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
10mg	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：

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Front Pharmacol, 2020, 11:610205

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JCI Insight, 2020, 142149

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Nat Biotechnol, 2020, 10.1038/s41587-020-0600-6

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Commun Biol, 2020, 3(1):388

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Int J Cancer, 2020, 147(4):1059-1070

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Sci Signal, 2020, 13(645):eaba8091

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Mol Cell, 2020, 80(5):862-875.e6

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CU Digital Repository, 2020, N/A

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Oncotarget, 2020, 11(23):2141-2159

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BMC Cancer, 2020, 20(1):775

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Cell Rep, 2020, 32(5):107985

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Nat Commun, 2019, 10(1):2189

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Nat Commun, 2019, 10(1):2910

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J Clin Invest, 2019, 129(3):1211-1228

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Nat Chem Biol, 2019, 15(12):1223-1231

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Nat Commun, 2019, 10(1):2954

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Cancer Res, 2019, 79(2):311-319

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Cancers (Basel), 2019, 11(10)

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Cancers (Basel), 2019, 11(12)

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Cell Death Discov, 2019, 5:127

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Cell Death Dis, 2019, 10(4):281

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Front Oncol, 2019, 9:353

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Cancer Immunol Res, 2019,

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J Biochem Mol Toxicol, 2019, 33(5):e22286

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Mol Cell, 2018, 69(6):1046-1061

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Nat Commun, 2018, 9(1):2678

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Nat Commun, 2018, 9(1):3982

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Nat Commun, 2018, 9(1):1849

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Nat Commun, 2018, 9(1):176

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EMBO J, 2018, 37(14)

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Clin Cancer Res, 2018, 24(7):1705-1715

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Cell Rep, 2018, 23(11):3127-3136

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Elife, 2018, 7

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Mol Cancer Ther, 2018, 17(9):1995-2003

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Am J Cancer Res, 2018, 8(9):1837-1846

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NPJ Breast Cancer, 2017, 3

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产品安全说明书

PARP抑制剂选择性比较

生物活性

产品描述

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	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 Theranostics 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 Mol Cancer Ther 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 Clin Cancer Res 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 EBioMedicine 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 Theranostics Measured dose response curve and IC50 of Talazoparib in W780 and W0069 cells.	29158830
Immunofluorescence	cleaved PARP / 53BP1; PubMed: 28958991 Mol Cancer Ther 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 Cancers (Basel) (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]

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)

参考文献

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	3年-20°C 粉状 2年-80°C 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

每只动物给药体积

动物数量

只

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，注：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：取 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。

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。

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

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
初始浓度:
稀释倍数:

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

通过输入化合物的化学式来计算其分子量：

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 (data from https://clinicaltrials.gov, updated on 2021-05-17)

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。

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

选择性强的PARP抑制剂

AG-14361 : PARP1-selective, K_i<5 nM.
选择性强的PARP抑制剂

UPF 1069 : PARP2-selective, IC50=0.3 μM.
活性最高的PARP抑制剂

MK-4827 (Niraparib) : PARP1, IC50=3.8 nM; PARP2, IC50=2.1 nM.
用于临床的PARP抑制剂

Iniparib (BSI-201) : Phase III for solid tumors.
最新的PARP抑制剂

PJ34 HCl ^New : PARP inhibitor with EC50 of 20 nM and is equally potent to PARP1/2.

研究领域

产品类型

定制您的化合物库

Talazoparib (BMN 673)

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

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)

参考文献

溶解度 (25°C)

化学数据

动物体内配方计算器 (澄清溶液)

计算器

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

稀释计算器

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

连续稀释计算器方程

连续稀释

计算结果

分子量计算器

总分子量：g/mol

摩尔浓度计算器

临床试验信息 (data from https://clinicaltrials.gov, updated on 2021-05-17)

技术支持

常见问题及建议解决方法

PARP Signaling Pathway Map

PARP Inhibitors with Unique Features

相关PARP产品