Talazoparib (BMN 673)

Catalog No.S7048 Synonyms: LT-673

For research use only.

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.

Talazoparib (BMN 673) Chemical Structure

CAS No. 1207456-01-6

Selleck's Talazoparib (BMN 673) has been cited by 162 publications

Purity & Quality Control

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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 NFTnUGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHVNE4yNTFyMDDuUS=> NHu5TpAzPC92OD:3NkBp M1zvNIlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvckBld3OnIHTldIVv\GWwdHz5 M1\3R|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MES3Olk4Lz5{NkC0O|Y6PzxxYU6=
BR5FVB1-Akt NG\2bmtCeG:ydH;zbZMhSXO|YYm= MnXINE4yNTFyMDDuUS=> MkfJO|IhcA>? NUHvcI15cW6mdXPld{BieG:ydH;zbZM> NEf2[WE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkC0O|Y6Pyd-Mk[wOFc3QTd:L3G+
Capan-1 NVraNlI1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTF4LkFihKnDueLCiUWuOQKBkcL3TdMg M{LVUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OE[0OVkxLz5{NUi2OFU6ODxxYU6=
MIA PaCa-2 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3BTWM2OD13OD6yN-KBkcLz4pEJPE4y6oDLwsXNxsA> M4HwSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OE[0OVkxLz5{NUi2OFU6ODxxYU6=
RD NUXISHloT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvzNIplUUN3ME24Mlchdk1? MmHWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{NkO1N|koRjJ3Mk[zOVM6RC:jPh?=
Rh41 NV\6Z2pjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4S2SmlEPTB;OD6xJI5O NIj3dpM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK2N|U{QSd-MkWyOlM2Ozl:L3G+
Rh18 MlPTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXLTWM2OD12Lkmgcm0> M1LXRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mk[zOVM6Lz5{NUK2N|U{QTxxYU6=
Rh30 NGnwOWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjuW5FmUUN3ME2zNU4yKG6P NIHVRYY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK2N|U{QSd-MkWyOlM2Ozl:L3G+
BT-12 NUTOeFV3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLsTWM2OD8kgJmxMFAxOCCwTR?= NUHFeWp4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyOlM2OzlpPkK1NlY{PTN7PD;hQi=>
CHLA-266 NVLMOWZJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnruTWM2OD8kgJmxMFAxOCCwTR?= MlnVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{NkO1N|koRjJ3Mk[zOVM6RC:jPh?=
TC-71 NXjZUItzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV6xO2FiUUN3ME2zMlchdk1? MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ4M{WzPUc,OjV{NkO1N|k9N2F-
CHLA-9 M3;zcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXLTWM2OD16LkKgcm0> MmrLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{NkO1N|koRjJ3Mk[zOVM6RC:jPh?=
CHLA-10 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LqWWlEPTB;NkeuPEBvVQ>? M2q1RlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mk[zOVM6Lz5{NUK2N|U{QTxxYU6=
CHLA-258 NXvjPG1pT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV2wdpI5UUN3ME20MlYhdk1? M1XufVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mk[zOVM6Lz5{NUK2N|U{QTxxYU6=
SJ-GBM2 NETmfWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrLPXVKSzVyPUG2MlIhdk1? NV;PRpUxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyOlM2OzlpPkK1NlY{PTN7PD;hQi=>
NB-1643 MoDFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVqyNZhrUUN3ME2xPE41KG6P NF2xWIo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK2N|U{QSd-MkWyOlM2Ozl:L3G+
NB-EBc1 NEjZToFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrxNGJKSzVyPUK1Mlghdk1? M1TZb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mk[zOVM6Lz5{NUK2N|U{QTxxYU6=
CHLA-90 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEToZ5ZKSzVyPvMAjVEtODByIH7N M3n2TlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mk[zOVM6Lz5{NUK2N|U{QTxxYU6=
CHLA-136 M3yzfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TUfmlEPTB;MUSuNkBvVQ>? M1O4VlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mk[zOVM6Lz5{NUK2N|U{QTxxYU6=
NALM-6 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NID0c4VKSzVyPUS5JI5O NWfWR4RSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyOlM2OzlpPkK1NlY{PTN7PD;hQi=>
COG-LL-317 NHj3N4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF3meWFKSzVyPUmuOEBvVQ>? MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ4M{WzPUc,OjV{NkO1N|k9N2F-
RS4;11 NFXCOpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnIUWIxUUN3ME21Nk43KG6P NX3QNYZNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyOlM2OzlpPkK1NlY{PTN7PD;hQi=>
MOLT-4 M3jiU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrZfmZDUUN3ME2xOk43KG6P MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ4M{WzPUc,OjV{NkO1N|k9N2F-
CCRF-CEM MnPyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLUTWM2OD14OUeuN{BvVQ>? NF;tNXo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK2N|U{QSd-MkWyOlM2Ozl:L3G+
Kasumi-1 NGfaUJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTd6Nj6yJI5O NVXrO3ZzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyOlM2OzlpPkK1NlY{PTN7PD;hQi=>
Karpas-299 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1XBNmlEPTB;N{WuO{BvVQ>? NF\KXog9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK2N|U{QSd-MkWyOlM2Ozl:L3G+
Ramos-RA1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3LXYg3UUN3ME22PE4{KG6P MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ4M{WzPUc,OjV{NkO1N|k9N2F-
DT40 MlTUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYPKZWRmUUN3ME20JI5O NHLqU4s9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO1OlgyOyd-MkSzOVY5OTN:L3G+
DU145 NHPkXmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTFzIH7N M3GzRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{W2PFE{Lz5{NEO1OlgyOzxxYU6=
H209 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoeyTWM2OD1zLkegcm0> NXjIVYQ6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwO|c{PTBpPkK0NFc4OzVyPD;hQi=>
H1048 NXfBT5B2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\rbYZKSzVyPUKuNkBvVQ>? MnjkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyN{ezOVAoRjJ2MEe3N|UxRC:jPh?=
H524 NIrTSXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTNwMTDuUS=> NUK0W|F3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwO|c{PTBpPkK0NFc4OzVyPD;hQi=>
H1930 NFLQZldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTRwMTDuUS=> NUL1enZRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwO|c{PTBpPkK0NFc4OzVyPD;hQi=>
H69 NFzROmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHflNXlKSzVyPUWuNkBvVQ>? NVu3N3RSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwO|c{PTBpPkK0NFc4OzVyPD;hQi=>
H2081 NWXMWoQ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFP1TVdKSzVyPU[uN{BvVQ>? MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB5N{O1NEc,OjRyN{ezOVA9N2F-
H2107 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TsPWlEPTB;Nz6zJI5O MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB5N{O1NEc,OjRyN{ezOVA9N2F-
H1092 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRThwOTDuUS=> MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB5N{O1NEc,OjRyN{ezOVA9N2F-
DMS-79 NYS1OHk4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfHVm1KSzVyPUmuN{BvVQ>? NWHpRZB7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwO|c{PTBpPkK0NFc4OzVyPD;hQi=>
H446 NYm4RnF6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTF|IH7N NXHKZlFWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwO|c{PTBpPkK0NFc4OzVyPD;hQi=>
