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 1941.03 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127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 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml7iNE4yNTFyMDDuUS=> MYOyOE81QC95MjDo MVPpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36g[I9{\SCmZYDlcoRmdnSueR?= M4TUVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MES3Olk4Lz5{NkC0O|Y6PzxxYU6=
BR5FVB1-Akt MUfBdI9xfG:|aYOgRZN{[Xl? NFrqcJMxNjFvMUCwJI5O MVq3NkBp MlLybY5lfWOnczDhdI9xfG:|aYO= NGKzdo89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkC0O|Y6Pyd-Mk[wOFc3QTd:L3G+
Capan-1 Mm\KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\VUGlEPTB;MU[uNQKBkcLz4pEJOU416oDLwsXNxsA> Mnu2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6NkS1PVAoRjJ3OE[0OVkxRC:jPh?=
MIA PaCa-2 NGWzTW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jnNGlEPTB;NUiuNlPjiIoEsfMAjVgvOeLCidM1UeKh Mm\JQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6NkS1PVAoRjJ3OE[0OVkxRC:jPh?=
RD NYThO4o6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrMTWM2OD16Lkegcm0> MlfHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{NkO1N|koRjJ3Mk[zOVM6RC:jPh?=
Rh41 NI\SXZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PqNGlEPTB;OD6xJI5O NIDrVXU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK2N|U{QSd-MkWyOlM2Ozl:L3G+
Rh18 NWLselhuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHoN2hUUUN3ME20Mlkhdk1? MmjqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{NkO1N|koRjJ3Mk[zOVM6RC:jPh?=
Rh30 M3LDUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXWTWM2OD1|MT6xJI5O MmHqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{NkO1N|koRjJ3Mk[zOVM6RC:jPh?=
BT-12 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUf0U494UUN3ME9ihKkyNDByMDDuUS=> MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ4M{WzPUc,OjV{NkO1N|k9N2F-
CHLA-266 NVvzXmNNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nzfWlEPTB-4pEJNUwxODBibl2= MoTYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{NkO1N|koRjJ3Mk[zOVM6RC:jPh?=
TC-71 NF:wV3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmqxTWM2OD1|Lkegcm0> MlXoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{NkO1N|koRjJ3Mk[zOVM6RC:jPh?=
CHLA-9 M3PZVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrHTG9wUUN3ME24MlIhdk1? MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ4M{WzPUc,OjV{NkO1N|k9N2F-
CHLA-10 Mlv4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTZ5Lkigcm0> M2W0clxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mk[zOVM6Lz5{NUK2N|U{QTxxYU6=
CHLA-258 M17hfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4Lsb2lEPTB;ND62JI5O NWK3[2l{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyOlM2OzlpPkK1NlY{PTN7PD;hQi=>
SJ-GBM2 NE\HTldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3juZWlEPTB;MU[uNkBvVQ>? NW\aPWxSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyOlM2OzlpPkK1NlY{PTN7PD;hQi=>
NB-1643 NFO4OopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2f5cWlEPTB;MUiuOEBvVQ>? M1TBT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mk[zOVM6Lz5{NUK2N|U{QTxxYU6=
NB-EBc1 NGPnepZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{WzTWlEPTB;MkWuPEBvVQ>? MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ4M{WzPUc,OjV{NkO1N|k9N2F-
CHLA-90 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fhN2lEPTB-4pEJNUwxODBibl2= MnPwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{NkO1N|koRjJ3Mk[zOVM6RC:jPh?=
CHLA-136 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXPrfFlFUUN3ME2xOE4zKG6P M4DwXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mk[zOVM6Lz5{NUK2N|U{QTxxYU6=
NALM-6 M2jXR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1OwT2lEPTB;NEmgcm0> M{jQOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mk[zOVM6Lz5{NUK2N|U{QTxxYU6=
COG-LL-317 NWHhRXgyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfvcplKSzVyPUmuOEBvVQ>? M4f2WFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mk[zOVM6Lz5{NUK2N|U{QTxxYU6=
