Talazoparib (BMN 673)

For research use only.

Catalog No.S7048 Synonyms: LT-673

139 publications

Talazoparib (BMN 673) Chemical Structure

CAS No. 1207456-01-6

Talazoparib (BMN 673, LT-673) is a novel PARP inhibitor with IC50 of 0.57 nM for PARP1 in a cell-free assay. It is also a potent inhibitor of PARP-2, but does not inhibit PARG and is highly sensitive to PTEN mutation. Phase 3.

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Selleck's Talazoparib (BMN 673) has been cited by 139 publications

Purity & Quality Control

Choose Selective PARP Inhibitors

Biological Activity

Description Talazoparib (BMN 673, LT-673) is a novel PARP inhibitor with IC50 of 0.57 nM for PARP1 in a cell-free assay. It is also a potent inhibitor of PARP-2, but does not inhibit PARG and is highly sensitive to PTEN mutation. Phase 3.
Features Most potent and selective PARPi reported thus far.
Targets
PARP1 [1]
(Cell-free assay)
0.57 nM
In vitro

BMN-673 selectively binds to PARP and prevents PARP-mediated DNA repair of single strand DNA breaks via the base-excision repair pathway. This enhances the accumulation of DNA strand breaks, promotes genomic instability and eventually leads to apoptosis. BMN 673 selectively kills cancer cells with BRCA-1 or BRCA-2 mutations. BMN 673 demonstrates single-agent cytotoxicityin BRCA-1 mutant (MX-1, IC50 = 0.3 nM) and BRCA-2 mutant cells (Capan-1, IC50 = 5 nM). In contrast, in MRC-5 normal human fibroblastand other tumor cell lines with wild-type BRCA-1 and BRCA-2 genes, IC50 of BMN 673 ranges between 90 nM and 1.9 μM. [1] In cultured human cancer cells, BMN 673 also significantly enhances the cytotoxic efficacy of both Temozolomide and SN-38. Off-target molecular screening did not identify significant non-specific activity for this class of PARP inhibitors. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BR5FVB1-Akt MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;lN5l[OC5zLUGwNEBvVQ>? NUDKT2gxOjRxNEivO|IhcA>? NIj5S49qdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDk[ZBmdmSnboTsfS=> MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjB2N{[5O{c,OjZyNEe2PVc9N2F-
BR5FVB1-Akt M{WzRWFxd3C2b4Ppd{BCe3OjeR?= NHrOUXoxNjFvMUCwJI5O NHPJV4Y4OiCq MnXBbY5lfWOnczDhdI9xfG:|aYO= MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjB2N{[5O{c,OjZyNEe2PVc9N2F-
Capan-1 MnPZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTF4LkFihKnDueLCiUWuOQKBkcL3TdMg MlH3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6NkS1PVAoRjJ3OE[0OVkxRC:jPh?=
MIA PaCa-2 M4T0PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTJR|UxRTV6LkKz5qCKyrIkgJm4MlHjiIoEtV5CpC=> MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh4NEW5NEc,OjV6NkS1PVA9N2F-
RD M{LvfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvLcHhIUUN3ME24Mlchdk1? MnGzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{NkO1N|koRjJ3Mk[zOVM6RC:jPh?=
Rh41 MlH1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\0[3ZRUUN3ME24MlEhdk1? NWXkZlJLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyOlM2OzlpPkK1NlY{PTN7PD;hQi=>
Rh18 MonFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUiyb|U5UUN3ME20Mlkhdk1? NEf6Z2M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK2N|U{QSd-MkWyOlM2Ozl:L3G+
Rh30 Mnn4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTNzLkGgcm0> NIPrTJQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK2N|U{QSd-MkWyOlM2Ozl:L3G+
BT-12 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRuLCiUGsNFAxKG6P MmL1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{NkO1N|koRjJ3Mk[zOVM6RC:jPh?=
CHLA-266 NHvaeJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRuLCiUGsNFAxKG6P NGPIfWI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK2N|U{QSd-MkWyOlM2Ozl:L3G+
TC-71 NG\uU4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M16xRmlEPTB;Mz63JI5O M33iVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mk[zOVM6Lz5{NUK2N|U{QTxxYU6=
CHLA-9 NUPWNmRIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjabZF2UUN3ME24MlIhdk1? M1HPbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mk[zOVM6Lz5{NUK2N|U{QTxxYU6=
