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142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 NXTme|hQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvkNE4yNTFyMDDuUS=> NF7Sb|EzPC92OD:3NkBp M1\Qd4lvcGmkaYTzJINmdGxicILvcIln\XKjdHnvckBld3OnIHTldIVv\GWwdHz5 M4nxT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MES3Olk4Lz5{NkC0O|Y6PzxxYU6=
BR5FVB1-Akt MmX2RZBweHSxc3nzJGF{e2G7 MWmwMlEuOTByIH7N NGSzXW84OiCq M1fSS4lv\HWlZYOgZZBweHSxc3nz MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjB2N{[5O{c,OjZyNEe2PVc9N2F-
Capan-1 NVHmZnd{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXG0VnFqUUN3ME2xOk4x6oDLwsJihKk2NjUkgJpCuW3DqA>? M335U|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OE[0OVkxLz5{NUi2OFU6ODxxYU6=
MIA PaCa-2 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTV6LkKz5qCKyrIkgJm4MlHjiIoEtV5CpC=> NGrndHo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUi2OFU6OCd-MkW4OlQ2QTB:L3G+
RD MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRThwNzDuUS=> M3:0eFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mk[zOVM6Lz5{NUK2N|U{QTxxYU6=
Rh41 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13URmlEPTB;OD6xJI5O MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ4M{WzPUc,OjV{NkO1N|k9N2F-
Rh18 MkThS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTRwOTDuUS=> NFHNWoM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK2N|U{QSd-MkWyOlM2Ozl:L3G+
Rh30 NYjuW29YT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;2OWlEPTB;M{GuNUBvVQ>? M13lS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mk[zOVM6Lz5{NUK2N|U{QTxxYU6=
BT-12 M37GfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPXTWM2OD8kgJmxMFAxOCCwTR?= NYD3ZXhwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyOlM2OzlpPkK1NlY{PTN7PD;hQi=>
CHLA-266 M4D0NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{TpZmlEPTB-4pEJNUwxODBibl2= MnywQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{NkO1N|koRjJ3Mk[zOVM6RC:jPh?=
TC-71 M{\KeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jE[WlEPTB;Mz63JI5O MnXVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{NkO1N|koRjJ3Mk[zOVM6RC:jPh?=
CHLA-9 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDNSG5LUUN3ME24MlIhdk1? Mn;ZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{NkO1N|koRjJ3Mk[zOVM6RC:jPh?=
CHLA-10 NHzWb2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1ntXmlEPTB;NkeuPEBvVQ>? NWq0PYxxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyOlM2OzlpPkK1NlY{PTN7PD;hQi=>
CHLA-258 M13q[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWey[G1wUUN3ME20MlYhdk1? NIfzUpo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK2N|U{QSd-MkWyOlM2Ozl:L3G+
SJ-GBM2 NETqeYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\nTWM2OD1zNj6yJI5O NHyxb|A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK2N|U{QSd-MkWyOlM2Ozl:L3G+
NB-1643 M2TlUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1X5NmlEPTB;MUiuOEBvVQ>? NUDL[WQ5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyOlM2OzlpPkK1NlY{PTN7PD;hQi=>
NB-EBc1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfZV5VKSzVyPUK1Mlghdk1? NV;pWXB3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyOlM2OzlpPkK1NlY{PTN7PD;hQi=>
CHLA-90 NYmzZ5VwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPTTWM2OD8kgJmxMFAxOCCwTR?= NW\VZ4pZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyOlM2OzlpPkK1NlY{PTN7PD;hQi=>
CHLA-136 MmnTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnBUIdpUUN3ME2xOE4zKG6P MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ4M{WzPUc,OjV{NkO1N|k9N2F-
NALM-6 NIW0[VFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmf2TWM2OD12OTDuUS=> MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ4M{WzPUc,OjV{NkO1N|k9N2F-
COG-LL-317 M1z0OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXzv[oFqUUN3ME25MlQhdk1? MoX4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{NkO1N|koRjJ3Mk[zOVM6RC:jPh?=
RS4;11 NUDybVM2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHNZlBKSzVyPUWyMlYhdk1? NYPKWIhHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyOlM2OzlpPkK1NlY{PTN7PD;hQi=>
MOLT-4 NX\YcYZmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVjtW5FjUUN3ME2xOk43KG6P NFiyPWs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK2N|U{QSd-MkWyOlM2Ozl:L3G+
CCRF-CEM MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITLPHhKSzVyPU[5O{4{KG6P NWHwOoN2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyOlM2OzlpPkK1NlY{PTN7PD;hQi=>
Kasumi-1 NULzcJdTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTd6Nj6yJI5O MoHtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{NkO1N|koRjJ3Mk[zOVM6RC:jPh?=
Karpas-299 NITWSHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;FfmlEPTB;N{WuO{BvVQ>? MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ4M{WzPUc,OjV{NkO1N|k9N2F-
Ramos-RA1 NFrvS|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTzWWRKSzVyPU[4MlMhdk1? M1;Y[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mk[zOVM6Lz5{NUK2N|U{QTxxYU6=
DT40 NFPNUGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2HETmlEPTB;NDDuUS=> NXu4[nBLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOVY5OTNpPkK0N|U3QDF|PD;hQi=>
DU145 Mn3OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH:zNnNKSzVyPUGxJI5O NXz1Z4V2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOVY5OTNpPkK0N|U3QDF|PD;hQi=>
H209 NYrucnlMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIj3c2RKSzVyPUGuO{BvVQ>? MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB5N{O1NEc,OjRyN{ezOVA9N2F-
H1048 M4Phdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXh[Is6UUN3ME2yMlIhdk1? MkDEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyN{ezOVAoRjJ2MEe3N|UxRC:jPh?=
H524 MmTKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2T4SmlEPTB;Mz6xJI5O NVe2e5M6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwO|c{PTBpPkK0NFc4OzVyPD;hQi=>
H1930 MoD5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTsZotkUUN3ME20MlEhdk1? NYXDcYJIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwO|c{PTBpPkK0NFc4OzVyPD;hQi=>
H69 NIH6UFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LxZ2lEPTB;NT6yJI5O M4TYd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEe3N|UxLz5{NEC3O|M2ODxxYU6=
H2081 NXXaT4gyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXzNWpKSzVyPU[uN{BvVQ>? MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB5N{O1NEc,OjRyN{ezOVA9N2F-
H2107 M4X0[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHHTWM2OD15LkOgcm0> NI\HWnQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC3O|M2OCd-MkSwO|c{PTB:L3G+
H1092 MkjKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXQRnNKSzVyPUiuPUBvVQ>? NIXCPJc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC3O|M2OCd-MkSwO|c{PTB:L3G+
DMS-79 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\EXlhKSzVyPUmuN{BvVQ>? NGrQWlg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC3O|M2OCd-MkSwO|c{PTB:L3G+
H446 M4L3cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHiTWM2OD1zMzDuUS=> MnnoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyN{ezOVAoRjJ2MEe3N|UxRC:jPh?=
COR-L279 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVzJR|UxRTF3IH7N M3nCN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEe3N|UxLz5{NEC3O|M2ODxxYU6=
LoVo NY\QcGh6TnWwY4Tpc44h[XO|YYm= MmDaN|AhdWmwcx?= MkDMSWM2OCB;IECuNFAzPSEQvF2= NEPlNWs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe2NVA6Pid-MkW3OlExQTZ:L3G+
MX1 NHG0ZmREgXSxdH;4bYNqfHliYYPzZZk> M2fxTWVEPTBiPTCwMlAxODNizszN MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjZ3MkexO{c,OjZ4NUK3NVc9N2F-
LoVo NGP1[ZVHfW6ldHnvckBie3OjeR?= NIfyRWY{OCCvaX7z NF23W2NGSzVyIE2gNE4xODJ3MTFOwG0> NUXSNm1ORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[2OVI4OTdpPkK2OlUzPzF5PD;hQi=>
LoVo M1Tq[mN6fG:2b4jpZ4l1gSCjc4PhfS=> NXzWNotmOC52IIXN MnPkOUBl[Xm| MWjHTVUxKD1iMD6wNFQh|ryP NX7JPHpQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[2OVI4OTdpPkK2OlUzPzF5PD;hQi=>
Capan1 NHvnVGdEgXSxdH;4bYNqfHliYYPzZZk> NXzNUlJuTUN3MDC9JFAvODB3IN88US=> NUDzTZhCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[2OVI4OTdpPkK2OlUzPzF5PD;hQi=>
MRC5 Mnn0R5l1d3SxeHnjbZR6KGG|c3H5 NIXOfFhGSzVyIE2gNE4{OSEQvF2= NH\xeVk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nk[1NlcyPyd-Mk[2OVI4OTd:L3G+
MX1 Moi1SpVv[3Srb36gZZN{[Xl? NEXjSIgyKG2pL3vn NUiyR3VrOiBuODDhcoQhOjRiaILz MULE[YNz\WG|ZTDpckBRSVJibHX2[YwhcW5iYYTofY1q[yCwdT;ueUBud3W|ZTD4[Y5w\3KjZoTl[EB4cXSqIHj1cYFvKE2[MTDj[YxteyCjdDCxJI1oN2upLDDwc{Bi\G2rbnnzeIVz\WRiYYOgd4lv\2ynIHTvd4UhdWWjc4Xy[YQh[W[2ZYKgNkAtQCCjbnSgNlQhcHK|IHL5JGVNUVOD NEP6U4Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nk[1NlcyPyd-Mk[2OVI4OTd:L3G+
MX1 M4e5TmFvfGm2dX3vdkBie3OjeR?= NVPzTmVJOC5|MzDt[{9s\w>? NIXxSIczQCCmYYnz NYHpOIxESW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhSlKFQUGg[IVncWOrZX70JIh2dWGwIF3YNUBk\WyuczD4[Y5w\3KjZoTl[EBqdiCjdHj5cYlkKG63L371JI1wfXOnIHH0JFAvOzNibXevb4ctKHCxIIHkJIFldWmwaYP0[ZJm\CCob4KgNlgh\GG7cx?= MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjZ3MkexO{c,OjZ4NUK3NVc9N2F-
MX1 MWPBcpRqfHWvb4KgZZN{[Xl? NHvrfmwxNjF4NTDt[{9s\w>? M4[3SlI5KGSjeYO= MmTnRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgRnJESTFiZHXmbYNq\W62IHj1cYFvKE2[MTDj[YxteyC6ZX7v[5Ji\nSnZDDpckBifGi7bXnjJI52N263IH3veZNmKGG|c3Xzd4VlKGG|IIT1cY9zKGe{b4f0bEBqdmirYnn0bY9vKGG2IECuNVY2KG2pL3vnMEBxdyCjZH3pcol{fGW{ZXSgeJdq[2ViYTDkZZkh\m:{IEK4JIRigXN? NHHDS4E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nk[1NlcyPyd-Mk[2OVI4OTd:L3G+
MX1 M1uzb2Z2dmO2aX;uJIF{e2G7 Mlq4NE4{OyCvZz;r[y=> Mor1VI91\W62aXH0bY9vKG:oIHPhdoJweGyjdHnuMYlv\HWlZXSgeJVud3JiZ4Lve5RpKGmwaHnibZRqd25ib3[gRnJESTFiZHXmbYNq\W62IHj1cYFvKE2[MTDj[YxteyC6ZX7v[5Ji\nSnZDDpckBifGi7bXnjJI52N263IH3veZNmKGG2IECuN|MhdWdxa3egdI8h[W6mIHHubY1idHNid3Xy[UB1emWjdHXkJJdqfGhiY3HyZo9xdGG2aX6gZZQhOzVibXevb4ctKGmyIH;uJIRigSBz Mmq0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ4NUK3NVcoRjJ4NkWyO|E4RC:jPh?=
MDA-MB-436 NWK5VJN1SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MmPCO{Bl[Xm| NVvlSIpqUUN3MDC9JFAvODByNzFOwG0> MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDZ7MkmxOkc,Ojh4OUK5NVY9N2F-
Capan1 NX7Rco1DSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NE\wS2g4KGSjeYO= MVPJR|UxKD1iMD6wNFE5KM7:TR?= M{HPZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NkmyPVE3Lz5{OE[5NlkyPjxxYU6=
VC8 Ml\5R5l1d3SxeHnjbZR6KGG|c3H5 M{K1N|Mh\GG7cx?= M3rjTmlEPTBiPTCwMlAxPDJizszN M1HNUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NkmyPVE3Lz5{OE[5NlkyPjxxYU6=
V79 NXfrb4dNS3m2b4TvfIlkcXS7IHHzd4F6 MXezJIRigXN? MWrJR|UxKD1iNT6wNVE1KM7:TR?= NYnQUVhlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki2PVI6OTZpPkK4OlkzQTF4PD;hQi=>
Capan1 MWfGeY5kfGmxbjDhd5NigQ>? NUHKd3o5OC5zIIXN M1nYOFQhcHK| MlzhTY5pcWKrdHnvckBw\iCSQWLQNUBqdiCEUlPBNkBl\W[rY3nlcpQhcHWvYX6gR4Fx[W5zIHPlcIx{KGG|c3Xzd4VlKGG|IHnuZ5Jm[XOnIHnuJHBCWlBzLVTORUB1emGycHnu[{BifCByLkGgeW0h[W[2ZYKgOEBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDZ7MkmxOkc,Ojh4OUK5NVY9N2F-
MDA-MB-436 MWfGeY5kfGmxbjDhd5NigQ>? M1HtfFEhfU1? NYq0VWx7PCCqcoO= NWjISmVyUW6qaXLpeIlwdiCxZjDQRXJROSCrbjDCVmNCOSCmZX\pZ4lmdnRiaIXtZY4hVUSDLV3CMVQ{PiClZXzsd{Bie3Onc4Pl[EBieyCrbnPy[YF{\SCrbjDQRXJROS2GTlGgeJJieHCrbnegZZQhOSC3TTDh[pRmeiB2IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= M4HzeVxiKHSjcnfleF0oZ2KuYX7rK{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、SDS / 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、SDS / 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
NCT04987931 Not yet recruiting Drug: Talazoparib Breast Cancer Pfizer August 10 2021 --
NCT04991480 Not yet recruiting Drug: ART4215|Drug: Talazoparib Advanced Cancer|Metastatic Cancer|Breast Cancer Artios Pharma Ltd August 2021 Phase 1|Phase 2
NCT04901702 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
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

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID