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157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 MmK2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1r1XFAvOS1zMECgcm0> NX;4RWlmOjRxNEivO|IhcA>? NWHUUnFVcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> MlrTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZyNEe2PVcoRjJ4MES3Olk4RC:jPh?=
BR5FVB1-Akt NXvMO5o5SXCxcITvd4l{KEG|c3H5 NF;HNW8xNjFvMUCwJI5O MVi3NkBp NUTt[2x4cW6mdXPld{BieG:ydH;zbZM> MoPDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZyNEe2PVcoRjJ4MES3Olk4RC:jPh?=
Capan-1 NVvKfYltT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{nlVWlEPTB;MU[uNQKBkcLz4pEJOU416oDLwsXNxsA> Mn65QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6NkS1PVAoRjJ3OE[0OVkxRC:jPh?=
MIA PaCa-2 MlXaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPhRlZKSzVyPUW4MlI{6oDLwsJihKk5NjIkgJpCuW3DqA>? MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh4NEW5NEc,OjV6NkS1PVA9N2F-
RD Mny2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDCXJlKSzVyPUiuO{BvVQ>? NEX2XJQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK2N|U{QSd-MkWyOlM2Ozl:L3G+
Rh41 NH3aUlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnoTWM2OD16LkGgcm0> MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ4M{WzPUc,OjV{NkO1N|k9N2F-
Rh18 NF;GSldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nIW2lEPTB;ND65JI5O M2HQZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mk[zOVM6Lz5{NUK2N|U{QTxxYU6=
Rh30 M1zhXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPtTWM2OD1|MT6xJI5O NIH5WY49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK2N|U{QSd-MkWyOlM2Ozl:L3G+
BT-12 NFLR[2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXrQRZV3UUN3ME9ihKkyNDByMDDuUS=> MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ4M{WzPUc,OjV{NkO1N|k9N2F-
CHLA-266 MoPBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkO0TWM2OD8kgJmxMFAxOCCwTR?= NV[1dmUyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyOlM2OzlpPkK1NlY{PTN7PD;hQi=>
TC-71 NYi1WHJ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnYRld7UUN3ME2zMlchdk1? Mn7PQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{NkO1N|koRjJ3Mk[zOVM6RC:jPh?=
CHLA-9 NVXtdFV4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjnWVJKSzVyPUiuNkBvVQ>? NWjLPYFZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyOlM2OzlpPkK1NlY{PTN7PD;hQi=>
CHLA-10 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\SRW15UUN3ME22O{45KG6P Ml\lQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{NkO1N|koRjJ3Mk[zOVM6RC:jPh?=
CHLA-258 NH;XO|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlf5TWM2OD12Lk[gcm0> MoTSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{NkO1N|koRjJ3Mk[zOVM6RC:jPh?=
SJ-GBM2 NVz1N2tMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoX5TWM2OD1zNj6yJI5O NGPwbpk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK2N|U{QSd-MkWyOlM2Ozl:L3G+
NB-1643 NXnaN4d4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTF6LkSgcm0> NEXYZXE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK2N|U{QSd-MkWyOlM2Ozl:L3G+
NB-EBc1 M3zNZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vYVGlEPTB;MkWuPEBvVQ>? NHO3S3A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK2N|U{QSd-MkWyOlM2Ozl:L3G+
CHLA-90 NGTrNmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3LKe2lEPTB-4pEJNUwxODBibl2= M4LjWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mk[zOVM6Lz5{NUK2N|U{QTxxYU6=
CHLA-136 MlizS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjXTWM2OD1zND6yJI5O Mln5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{NkO1N|koRjJ3Mk[zOVM6RC:jPh?=
NALM-6 M{jVd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTR7IH7N MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ4M{WzPUc,OjV{NkO1N|k9N2F-
COG-LL-317 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTlwNDDuUS=> NFGzUHk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK2N|U{QSd-MkWyOlM2Ozl:L3G+