RS4;11 MkfnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHrbph6UUN3ME21Nk43KG6P MnHrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{NkO1N|koRjJ3Mk[zOVM6RC:jPh?=
MOLT-4 MkjvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHYTWM2OD1zNj62JI5O Ml24QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{NkO1N|koRjJ3Mk[zOVM6RC:jPh?=
CCRF-CEM MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4q4TGlEPTB;Nkm3MlMhdk1? NIjUTGo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK2N|U{QSd-MkWyOlM2Ozl:L3G+
Kasumi-1 NIHYbVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTd6Nj6yJI5O M1K0flxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mk[zOVM6Lz5{NUK2N|U{QTxxYU6=
Karpas-299 NHPjSoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTd3Lkegcm0> MonQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{NkO1N|koRjJ3Mk[zOVM6RC:jPh?=
Ramos-RA1 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTZ6LkOgcm0> M4P1TlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mk[zOVM6Lz5{NUK2N|U{QTxxYU6=
DT40 NWjTe3FPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3Pyd2lEPTB;NDDuUS=> M37ZN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{W2PFE{Lz5{NEO1OlgyOzxxYU6=
DU145 MnnFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlP6TWM2OD1zMTDuUS=> MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN3NkixN{c,OjR|NU[4NVM9N2F-
H209 NHP5bVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PXe2lEPTB;MT63JI5O M{Ppb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEe3N|UxLz5{NEC3O|M2ODxxYU6=
H1048 MkHJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn3kTWM2OD1{LkKgcm0> MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB5N{O1NEc,OjRyN{ezOVA9N2F-
H524 Ml3tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjueHZbUUN3ME2zMlEhdk1? NXPTd5hkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwO|c{PTBpPkK0NFc4OzVyPD;hQi=>
H1930 MmHFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHBWm9tUUN3ME20MlEhdk1? MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB5N{O1NEc,OjRyN{ezOVA9N2F-
H69 NWfsW3BCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojyTWM2OD13LkKgcm0> NWrRPWR[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwO|c{PTBpPkK0NFc4OzVyPD;hQi=>
H2081 NXfGTXI2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlzETWM2OD14LkOgcm0> NFvsUJY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC3O|M2OCd-MkSwO|c{PTB:L3G+
H2107 Mlr3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEjqcoJKSzVyPUeuN{BvVQ>? NEP3fFE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC3O|M2OCd-MkSwO|c{PTB:L3G+
H1092 NWLrcVhPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVP6SnpZUUN3ME24Mlkhdk1? NFO4VIU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC3O|M2OCd-MkSwO|c{PTB:L3G+
DMS-79 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXFdFhKSzVyPUmuN{BvVQ>? Mn\NQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyN{ezOVAoRjJ2MEe3N|UxRC:jPh?=
H446 MnHTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M17nWmlEPTB;MUOgcm0> NYXr[o9CRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwO|c{PTBpPkK0NFc4OzVyPD;hQi=>
COR-L279 NVP6O5N4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XTWmlEPTB;MUWgcm0> NEGwd3c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC3O|M2OCd-MkSwO|c{PTB:L3G+
LoVo MkTwSpVv[3Srb36gZZN{[Xl? MX:zNEBucW6| NYXLN2x4TUN3MDC9JFAvODB{NTFOwG0> NUHRUpNpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3OlExQTZpPkK1O|YyODl4PD;hQi=>
MX1 NX7uSXhqS3m2b4TvfIlkcXS7IHHzd4F6 M4LlV2VEPTBiPTCwMlAxODNizszN NXLlTYR6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[2OVI4OTdpPkK2OlUzPzF5PD;hQi=>
LoVo NWrMOXVQTnWwY4Tpc44h[XO|YYm= NUXoV2VTOzBibXnudy=> MWHFR|UxKD1iMD6wNFI2OSEQvF2= M2Htb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NkWyO|E4Lz5{Nk[1NlcyPzxxYU6=
LoVo MY\DfZRwfG:6aXPpeJkh[XO|YYm= MlO4NE41KHWP MnjZOUBl[Xm| M13zU2dKPTBiPTCwMlAxPCEQvF2= NELTZ4s9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nk[1NlcyPyd-Mk[2OVI4OTd:L3G+
Capan1 NXHqfok6S3m2b4TvfIlkcXS7IHHzd4F6 MkDpSWM2OCB;IECuNFA2KM7:TR?= NYjuRnlQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[2OVI4OTdpPkK2OlUzPzF5PD;hQi=>
MRC5 MYTDfZRwfG:6aXPpeJkh[XO|YYm= MoriSWM2OCB;IECuN|Eh|ryP NE\WPFA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nk[1NlcyPyd-Mk[2OVI4OTd:L3G+
MX1 NV;yUmxbTnWwY4Tpc44h[XO|YYm= M1vJRVEhdWdxa3e= NWfWeGZHOiBuODDhcoQhOjRiaILz MVnE[YNz\WG|ZTDpckBRSVJibHX2[YwhcW5iYYTofY1q[yCwdT;ueUBud3W|ZTD4[Y5w\3KjZoTl[EB4cXSqIHj1cYFvKE2[MTDj[YxteyCjdDCxJI1oN2upLDDwc{Bi\G2rbnnzeIVz\WRiYYOgd4lv\2ynIHTvd4UhdWWjc4Xy[YQh[W[2ZYKgNkAtQCCjbnSgNlQhcHK|IHL5JGVNUVOD MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjZ3MkexO{c,OjZ4NUK3NVc9N2F-
MX1 NWqx[FFbSW62aYT1cY9zKGG|c3H5 M4r4[VAvOzNibXevb4c> NWXTdmtPOjhiZHH5dy=> NFPBO|RCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBDWkODMTDk[YZq[2mnboSgbJVu[W5iTWixJINmdGy|IIjlco9oemGodHXkJIlvKGG2aIntbYMhdnVxboWgcY92e2ViYYSgNE4{OyCvZz;r[{wheG9icXSgZYRucW6rc4TldoVlKG[xcjCyPEBl[Xm| MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjZ3MkexO{c,OjZ4NUK3NVc9N2F-
MX1 NIjLXnZCdnSrdIXtc5Ih[XO|YYm= M331RVAvOTZ3IH3nM4to NF\mNo8zQCCmYYnz NXnPcYE3SW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhSlKFQUGg[IVncWOrZX70JIh2dWGwIF3YNUBk\WyuczD4[Y5w\3KjZoTl[EBqdiCjdHj5cYlkKG63L371JI1wfXOnIHHzd4V{e2WmIHHzJJR2dW:{IHfyc5d1cCCrbnjpZol1cW:wIHH0JFAvOTZ3IH3nM4toNCCybzDh[I1qdmm|dHXy[YQhfHerY3WgZUBl[XliZn;yJFI5KGSjeYO= M1jZZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NkWyO|E4Lz5{Nk[1NlcyPzxxYU6=
MX1 Mn3MSpVv[3Srb36gZZN{[Xl? MnfaNE4{OyCvZz;r[y=> MoHXVI91\W62aXH0bY9vKG:oIHPhdoJweGyjdHnuMYlv\HWlZXSgeJVud3JiZ4Lve5RpKGmwaHnibZRqd25ib3[gRnJESTFiZHXmbYNq\W62IHj1cYFvKE2[MTDj[YxteyC6ZX7v[5Ji\nSnZDDpckBifGi7bXnjJI52N263IH3veZNmKGG2IECuN|MhdWdxa3egdI8h[W6mIHHubY1idHNid3Xy[UB1emWjdHXkJJdqfGhiY3HyZo9xdGG2aX6gZZQhOzVibXevb4ctKGmyIH;uJIRigSBz Ml3rQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ4NUK3NVcoRjJ4NkWyO|E4RC:jPh?=
MDA-MB-436 M1rib2FvfGmycn;sbYZmemG2aY\lJIF{e2G7 MnHWO{Bl[Xm| MoDVTWM2OCB;IECuNFAxPyEQvF2= NHzC[IY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OE[5NlkyPid-Mki2PVI6OTZ:L3G+
Capan1 MVHBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? M33mcFch\GG7cx?= NWXaTpI5UUN3MDC9JFAvODBzODFOwG0> NH;jVpo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OE[5NlkyPid-Mki2PVI6OTZ:L3G+
VC8 MnTiR5l1d3SxeHnjbZR6KGG|c3H5 NVrIV5pUOyCmYYnz NYjoe49WUUN3MDC9JFAvODB2MjFOwG0> NFz3OIY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OE[5NlkyPid-Mki2PVI6OTZ:L3G+
V79 NWPEOFk2S3m2b4TvfIlkcXS7IHHzd4F6 Mn73N{Bl[Xm| MnG3TWM2OCB;IEWuNFEyPCEQvF2= MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDZ7MkmxOkc,Ojh4OUK5NVY9N2F-
Capan1 Mnr1SpVv[3Srb36gZZN{[Xl? MXWwMlEhfU1? MYW0JIhzew>? NFr5Xo9KdmirYnn0bY9vKG:oIGDBVnAyKGmwIFLSR2EzKGSnZnnjbYVvfCCqdX3hckBE[XCjbkGgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5kemWjc3WgbY4hWEGUUEGtSG5CKHS{YYDwbY5oKGG2IECuNUB2VSCjZoTldkA1KGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? NE\DU2g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OE[5NlkyPid-Mki2PVI6OTZ:L3G+
MDA-MB-436 NUDIeJpQTnWwY4Tpc44h[XO|YYm= MUixJJVO M{\JTlQhcHK| MXvJcohq[mm2aX;uJI9nKFCDUmCxJIlvKEKUQ1GxJIRm\mmlaXXueEBpfW2jbjDNSGEuVUJvNEO2JINmdGy|IHHzd4V{e2WmIHHzJIlv[3KnYYPlJIlvKFCDUmCxMWRPSSC2cnHwdIlv\yCjdDCxJJVOKGGodHXyJFQhcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? NUjwUXRkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki2PVI6OTZpPkK4OlkzQTF4PD;hQi=>

... 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
NCT04692662 Not yet recruiting Drug: talazoparib Solid Tumors National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) January 8 2021 Phase 2
NCT04672460 Not yet recruiting Drug: TALZENNA capsule|Drug: Talazoparib soft gel capsule Advanced Solid Tumors Pfizer December 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
NCT04134884 Recruiting Drug: Talazoparib|Drug: ASTX727 Metastatic Breast Cancer|Triple Negative Breast Cancer|Hormone Receptor Positive Tumor Kathy Miller|Pfizer|Astex Pharmaceuticals Inc.|Van Andel Institute Stand Up to Cancer Team|Indiana University March 30 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

相关PARP产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID