Talazoparib (BMN 673)

For research use only. Not for use in humans.

目录号:S7048 别名: LT-673

Talazoparib (BMN 673) Chemical Structure

CAS No. 1207456-01-6

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。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 4005.46 现货
RMB 3831.14 现货
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客户使用Selleck生产的Talazoparib (BMN 673)发表文献137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 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 NX[xc5NOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVm3bpdbOC5zLUGwNEBvVQ>? NHK4d4czPC92OD:3NkBp MV\pcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36g[I9{\SCmZYDlcoRmdnSueR?= NFHP[4Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkC0O|Y6Pyd-Mk[wOFc3QTd:L3G+
BR5FVB1-Akt MmjRRZBweHSxc3nzJGF{e2G7 NFGyeIkxNjFvMUCwJI5O NHrveIU4OiCq NXG1WWJvcW6mdXPld{BieG:ydH;zbZM> NX\VS5FzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wOFc3QTdpPkK2NFQ4Pjl5PD;hQi=>
Capan-1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTWT|lKSzVyPUG2MlDjiIoEsfMAjVUvPOLCidM1UeKh NWPaPY54RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4OlQ2QTBpPkK1PFY1PTlyPD;hQi=>
MIA PaCa-2 NI\WXXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTlfVV{UUN3ME21PE4zO+LCidMx5qCKQC5z4pEJxtVOyqB? NXXmemdDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4OlQ2QTBpPkK1PFY1PTlyPD;hQi=>
RD NHXPclVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\OW|NKSzVyPUiuO{BvVQ>? Mo\vQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{NkO1N|koRjJ3Mk[zOVM6RC:jPh?=
Rh41 NYDLUVcyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGq2Z3ZKSzVyPUiuNUBvVQ>? NFrtWpo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK2N|U{QSd-MkWyOlM2Ozl:L3G+
Rh18 MkXzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkL0TWM2OD12Lkmgcm0> NHLIU4s9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK2N|U{QSd-MkWyOlM2Ozl:L3G+
Rh30 MlPiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zaZWlEPTB;M{GuNUBvVQ>? NXGzTJlGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyOlM2OzlpPkK1NlY{PTN7PD;hQi=>
BT-12 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDITHpKSzVyPvMAjVEtODByIH7N MkPSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{NkO1N|koRjJ3Mk[zOVM6RC:jPh?=
CHLA-266 NXXPVo1JT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRuLCiUGsNFAxKG6P MmnmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{NkO1N|koRjJ3Mk[zOVM6RC:jPh?=
TC-71 NYTRXXUyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTNwNzDuUS=> MnXwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{NkO1N|koRjJ3Mk[zOVM6RC:jPh?=
CHLA-9 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\nc|JDUUN3ME24MlIhdk1? MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ4M{WzPUc,OjV{NkO1N|k9N2F-
CHLA-10 Ml;uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DURmlEPTB;NkeuPEBvVQ>? M4\GdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mk[zOVM6Lz5{NUK2N|U{QTxxYU6=
CHLA-258 NYPq[pdVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXO0ZWpVUUN3ME20MlYhdk1? NX7QWZZTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyOlM2OzlpPkK1NlY{PTN7PD;hQi=>
SJ-GBM2 NIXwNZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NILGPYNKSzVyPUG2MlIhdk1? NXv3bJpyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyOlM2OzlpPkK1NlY{PTN7PD;hQi=>
NB-1643 NHjJUVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXj6cHpbUUN3ME2xPE41KG6P M2fG[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mk[zOVM6Lz5{NUK2N|U{QTxxYU6=
NB-EBc1 NG\JXFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\GTWM2OD1{NT64JI5O NUSwcpFtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyOlM2OzlpPkK1NlY{PTN7PD;hQi=>
CHLA-90 NFu5SoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HwemlEPTB-4pEJNUwxODBibl2= MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ4M{WzPUc,OjV{NkO1N|k9N2F-
CHLA-136 M3u0eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;ROW9EUUN3ME2xOE4zKG6P NEPxTZU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK2N|U{QSd-MkWyOlM2Ozl:L3G+
NALM-6 NYPifllYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYr4VXZZUUN3ME20PUBvVQ>? M4izblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mk[zOVM6Lz5{NUK2N|U{QTxxYU6=
COG-LL-317 NWjoZXRLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXtTWM2OD17LkSgcm0> NHfyXoc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK2N|U{QSd-MkWyOlM2Ozl:L3G+
RS4;11 MlfVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTV{Lk[gcm0> NWnnT24{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyOlM2OzlpPkK1NlY{PTN7PD;hQi=>
MOLT-4 M3PaSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTF4Lk[gcm0> MmHIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{NkO1N|koRjJ3Mk[zOVM6RC:jPh?=
CCRF-CEM NHfRPI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3fGWGlEPTB;Nkm3MlMhdk1? MmrRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{NkO1N|koRjJ3Mk[zOVM6RC:jPh?=
Kasumi-1 NXzWN2Z2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTd6Nj6yJI5O NU\kcJJXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyOlM2OzlpPkK1NlY{PTN7PD;hQi=>
Karpas-299 Ml;lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlj0TWM2OD15NT63JI5O NHPmTok9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK2N|U{QSd-MkWyOlM2Ozl:L3G+
Ramos-RA1 NFfsTGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nQS2lEPTB;NkiuN{BvVQ>? Mnq0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{NkO1N|koRjJ3Mk[zOVM6RC:jPh?=
DT40 MkX4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzidHFKSzVyPUSgcm0> MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN3NkixN{c,OjR|NU[4NVM9N2F-
DU145 MoXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTFzIH7N NFX5WpU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO1OlgyOyd-MkSzOVY5OTN:L3G+
H209 M3jMbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTFwNzDuUS=> M1TnW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEe3N|UxLz5{NEC3O|M2ODxxYU6=
H1048 NWjrVlQ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTJwMjDuUS=> MnfKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyN{ezOVAoRjJ2MEe3N|UxRC:jPh?=
H524 M2riWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUflXYVZUUN3ME2zMlEhdk1? M3XKRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEe3N|UxLz5{NEC3O|M2ODxxYU6=
H1930 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHOV3RKSzVyPUSuNUBvVQ>? MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB5N{O1NEc,OjRyN{ezOVA9N2F-
H69 NYXpOWNST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;JR|UxRTVwMjDuUS=> M4LBPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEe3N|UxLz5{NEC3O|M2ODxxYU6=
H2081 NHPWfGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonBTWM2OD14LkOgcm0> NIS1WZQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC3O|M2OCd-MkSwO|c{PTB:L3G+
H2107 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LoXmlEPTB;Nz6zJI5O MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB5N{O1NEc,OjRyN{ezOVA9N2F-
H1092 M1TqOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4PhOWlEPTB;OD65JI5O NH\Nc|U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC3O|M2OCd-MkSwO|c{PTB:L3G+
DMS-79 MofhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGLpXodKSzVyPUmuN{BvVQ>? MmL6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyN{ezOVAoRjJ2MEe3N|UxRC:jPh?=
H446 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HHSmlEPTB;MUOgcm0> NELmPIc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC3O|M2OCd-MkSwO|c{PTB:L3G+
COR-L279 MnP5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzNSXdLUUN3ME2xOUBvVQ>? MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB5N{O1NEc,OjRyN{ezOVA9N2F-
LoVo MUDGeY5kfGmxbjDhd5NigQ>? NYKwNXlNOzBibXnudy=> NVvwT3NRTUN3MDC9JFAvODB{NTFOwG0> M2jTU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{[xNFk3Lz5{NUe2NVA6PjxxYU6=
MX1 NGrlUphEgXSxdH;4bYNqfHliYYPzZZk> MYLFR|UxKD1iMD6wNFA{KM7:TR?= M2HQXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NkWyO|E4Lz5{Nk[1NlcyPzxxYU6=
LoVo NUniVnFtTnWwY4Tpc44h[XO|YYm= M3G1TFMxKG2rboO= Mof4SWM2OCB;IECuNFAzPTFizszN MoHLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ4NUK3NVcoRjJ4NkWyO|E4RC:jPh?=
LoVo MUHDfZRwfG:6aXPpeJkh[XO|YYm= M2PYWVAvPCC3TR?= M1fKXFUh\GG7cx?= NWDQXmV[T0l3MDC9JFAvODB2IN88US=> M3PZPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NkWyO|E4Lz5{Nk[1NlcyPzxxYU6=
Capan1 NIfsOnJEgXSxdH;4bYNqfHliYYPzZZk> MWHFR|UxKD1iMD6wNFUh|ryP M1G1TVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NkWyO|E4Lz5{Nk[1NlcyPzxxYU6=
MRC5 MVTDfZRwfG:6aXPpeJkh[XO|YYm= MnrGSWM2OCB;IECuN|Eh|ryP MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjZ3MkexO{c,OjZ4NUK3NVc9N2F-
MX1 M{HIZWZ2dmO2aX;uJIF{e2G7 MYWxJI1oN2up MlrKNkAtQCCjbnSgNlQhcHK| MnWxSIVkemWjc3WgbY4hWEGUIHzleoVtKGmwIHH0bJlucWNiboWvcpUhdW:3c3WgfIVvd2e{YX\0[YQhf2m2aDDoeY1idiCPWEGgZ4VtdHNiYYSgNUBu\y:tZzygdI8h[WSvaX7pd5RmemWmIHHzJJNqdmeuZTDkc5NmKG2nYYP1doVlKGGodHXyJFIhNDhiYX7kJFI1KGi{czDifUBGVEmVQR?= M4fZRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NkWyO|E4Lz5{Nk[1NlcyPzxxYU6=
MX1 MXHBcpRqfHWvb4KgZZN{[Xl? M4jvVlAvOzNibXevb4c> NHnWSYEzQCCmYYnz MlT3RY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgRnJESTFiZHXmbYNq\W62IHj1cYFvKE2[MTDj[YxteyC6ZX7v[5Ji\nSnZDDpckBifGi7bXnjJI52N263IH3veZNmKGG2IECuN|MhdWdxa3esJJBwKHGmIHHkcYlvcXO2ZYLl[EBnd3JiMkig[IF6ew>? MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjZ3MkexO{c,OjZ4NUK3NVc9N2F-
MX1 NHTMNGtCdnSrdIXtc5Ih[XO|YYm= NWPod5FWOC5zNkWgcYcwc2d? M1n4WFI5KGSjeYO= NFqxRVZCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBDWkODMTDk[YZq[2mnboSgbJVu[W5iTWixJINmdGy|IIjlco9oemGodHXkJIlvKGG2aIntbYMhdnVxboWgcY92e2ViYYPz[ZN{\WRiYYOgeJVud3JiZ4Lve5RpKGmwaHnibZRqd25iYYSgNE4yPjVibXevb4ctKHCxIHHkcYlvcXO2ZYLl[EB1f2mlZTDhJIRigSCob4KgNlgh\GG7cx?= MnnPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ4NUK3NVcoRjJ4NkWyO|E4RC:jPh?=
MX1 NGWxfWRHfW6ldHnvckBie3OjeR?= MkPUNE4{OyCvZz;r[y=> M2DIW3BwfGWwdHnheIlwdiCxZjDjZZJjd3CuYYTpck1qdmS3Y3XkJJR2dW:{IHfyc5d1cCCrbnjpZol1cW:wIH;mJGJTS0FzIHTl[olkcWWwdDDoeY1idiCPWEGgZ4VtdHNieHXuc4dz[W[2ZXSgbY4h[XSqeX3pZ{BvfS:wdTDtc5V{\SCjdDCwMlM{KG2pL3vnJJBwKGGwZDDhcolu[Wy|IIfldoUhfHKnYYTl[EB4cXSqIHPhdoJweGyjdHnuJIF1KDN3IH3nM4toNCCrcDDvckBl[XliMR?= MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjZ3MkexO{c,OjZ4NUK3NVc9N2F-
MDA-MB-436 M3PTW2FvfGmycn;sbYZmemG2aY\lJIF{e2G7 NWnqXVhbPyCmYYnz M{DBN2lEPTBiPTCwMlAxODdizszN M4r3d|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NkmyPVE3Lz5{OE[5NlkyPjxxYU6=
Capan1 NGfJ[IhCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NEPlWm04KGSjeYO= M2q2bWlEPTBiPTCwMlAxOThizszN MmfVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh4OUK5NVYoRjJ6NkmyPVE3RC:jPh?=
VC8 M2G5N2N6fG:2b4jpZ4l1gSCjc4PhfS=> Mn\qN{Bl[Xm| M2XmVGlEPTBiPTCwMlAxPDJizszN NW\WS3BmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki2PVI6OTZpPkK4OlkzQTF4PD;hQi=>
V79 NXHO[W92S3m2b4TvfIlkcXS7IHHzd4F6 M4DWbFMh\GG7cx?= MVLJR|UxKD1iNT6wNVE1KM7:TR?= MmfCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh4OUK5NVYoRjJ6NkmyPVE3RC:jPh?=
Capan1 MoLmSpVv[3Srb36gZZN{[Xl? NV;KNJVmOC5zIIXN M330VlQhcHK| MYTJcohq[mm2aX;uJI9nKFCDUmCxJIlvKEKUQ1GyJIRm\mmlaXXueEBpfW2jbjDDZZBidjFiY3XscJMh[XO|ZYPz[YQh[XNiaX7jdoVie2ViaX6gVGFTWDFvRF7BJJRz[XCyaX7nJIF1KDBwMTD1UUBi\nSncjC0JIhzeyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM> MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDZ7MkmxOkc,Ojh4OUK5NVY9N2F-
MDA-MB-436 MULGeY5kfGmxbjDhd5NigQ>? M3LFS|EhfU1? NFHBO201KGi{cx?= MoTLTY5pcWKrdHnvckBw\iCSQWLQNUBqdiCEUlPBNUBl\W[rY3nlcpQhcHWvYX6gUWRCNU2ELUSzOkBk\WyuczDhd5Nme3OnZDDhd{BqdmO{ZXHz[UBqdiCSQWLQNU1FVkFidILhdJBqdmdiYYSgNUB2VSCjZoTldkA1KGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? M1vCS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NkmyPVE3Lz5{OE[5NlkyPjxxYU6=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
cleaved-PARP / cleaved-caspase3 / γ-H2AX; 

PubMed: 29158830     


Western Blot data testing protein expression after treatment with Olaparib, Niraparib, and Talazoparib on Brca1-deficient cell line in W0069 cells.

pKAP1 / pChk2 / pChk1; 

PubMed: 28947502     


Western blot images (representative from 3 independent experiments) showing the impact of a 24 hour pre-treatment with TAL ± TMZ on DNA damage signaling in U251 (MGMT-low) and T98G (MGMT-high) cells. 

PD-L1; 

PubMed: 28167507     


MDA-MDA-MB-231 and BT549 cells were treated with 10 μM olaparib or 10 nM talazoparib for 24 hours, and subjected to immunoblotting with the indicated antibodies. PD-L1 knockout (K/O) cells were included as a negative control. 

p-ATM; 

PubMed: 30472087     


Western blot analysis of the DNA damage sensors ATM, p-ATM (Ser1981), CHK1, p-CHK1 (Ser317), CHK2 and p-CHK2 (Thr68) in MV4-11 and HL-60 cells. GAPDH served as a loading control.

29158830 28947502 28167507 30472087
Growth inhibition assay
Cell viability; 

PubMed: 29158830     


Measured dose response curve and IC50 of Talazoparib in W780 and W0069 cells.

29158830
Immunofluorescence
cleaved PARP / 53BP1; 

PubMed: 28958991     


Cleaved-PARP and 53BP1 expression. Representative images with 10× objective from high-content imaging of control cells in the left column, and cells treated with veliparib, olaparib, and talazoparib in three right columns. 53BP1 expression is seen in: A, HCC1143; B, MDAMB231; and C, HCC1806. Blue represents nuclear staining and pink foci represent 53BP1 foci. Cleaved-PARP expression is seen in D, HCC1143 and E, HCC1806. Blue represents nuclear staining and green represents cleaved-PARP expression.

RAD51; 

PubMed: 30621214     


(A) MCF7 and (B) MCF7-T cells were treated with either 100 nM tamoxifen (Tamox) or 1 nM talazoparib (Talaz) for 72 h, alone and in combination. 24 h post treatment RAD51 foci formation assay was performed. Scale bar: 20 µm.

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]

- 合并
  • 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
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 38 mg/mL warmed (99.9 mM)
Water Insoluble
Ethanol Insoluble

* 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 粉状
溶于溶剂
别名 LT-673

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)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
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
计算重置

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
NCT04703920 Recruiting Drug: Talazoparib|Drug: Belinostat Metastatic Breast Cancer|Metastatic Castration-resistant Prostate Cancer|Metastatic Ovarian Carcinoma University of Michigan Rogel Cancer Center|Pfizer|Acrotech Biopharma LLC March 4 2021 Phase 1
NCT04672460 Recruiting Drug: TALZENNA capsule|Drug: Talazoparib soft gel capsule Advanced Solid Tumors Pfizer December 21 2020 Phase 1
NCT04497116 Recruiting Drug: RP-3500|Drug: Talazoparib: oral PARP inhibitor Advanced Solid Tumor Adult Repare Therapeutics July 22 2020 Phase 1|Phase 2
NCT04337970 Recruiting Drug: Talazoparib|Drug: Axitinib Kidney Cancer|Renal Cell Carcinoma|Unresectable Renal Cell Carcinoma|Metastatic Renal Cell Carcinoma Memorial Sloan Kettering Cancer Center April 6 2020 Phase 1|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:

    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"

PARP Signaling Pathway Map

PARP Inhibitors with Unique Features

相关PARP产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID