 M3PaVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUP3UoIxUUN3ME20MlYhdk1? Mm\nQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{NkO1N|koRjJ3Mk[zOVM6RC:jPh?=
SJ-GBM2 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTF4LkKgcm0> Ml:1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{NkO1N|koRjJ3Mk[zOVM6RC:jPh?=
NB-1643 MnLRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml61TWM2OD1zOD60JI5O M4jB[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mk[zOVM6Lz5{NUK2N|U{QTxxYU6=
NB-EBc1 MmHGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFezeXlKSzVyPUK1Mlghdk1? MkLNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{NkO1N|koRjJ3Mk[zOVM6RC:jPh?=
CHLA-90 NFHnVlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4rDdmlEPTB-4pEJNUwxODBibl2= M1rvdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mk[zOVM6Lz5{NUK2N|U{QTxxYU6=
CHLA-136 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2Pt[GlEPTB;MUSuNkBvVQ>? MkXOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{NkO1N|koRjJ3Mk[zOVM6RC:jPh?=
NALM-6 NGrabI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXsOmdKSzVyPUS5JI5O NHK1SWY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK2N|U{QSd-MkWyOlM2Ozl:L3G+
COG-LL-317 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTlwNDDuUS=> M17We|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mk[zOVM6Lz5{NUK2N|U{QTxxYU6=
RS4;11 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfSR4RkUUN3ME21Nk43KG6P M3HtfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mk[zOVM6Lz5{NUK2N|U{QTxxYU6=
MOLT-4 NV;ESJFkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTF4Lk[gcm0> NYHIdGRZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyOlM2OzlpPkK1NlY{PTN7PD;hQi=>
CCRF-CEM NILWT4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUHGXHRGUUN3ME22PVcvOyCwTR?= NYnuNZJMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyOlM2OzlpPkK1NlY{PTN7PD;hQi=>
Kasumi-1 NUPKVnRpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlu0TWM2OD15OE[uNkBvVQ>? NE\EcZA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK2N|U{QSd-MkWyOlM2Ozl:L3G+
Karpas-299 M1jDVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUD2ZYdmUUN3ME23OU44KG6P MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ4M{WzPUc,OjV{NkO1N|k9N2F-
Ramos-RA1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDRTWM2OD14OD6zJI5O M4HaZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mk[zOVM6Lz5{NUK2N|U{QTxxYU6=
DT40 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIWzcYRKSzVyPUSgcm0> MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN3NkixN{c,OjR|NU[4NVM9N2F-
DU145 Mn2zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPRZ|dyUUN3ME2xNUBvVQ>? NI\s[XU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO1OlgyOyd-MkSzOVY5OTN:L3G+
H209 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjjV|JiUUN3ME2xMlchdk1? NUW5eJU{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwO|c{PTBpPkK0NFc4OzVyPD;hQi=>
H1048 M1TEU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{LYW2lEPTB;Mj6yJI5O M1roZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEe3N|UxLz5{NEC3O|M2ODxxYU6=
H524 M3Phfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTNwMTDuUS=> NGXkXGc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC3O|M2OCd-MkSwO|c{PTB:L3G+
H1930 NVPrdnFsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFrlcWZKSzVyPUSuNUBvVQ>? MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB5N{O1NEc,OjRyN{ezOVA9N2F-
H69 M4\BUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTVwMjDuUS=> M3HnN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEe3N|UxLz5{NEC3O|M2ODxxYU6=
H2081 M2PrOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULBS5FGUUN3ME22MlMhdk1? M4KxPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEe3N|UxLz5{NEC3O|M2ODxxYU6=
H2107 M{LnWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDmOoVUUUN3ME23MlMhdk1? MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB5N{O1NEc,OjRyN{ezOVA9N2F-
H1092 M{HHbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHrTFFFUUN3ME24Mlkhdk1? NXm0N3hwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwO|c{PTBpPkK0NFc4OzVyPD;hQi=>
DMS-79 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTlwMzDuUS=> M3P0S|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEe3N|UxLz5{NEC3O|M2ODxxYU6=
H446 M2m5eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4X1[GlEPTB;MUOgcm0> NFHBZno9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC3O|M2OCd-MkSwO|c{PTB:L3G+
COR-L279 NEjLZYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnWUXhKSzVyPUG1JI5O NGfj[pE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC3O|M2OCd-MkSwO|c{PTB:L3G+
LoVo Ml;DSpVv[3Srb36gZZN{[Xl? MoLiN|AhdWmwcx?= MlrlSWM2OCB;IECuNFAzPSEQvF2= M4HPRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{[xNFk3Lz5{NUe2NVA6PjxxYU6=
MX1 NYXUT5BUS3m2b4TvfIlkcXS7IHHzd4F6 MX3FR|UxKD1iMD6wNFA{KM7:TR?= NGLlfJM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nk[1NlcyPyd-Mk[2OVI4OTd:L3G+
LoVo MVnGeY5kfGmxbjDhd5NigQ>? Moi3N|AhdWmwcx?= MV;FR|UxKD1iMD6wNFI2OSEQvF2= MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjZ3MkexO{c,OjZ4NUK3NVc9N2F-
LoVo M4H0SGN6fG:2b4jpZ4l1gSCjc4PhfS=> NFu4fpUxNjRidV2= MWS1JIRigXN? NH;DeXFIUTVyIE2gNE4xODRizszN MlW5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ4NUK3NVcoRjJ4NkWyO|E4RC:jPh?=
Capan1 MUHDfZRwfG:6aXPpeJkh[XO|YYm= M2fj[GVEPTBiPTCwMlAxPSEQvF2= MnjvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ4NUK3NVcoRjJ4NkWyO|E4RC:jPh?=
MRC5 NIi0VmlEgXSxdH;4bYNqfHliYYPzZZk> M1nmfmVEPTBiPTCwMlMyKM7:TR?= NEXkTlU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nk[1NlcyPyd-Mk[2OVI4OTd:L3G+
MX1 NXvGU|ZLTnWwY4Tpc44h[XO|YYm= NFH5UGEyKG2pL3vn MVWyJEw5KGGwZDCyOEBpenN? NF;JR49F\WO{ZXHz[UBqdiCSQWKgcIV3\WxiaX6gZZRpgW2rYzDueU9vfSCvb4Xz[UB5\W6xZ4Lh[pRm\CC5aYToJIh2dWGwIF3YNUBk\WyuczDheEAyKG2pL3vnMEBxdyCjZH3pcol{fGW{ZXSgZZMhe2mwZ3zlJIRwe2VibXXhd5Vz\WRiYX\0[ZIhOiBuODDhcoQhOjRiaILzJIJ6KEWOSWPB M4\4Z|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NkWyO|E4Lz5{Nk[1NlcyPzxxYU6=
MX1 NGfkUFRCdnSrdIXtc5Ih[XO|YYm= NUHT[pN3OC5|MzDt[{9s\w>? MY[yPEBl[Xm| M4i5b2FvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JGJTS0FzIHTl[olkcWWwdDDoeY1idiCPWEGgZ4VtdHNieHXuc4dz[W[2ZXSgbY4h[XSqeX3pZ{BvfS:wdTDtc5V{\SCjdDCwMlM{KG2pL3vnMEBxdyCzZDDh[I1qdmm|dHXy[YQh\m:{IEK4JIRigXN? MlfmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ4NUK3NVcoRjJ4NkWyO|E4RC:jPh?=
MX1 MVTBcpRqfHWvb4KgZZN{[Xl? NX;SPIM1OC5zNkWgcYcwc2d? NHvNcHMzQCCmYYnz NVHDV|FNSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhSlKFQUGg[IVncWOrZX70JIh2dWGwIF3YNUBk\WyuczD4[Y5w\3KjZoTl[EBqdiCjdHj5cYlkKG63L371JI1wfXOnIHHzd4V{e2WmIHHzJJR2dW:{IHfyc5d1cCCrbnjpZol1cW:wIHH0JFAvOTZ3IH3nM4toNCCybzDh[I1qdmm|dHXy[YQhfHerY3WgZUBl[XliZn;yJFI5KGSjeYO= NFvBcXU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nk[1NlcyPyd-Mk[2OVI4OTd:L3G+
MX1 NV7a[WFjTnWwY4Tpc44h[XO|YYm= MnTJNE4{OyCvZz;r[y=> MVfQc5RmdnSrYYTpc44hd2ZiY3HyZo9xdGG2aX6tbY5lfWOnZDD0eY1weiCpcn;3eIghcW6qaXLpeIlwdiCxZjDCVmNCOSCmZX\pZ4lmdnRiaIXtZY4hVVhzIHPlcIx{KHinbn;ndoFnfGWmIHnuJIF1cHmvaXOgcpUwdnVibX;1d4Uh[XRiMD6zN{Bu\y:tZzDwc{BidmRiYX7pcYFteyC5ZYLlJJRz\WG2ZXSge4l1cCClYYLic5Bt[XSrbjDheEA{PSCvZz;r[{whcXBib36g[IF6KDF? NXPOUY84RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[2OVI4OTdpPkK2OlUzPzF5PD;hQi=>
MDA-MB-436 NYnWZW14SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NF:4UJc4KGSjeYO= MXvJR|UxKD1iMD6wNFA4KM7:TR?= MmPZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh4OUK5NVYoRjJ6NkmyPVE3RC:jPh?=
Capan1 NYfvWJd2SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M3zYNFch\GG7cx?= M3;TeWlEPTBiPTCwMlAxOThizszN NUXKVIJGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki2PVI6OTZpPkK4OlkzQTF4PD;hQi=>
VC8 M1;lN2N6fG:2b4jpZ4l1gSCjc4PhfS=> MmToN{Bl[Xm| MoKwTWM2OCB;IECuNFA1OiEQvF2= NGnaeW89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OE[5NlkyPid-Mki2PVI6OTZ:L3G+
V79 M3zhOGN6fG:2b4jpZ4l1gSCjc4PhfS=> M1XKTFMh\GG7cx?= M3jaUWlEPTBiPTC1MlAyOTRizszN MkGwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh4OUK5NVYoRjJ6NkmyPVE3RC:jPh?=
Capan1 MlL1SpVv[3Srb36gZZN{[Xl? M2X5TVAvOSC3TR?= MVK0JIhzew>? M{\NNGlvcGmkaYTpc44hd2ZiUFHSVFEhcW5iQmLDRVIh\GWoaXPp[Y51KGi3bXHuJGNieGGwMTDj[YxteyCjc4Pld5Nm\CCjczDpcoNz\WG|ZTDpckBRSVKSMT3EUmEhfHKjcIDpcoch[XRiMD6xJJVOKGGodHXyJFQhcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? NYXrU4VQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki2PVI6OTZpPkK4OlkzQTF4PD;hQi=>
MDA-MB-436 M{L2OWZ2dmO2aX;uJIF{e2G7 MknGNUB2VQ>? M4XsVVQhcHK| NX\mSnY{UW6qaXLpeIlwdiCxZjDQRXJROSCrbjDCVmNCOSCmZX\pZ4lmdnRiaIXtZY4hVUSDLV3CMVQ{PiClZXzsd{Bie3Onc4Pl[EBieyCrbnPy[YF{\SCrbjDQRXJROS2GTlGgeJJieHCrbnegZZQhOSC3TTDh[pRmeiB2IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= NEm1SFc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OE[5NlkyPid-Mki2PVI6OTZ:L3G+
Assay
Methods Test Index PMID
Western blot cleaved-PARP / cleaved-caspase3 / γ-H2AX pKAP1 / pChk2 / pChk1 PD-L1 p-ATM 29158830 28947502 28167507 30472087
Growth inhibition assay Cell viability 29158830
Immunofluorescence cleaved PARP / 53BP1 RAD51 28958991 30621214
体内研究 在大鼠的药代动力学研究中,BMN673每天单独给药,具有>50%口服生物有效性和药代动力学特性。在MX-1移植瘤肿瘤模型研究中, BMN 673每天口服给药,显著增强细胞毒性疗法的抗肿瘤效果,这种作用具有剂量依赖性。[2]

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)

动物实验:

[2]

  • Animal Models: MX-1模型(BRCA-1缺陷的)
  • Dosages: 0.33 mg/kg/day,每天一次
  • Administration: 口服处理

溶解度(25°C)

体外

* 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 380.35
化学式

 

C19H14F2N6O
 
CAS号 1207456-01-6
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
NCT05141708 Not yet recruiting Drug: Talazoparib Metastatic Breast Cancer|Breast Neoplasms Pfizer December 2021 --
NCT05053854 Recruiting Drug: Talazoparib Neuroendocrine Tumors Peter MacCallum Cancer Centre Australia September 27 2021 Phase 1
NCT04991480 Recruiting Drug: ART4215|Drug: Talazoparib Advanced Cancer|Metastatic Cancer|Breast Cancer Artios Pharma Ltd September 13 2021 Phase 1|Phase 2
NCT04987931 Completed Drug: Talazoparib Breast Cancer Pfizer August 20 2021 --
NCT04901702 Active not recruiting Drug: Onivyde|Drug: Talazoparib|Drug: Temozolomide Recurrent Solid Tumor|Recurrent Ewing Sarcoma|Recurrent Hepatoblastoma|Recurrent Malignant Germ Cell Tumor|Recurrent Malignant Solid Neoplasm|Recurrent Neuroblastoma|Recurrent Osteosarcoma|Recurrent Peripheral Primitive Neuroectodermal Tumor|Recurrent Rhabdoid Tumor|Recurrent Rhabdomyosarcoma|Recurrent Soft Tissue Sarcoma|Recurrent Wilms Tumor|Refractory Ewing Sarcoma|Refractory Hepatoblastoma|Refractory Malignant Germ Cell Tumor|Refractory Malignant Solid Neoplasm|Refractory Neuroblastoma|Refractory Osteosarcoma|Refractory Peripheral Primitive Neuroectodermal Tumor|Refractory Rhabdoid Tumor|Refractory Rhabdomyosarcoma|Refractory Soft Tissue Sarcoma St. Jude Children''s Research Hospital|Pfizer|Ipsen June 9 2021 Phase 1|Phase 2

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

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常见问题及建议解决方法

问题 1:
Which solvent do you recommend to dilute the inhibitor for in vivo study in mice?

回答:
BMN673 (S7048) can be dissolved in vehicle (10% DMAc, 6% Solutol, and 84% PBS) according to the paper: http://clincancerres.aacrjournals.org/content/19/18/5003.full. Quote from Method and Material section "Xenograft experiments: BMN 673 (various doses as indicated), or vehicle (10% DMAc, 6% Solutol, and 84% PBS) was administered by oral gavage"