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157篇：

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Cancers (Basel), 2020, 12(11)E3205

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Sci Rep, 2020, 10(1):14253

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Sci Rep, 2020, 10(1):20210

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Sci Rep, 2020, 17;10(1):2585

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Front Pharmacol, 2020, 11:610205

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Biochemistry, 2020, 10.1021/acs.biochem.0c00256

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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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Am J Cancer Res, 2020, 10(2):648-661

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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 Commun, 2019, 10(1):2954

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PubMed: 31810230 ( click the link to review the publication )

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EMBO J, 2018, 37(14)

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

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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	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 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、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

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
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 2022-01-17)

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

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.
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.

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157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 2022-01-17)

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