CHLA-10 M3f4emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXnWFRsUUN3ME22O{45KG6P M{D6OFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mk[zOVM6Lz5{NUK2N|U{QTxxYU6=
CHLA-258 NH:wTnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIqyXoZKSzVyPUSuOkBvVQ>? M3fiTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mk[zOVM6Lz5{NUK2N|U{QTxxYU6=
SJ-GBM2 MofnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\VTWM2OD1zNj6yJI5O NXLmcJdTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyOlM2OzlpPkK1NlY{PTN7PD;hQi=>
NB-1643 NHLsVlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTF6LkSgcm0> NYGxWIVCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyOlM2OzlpPkK1NlY{PTN7PD;hQi=>
NB-EBc1 NV:3d|BST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1r6cGlEPTB;MkWuPEBvVQ>? M2jjeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mk[zOVM6Lz5{NUK2N|U{QTxxYU6=
CHLA-90 NFvu[ppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDQUYs6UUN3ME9ihKkyNDByMDDuUS=> M4P6VFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mk[zOVM6Lz5{NUK2N|U{QTxxYU6=
CHLA-136 Ml\ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYW2[HdSUUN3ME2xOE4zKG6P MkXKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{NkO1N|koRjJ3Mk[zOVM6RC:jPh?=
NALM-6 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LYOWlEPTB;NEmgcm0> MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ4M{WzPUc,OjV{NkO1N|k9N2F-
COG-LL-317 NHzmfVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTlwNDDuUS=> NHHhc5I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK2N|U{QSd-MkWyOlM2Ozl:L3G+
RS4;11 MonHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPKTWM2OD13Mj62JI5O MoPEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{NkO1N|koRjJ3Mk[zOVM6RC:jPh?=
MOLT-4 NEC5N2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFraS4FKSzVyPUG2MlYhdk1? M4rCc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mk[zOVM6Lz5{NUK2N|U{QTxxYU6=
CCRF-CEM NVfDUXFUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHqe4FKSzVyPU[5O{4{KG6P NInaZWo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK2N|U{QSd-MkWyOlM2Ozl:L3G+
Kasumi-1 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXzbplvUUN3ME23PFYvOiCwTR?= MnnrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{NkO1N|koRjJ3Mk[zOVM6RC:jPh?=
Karpas-299 NV7G[Wd5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\NXHhKSzVyPUe1Mlchdk1? NFTV[nI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK2N|U{QSd-MkWyOlM2Ozl:L3G+
Ramos-RA1 M4exT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2S5OmlEPTB;NkiuN{BvVQ>? MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ4M{WzPUc,OjV{NkO1N|k9N2F-
DT40 MmThS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LIdmlEPTB;NDDuUS=> M2PkeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{W2PFE{Lz5{NEO1OlgyOzxxYU6=
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H1048 NXjPXWxLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRTJwMjDuUS=> NYHaVZoxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwO|c{PTBpPkK0NFc4OzVyPD;hQi=>
H524 NXLSTYNyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;yTWM2OD1|LkGgcm0> NFK0[Ww9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC3O|M2OCd-MkSwO|c{PTB:L3G+
H1930 NYfadnJsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTRwMTDuUS=> MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB5N{O1NEc,OjRyN{ezOVA9N2F-
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H2081 MmjOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrU[4dGUUN3ME22MlMhdk1? NXixW5Z[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwO|c{PTBpPkK0NFc4OzVyPD;hQi=>
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DMS-79 MnHoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDPXJptUUN3ME25MlMhdk1? NIDEV5Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC3O|M2OCd-MkSwO|c{PTB:L3G+
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MX1 NHe5UJFCdnSrdIXtc5Ih[XO|YYm= MlnHNE4{OyCvZz;r[y=> MkX3Nlgh\GG7cx?= MXnBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDCVmNCOSCmZX\pZ4lmdnRiaIXtZY4hVVhzIHPlcIx{KHinbn;ndoFnfGWmIHnuJIF1cHmvaXOgcpUwdnVibX;1d4Uh[XRiMD6zN{Bu\y:tZzygdI8heWRiYXTtbY5qe3SncnXkJIZweiB{ODDkZZl{ M3WwcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NkWyO|E4Lz5{Nk[1NlcyPzxxYU6=
MX1 Ml7hRY51cXS3bX;yJIF{e2G7 MkfONE4yPjVibXevb4c> M1nDTFI5KGSjeYO= M125PGFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JGJTS0FzIHTl[olkcWWwdDDoeY1idiCPWEGgZ4VtdHNieHXuc4dz[W[2ZXSgbY4h[XSqeX3pZ{BvfS:wdTDtc5V{\SCjc4Pld5Nm\CCjczD0eY1weiCpcn;3eIghcW6qaXLpeIlwdiCjdDCwMlE3PSCvZz;r[{wheG9iYXTtbY5qe3SncnXkJJR4cWOnIHGg[IF6KG[xcjCyPEBl[Xm| NVG5TI1LRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[2OVI4OTdpPkK2OlUzPzF5PD;hQi=>
MX1 NH7PVYlHfW6ldHnvckBie3OjeR?= MXywMlM{KG2pL3vn Ml7SVI91\W62aXH0bY9vKG:oIHPhdoJweGyjdHnuMYlv\HWlZXSgeJVud3JiZ4Lve5RpKGmwaHnibZRqd25ib3[gRnJESTFiZHXmbYNq\W62IHj1cYFvKE2[MTDj[YxteyC6ZX7v[5Ji\nSnZDDpckBifGi7bXnjJI52N263IH3veZNmKGG2IECuN|MhdWdxa3egdI8h[W6mIHHubY1idHNid3Xy[UB1emWjdHXkJJdqfGhiY3HyZo9xdGG2aX6gZZQhOzVibXevb4ctKGmyIH;uJIRigSBz MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjZ3MkexO{c,OjZ4NUK3NVc9N2F-
MDA-MB-436 MmfMRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MWm3JIRigXN? MonzTWM2OCB;IECuNFAxPyEQvF2= M3PCT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NkmyPVE3Lz5{OE[5NlkyPjxxYU6=
Capan1 MUDBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MXG3JIRigXN? NHzIXVJKSzVyIE2gNE4xODF6IN88US=> MoLlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh4OUK5NVYoRjJ6NkmyPVE3RC:jPh?=
VC8 MXvDfZRwfG:6aXPpeJkh[XO|YYm= MXmzJIRigXN? M2X2Z2lEPTBiPTCwMlAxPDJizszN MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDZ7MkmxOkc,Ojh4OUK5NVY9N2F-
V79 NW\5XnBTS3m2b4TvfIlkcXS7IHHzd4F6 MYWzJIRigXN? NHzUVGtKSzVyIE2gOU4xOTF2IN88US=> MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDZ7MkmxOkc,Ojh4OUK5NVY9N2F-
Capan1 NEX4TZhHfW6ldHnvckBie3OjeR?= MWKwMlEhfU1? M2ewb|QhcHK| NV\hdHdtUW6qaXLpeIlwdiCxZjDQRXJROSCrbjDCVmNCOiCmZX\pZ4lmdnRiaIXtZY4hS2GyYX6xJINmdGy|IHHzd4V{e2WmIHHzJIlv[3KnYYPlJIlvKFCDUmCxMWRPSSC2cnHwdIlv\yCjdDCwMlEhfU1iYX\0[ZIhPCCqcoOgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m| MnK5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh4OUK5NVYoRjJ6NkmyPVE3RC:jPh?=
MDA-MB-436 M{[wTmZ2dmO2aX;uJIF{e2G7 MlWyNUB2VQ>? NIO3WVA1KGi{cx?= MWTJcohq[mm2aX;uJI9nKFCDUmCxJIlvKEKUQ1GxJIRm\mmlaXXueEBpfW2jbjDNSGEuVUJvNEO2JINmdGy|IHHzd4V{e2WmIHHzJIlv[3KnYYPlJIlvKFCDUmCxMWRPSSC2cnHwdIlv\yCjdDCxJJVOKGGodHXyJFQhcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? NUL4b3E6RGFidHHy[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
In vivo In rat pharmacokinetic studies, BMN 673 displays >50% oralbioavailability and pharmacokinetic properties that enable singledaily dosing. In MX-1 xenograft tumor model studies, daily oral dosingof BMN 673 significantly enhances the antitumor effects ofcytotoxic therapies in a dose-dependent manner. [2]

Protocol

Animal Research:

[2]

- Collapse
  • Animal Models: MX-1 model (BRCA-1 deficient)
  • Dosages: 0.33 mg/kg/day, once daily
  • Administration: Oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 38 mg/mL warmed (99.9 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 380.35
Formula

 

C19H14F2N6O
 
CAS No. 1207456-01-6
Storage powder
in solvent
Synonyms LT-673
Smiles CN1C(=NC=N1)C2C(NC3=CC(=CC4=C3C2=NNC4=O)F)C5=CC=C(C=C5)F

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
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Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • 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):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

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

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Frequently Asked Questions

  • Question 1:

    Which solvent do you recommend to dilute the inhibitor for in vivo study in mice?

  • Answer:

    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