RS4;11 NUCyNZhIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFrDfJFKSzVyPUWyMlYhdk1? NGXrXVM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK2N|U{QSd-MkWyOlM2Ozl:L3G+
MOLT-4 NWruXJd4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;ySWlEPTB;MU[uOkBvVQ>? NY\qZWM4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyOlM2OzlpPkK1NlY{PTN7PD;hQi=>
CCRF-CEM NYrKfHBwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LlfWlEPTB;Nkm3MlMhdk1? MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ4M{WzPUc,OjV{NkO1N|k9N2F-
Kasumi-1 NUTFNHFlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLTb2c3UUN3ME23PFYvOiCwTR?= NXTzbm96RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyOlM2OzlpPkK1NlY{PTN7PD;hQi=>
Karpas-299 MljwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfPbJJKSzVyPUe1Mlchdk1? NEPqW2E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK2N|U{QSd-MkWyOlM2Ozl:L3G+
Ramos-RA1 NVn0dVdzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHHS4pKSzVyPU[4MlMhdk1? NUTUemlJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyOlM2OzlpPkK1NlY{PTN7PD;hQi=>
DT40 NFWyUXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTRibl2= MmjxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NU[4NVMoRjJ2M{W2PFE{RC:jPh?=
DU145 NHnrOWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;NOnZKSzVyPUGxJI5O NITDfm89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO1OlgyOyd-MkSzOVY5OTN:L3G+
H209 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTFwNzDuUS=> NF;BOlY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC3O|M2OCd-MkSwO|c{PTB:L3G+
H1048 M2\4bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzvT5BKSzVyPUKuNkBvVQ>? MlnrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyN{ezOVAoRjJ2MEe3N|UxRC:jPh?=
H524 NEXWXINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TmZ2lEPTB;Mz6xJI5O NFXPZ3Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC3O|M2OCd-MkSwO|c{PTB:L3G+
H1930 M3PJUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2DsemlEPTB;ND6xJI5O MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB5N{O1NEc,OjRyN{ezOVA9N2F-
H69 M1KxPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fFfWlEPTB;NT6yJI5O MmXMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyN{ezOVAoRjJ2MEe3N|UxRC:jPh?=
H2081 M3jMfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LGdGlEPTB;Nj6zJI5O NIr3WYY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC3O|M2OCd-MkSwO|c{PTB:L3G+
H2107 MnvOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTdwMzDuUS=> NHTrUlE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC3O|M2OCd-MkSwO|c{PTB:L3G+
H1092 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LB[mlEPTB;OD65JI5O MmrOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyN{ezOVAoRjJ2MEe3N|UxRC:jPh?=
DMS-79 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWX2[FdtUUN3ME25MlMhdk1? MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB5N{O1NEc,OjRyN{ezOVA9N2F-
H446 NHnuTVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDjb5BKSzVyPUGzJI5O NF;ydpU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC3O|M2OCd-MkSwO|c{PTB:L3G+
COR-L279 MoTkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDHTWM2OD1zNTDuUS=> MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB5N{O1NEc,OjRyN{ezOVA9N2F-
LoVo NHrh[GdHfW6ldHnvckBie3OjeR?= NFrXb4E{OCCvaX7z MkDOSWM2OCB;IECuNFAzPSEQvF2= NYDhc48zRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3OlExQTZpPkK1O|YyODl4PD;hQi=>
MX1 NYLSbGZkS3m2b4TvfIlkcXS7IHHzd4F6 NGTYcJZGSzVyIE2gNE4xODB|IN88US=> NG[1OYk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nk[1NlcyPyd-Mk[2OVI4OTd:L3G+
LoVo M2jEdWZ2dmO2aX;uJIF{e2G7 NWjpRY9QOzBibXnudy=> MWnFR|UxKD1iMD6wNFI2OSEQvF2= NGCzZYQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nk[1NlcyPyd-Mk[2OVI4OTd:L3G+
LoVo MorJR5l1d3SxeHnjbZR6KGG|c3H5 NUfNWmtsOC52IIXN MVG1JIRigXN? MonNS2k2OCB;IECuNFA1KM7:TR?= M3\SeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NkWyO|E4Lz5{Nk[1NlcyPzxxYU6=
Capan1 NYPmcVYzS3m2b4TvfIlkcXS7IHHzd4F6 MnmzSWM2OCB;IECuNFA2KM7:TR?= NFPXfJA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nk[1NlcyPyd-Mk[2OVI4OTd:L3G+
MRC5 M3j3OWN6fG:2b4jpZ4l1gSCjc4PhfS=> MWrFR|UxKD1iMD6zNUDPxE1? NF3uRlU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nk[1NlcyPyd-Mk[2OVI4OTd:L3G+
MX1 M{[1OGZ2dmO2aX;uJIF{e2G7 M{fKT|EhdWdxa3e= NHHQR2UzKCx6IHHu[EAzPCCqcoO= MYTE[YNz\WG|ZTDpckBRSVJibHX2[YwhcW5iYYTofY1q[yCwdT;ueUBud3W|ZTD4[Y5w\3KjZoTl[EB4cXSqIHj1cYFvKE2[MTDj[YxteyCjdDCxJI1oN2upLDDwc{Bi\G2rbnnzeIVz\WRiYYOgd4lv\2ynIHTvd4UhdWWjc4Xy[YQh[W[2ZYKgNkAtQCCjbnSgNlQhcHK|IHL5JGVNUVOD NUDmXIFDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[2OVI4OTdpPkK2OlUzPzF5PD;hQi=>
MX1 NWPu[ZBJSW62aYT1cY9zKGG|c3H5 NU\SRYR4OC5|MzDt[{9s\w>? Mm[zNlgh\GG7cx?= NFnLdmtCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBDWkODMTDk[YZq[2mnboSgbJVu[W5iTWixJINmdGy|IIjlco9oemGodHXkJIlvKGG2aIntbYMhdnVxboWgcY92e2ViYYSgNE4{OyCvZz;r[{wheG9icXSgZYRucW6rc4TldoVlKG[xcjCyPEBl[Xm| NVS2NoFHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[2OVI4OTdpPkK2OlUzPzF5PD;hQi=>
MX1 MUjBcpRqfHWvb4KgZZN{[Xl? M{XWVlAvOTZ3IH3nM4to NXLMNWxMOjhiZHH5dy=> MWTBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDCVmNCOSCmZX\pZ4lmdnRiaIXtZY4hVVhzIHPlcIx{KHinbn;ndoFnfGWmIHnuJIF1cHmvaXOgcpUwdnVibX;1d4Uh[XO|ZYPz[YQh[XNidIXtc5Ih\3Kxd4ToJIlvcGmkaYTpc44h[XRiMD6xOlUhdWdxa3esJJBwKGGmbXnubZN1\XKnZDD0e4lk\SCjIHThfUBnd3JiMkig[IF6ew>? M{f1PFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NkWyO|E4Lz5{Nk[1NlcyPzxxYU6=
MX1 M{LWb2Z2dmO2aX;uJIF{e2G7 NFLY[mUxNjN|IH3nM4to MV3Qc5RmdnSrYYTpc44hd2ZiY3HyZo9xdGG2aX6tbY5lfWOnZDD0eY1weiCpcn;3eIghcW6qaXLpeIlwdiCxZjDCVmNCOSCmZX\pZ4lmdnRiaIXtZY4hVVhzIHPlcIx{KHinbn;ndoFnfGWmIHnuJIF1cHmvaXOgcpUwdnVibX;1d4Uh[XRiMD6zN{Bu\y:tZzDwc{BidmRiYX7pcYFteyC5ZYLlJJRz\WG2ZXSge4l1cCClYYLic5Bt[XSrbjDheEA{PSCvZz;r[{whcXBib36g[IF6KDF? NF\K[lU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nk[1NlcyPyd-Mk[2OVI4OTd:L3G+
MDA-MB-436 NXy5OGhISW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M1LpXlch\GG7cx?= M1LnPGlEPTBiPTCwMlAxODdizszN NXuxZ2lZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki2PVI6OTZpPkK4OlkzQTF4PD;hQi=>
Capan1 MVvBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MlnWO{Bl[Xm| MkD1TWM2OCB;IECuNFAyQCEQvF2= MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDZ7MkmxOkc,Ojh4OUK5NVY9N2F-
VC8 NV\HXXh5S3m2b4TvfIlkcXS7IHHzd4F6 MVOzJIRigXN? MYTJR|UxKD1iMD6wNFQzKM7:TR?= NILEOVU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OE[5NlkyPid-Mki2PVI6OTZ:L3G+
V79 MWjDfZRwfG:6aXPpeJkh[XO|YYm= Mn;LN{Bl[Xm| MlLxTWM2OCB;IEWuNFEyPCEQvF2= NGWwem49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OE[5NlkyPid-Mki2PVI6OTZ:L3G+
Capan1 M{fkZ2Z2dmO2aX;uJIF{e2G7 NELHXm0xNjFidV2= M3XITVQhcHK| M4PYeGlvcGmkaYTpc44hd2ZiUFHSVFEhcW5iQmLDRVIh\GWoaXPp[Y51KGi3bXHuJGNieGGwMTDj[YxteyCjc4Pld5Nm\CCjczDpcoNz\WG|ZTDpckBRSVKSMT3EUmEhfHKjcIDpcoch[XRiMD6xJJVOKGGodHXyJFQhcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? M1vJb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NkmyPVE3Lz5{OE[5NlkyPjxxYU6=
MDA-MB-436 MX\GeY5kfGmxbjDhd5NigQ>? NX7QTWN1OSC3TR?= MWW0JIhzew>? NYrJTGxYUW6qaXLpeIlwdiCxZjDQRXJROSCrbjDCVmNCOSCmZX\pZ4lmdnRiaIXtZY4hVUSDLV3CMVQ{PiClZXzsd{Bie3Onc4Pl[EBieyCrbnPy[YF{\SCrbjDQRXJROS2GTlGgeJJieHCrbnegZZQhOSC3TTDh[pRmeiB2IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= M1rqelxiKHSjcnfleF0oZ2KuYX7rK{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
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

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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"

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID