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
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127篇：

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Sci Rep, 2020, 10(1):14253

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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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Transl Oncol, 2020, 13(11):100834

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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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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

PubMed: 31273204 ( click the link to review the publication )

Nucleic Acids Res, 2019, 47(11):5634-5647

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J Thorac Oncol, 2019, 14(10):1743-1752

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Clin Cancer Res, 2019, 10.1158/1078-0432

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EMBO Rep, 2019, 20(5)

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Theranostics, 2019, 9(21):6224-6238

PubMed: 31534547 ( click the link to review the publication )

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

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J Med Chem, 2019, 62(11):5330-5357

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Cancers (Basel), 2019, 11(10)

PubMed: 31623402 ( click the link to review the publication )

Cancers (Basel), 2019, 11(12)

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

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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Int J Biol Sci, 2019, 15(9):1942-1954

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Biochem Biophys Res Commun, 2019, 510(4):501-507

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Leuk Lymphoma, 2019, 60(4):1098-1101

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AMB Express, 2019, 9(1):108

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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

PubMed: 29547717 ( click the link to review the publication )

J Clin Invest, 2018, 128(7):2951-2965

PubMed: 29649003 ( click the link to review the publication )

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

PubMed: 30088474 ( click the link to review the publication )

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

PubMed: 29898896 ( click the link to review the publication )

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

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Cancer Chemother Pharmacol, 2018, 81(2):255-267

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SLAS Discov, 2018, 23(6):545-553

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Anticancer Res, 2018, 38(8):4493-4503

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Oncotarget, 2018, 9(4):4647-4660

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J Clin Invest, 2017, 127(6):2392-2406

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Sci Adv, 2017, 3(4):e1600957

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Clin Cancer Res, 2017, 23(14):3711-3720

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NPJ Breast Cancer, 2017, 3

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Nat Commun, 2016, 7:13837

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Oncotarget, 2016, 7(40):65157-65170

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Nat Commun, 2015, 6:8940

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Mol Cancer Ther, 2015, 14(12):2818-30

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DNA Repair , 2015, 10.1016/j.dnarep.2015.02.004

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Front Microbiol, 2015, 6:878

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Mol Cell Biol, 2015, 35(23):3934-44

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Cancer Discov, 2015, 5(7):752-67

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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	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 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 2020-01-06)

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。

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127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 2020-01-06)

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