COR-L279 M{S5NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrnOYhjUUN3ME2xOUBvVQ>? Mn;tQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyN{ezOVAoRjJ2MEe3N|UxRC:jPh?=
LoVo NX;4TlZzTnWwY4Tpc44h[XO|YYm= M4jkWVMxKG2rboO= NGPuXYdGSzVyIE2gNE4xODJ3IN88US=> NVnZR41wRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3OlExQTZpPkK1O|YyODl4PD;hQi=>
MX1 NIT4eIdEgXSxdH;4bYNqfHliYYPzZZk> MVjFR|UxKD1iMD6wNFA{KM7:TR?= MmTtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ4NUK3NVcoRjJ4NkWyO|E4RC:jPh?=
LoVo NY\P[Vg{TnWwY4Tpc44h[XO|YYm= MnHDN|AhdWmwcx?= M3;0VmVEPTBiPTCwMlAxOjVzIN88US=> NFzuPXk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nk[1NlcyPyd-Mk[2OVI4OTd:L3G+
LoVo MWfDfZRwfG:6aXPpeJkh[XO|YYm= M3rVWlAvPCC3TR?= MXu1JIRigXN? M{Di[GdKPTBiPTCwMlAxPCEQvF2= NYrFW5N5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[2OVI4OTdpPkK2OlUzPzF5PD;hQi=>
Capan1 Ml7lR5l1d3SxeHnjbZR6KGG|c3H5 NV:5WJdmTUN3MDC9JFAvODB3IN88US=> M2rKe|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NkWyO|E4Lz5{Nk[1NlcyPzxxYU6=
MRC5 M4D4ZWN6fG:2b4jpZ4l1gSCjc4PhfS=> NF\R[JJGSzVyIE2gNE4{OSEQvF2= MmSyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ4NUK3NVcoRjJ4NkWyO|E4RC:jPh?=
MX1 MXHGeY5kfGmxbjDhd5NigQ>? MmjONUBu\y:tZx?= NYroN2NvOiBuODDhcoQhOjRiaILz Mo[wSIVkemWjc3WgbY4hWEGUIHzleoVtKGmwIHH0bJlucWNiboWvcpUhdW:3c3WgfIVvd2e{YX\0[YQhf2m2aDDoeY1idiCPWEGgZ4VtdHNiYYSgNUBu\y:tZzygdI8h[WSvaX7pd5RmemWmIHHzJJNqdmeuZTDkc5NmKG2nYYP1doVlKGGodHXyJFIhNDhiYX7kJFI1KGi{czDifUBGVEmVQR?= NVfRN4VuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[2OVI4OTdpPkK2OlUzPzF5PD;hQi=>
MX1 MXnBcpRqfHWvb4KgZZN{[Xl? MVywMlM{KG2pL3vn M1HGXlI5KGSjeYO= M3PUWGFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JGJTS0FzIHTl[olkcWWwdDDoeY1idiCPWEGgZ4VtdHNieHXuc4dz[W[2ZXSgbY4h[XSqeX3pZ{BvfS:wdTDtc5V{\SCjdDCwMlM{KG2pL3vnMEBxdyCzZDDh[I1qdmm|dHXy[YQh\m:{IEK4JIRigXN? NVPjSG9SRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[2OVI4OTdpPkK2OlUzPzF5PD;hQi=>
MX1 MnmwRY51cXS3bX;yJIF{e2G7 NHrXbJIxNjF4NTDt[{9s\w>? MojnNlgh\GG7cx?= NVryOotlSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhSlKFQUGg[IVncWOrZX70JIh2dWGwIF3YNUBk\WyuczD4[Y5w\3KjZoTl[EBqdiCjdHj5cYlkKG63L371JI1wfXOnIHHzd4V{e2WmIHHzJJR2dW:{IHfyc5d1cCCrbnjpZol1cW:wIHH0JFAvOTZ3IH3nM4toNCCybzDh[I1qdmm|dHXy[YQhfHerY3WgZUBl[XliZn;yJFI5KGSjeYO= MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjZ3MkexO{c,OjZ4NUK3NVc9N2F-
MX1 NWHl[Id{TnWwY4Tpc44h[XO|YYm= MXGwMlM{KG2pL3vn M2\yNnBwfGWwdHnheIlwdiCxZjDjZZJjd3CuYYTpck1qdmS3Y3XkJJR2dW:{IHfyc5d1cCCrbnjpZol1cW:wIH;mJGJTS0FzIHTl[olkcWWwdDDoeY1idiCPWEGgZ4VtdHNieHXuc4dz[W[2ZXSgbY4h[XSqeX3pZ{BvfS:wdTDtc5V{\SCjdDCwMlM{KG2pL3vnJJBwKGGwZDDhcolu[Wy|IIfldoUhfHKnYYTl[EB4cXSqIHPhdoJweGyjdHnuJIF1KDN3IH3nM4toNCCrcDDvckBl[XliMR?= MkXWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ4NUK3NVcoRjJ4NkWyO|E4RC:jPh?=
MDA-MB-436 NFLoN2xCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MUW3JIRigXN? MWjJR|UxKD1iMD6wNFA4KM7:TR?= NIDOdXg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OE[5NlkyPid-Mki2PVI6OTZ:L3G+
Capan1 MmXhRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M2\WZ|ch\GG7cx?= MXLJR|UxKD1iMD6wNFE5KM7:TR?= MlTlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh4OUK5NVYoRjJ6NkmyPVE3RC:jPh?=
VC8 NGHjWYlEgXSxdH;4bYNqfHliYYPzZZk> Mn3zN{Bl[Xm| NGXv[mxKSzVyIE2gNE4xODR{IN88US=> NEO0V489[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OE[5NlkyPid-Mki2PVI6OTZ:L3G+
V79 NYrkTJAyS3m2b4TvfIlkcXS7IHHzd4F6 NXnlZW9UOyCmYYnz NFXETWtKSzVyIE2gOU4xOTF2IN88US=> NGK0bXU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OE[5NlkyPid-Mki2PVI6OTZ:L3G+
Capan1 MmrmSpVv[3Srb36gZZN{[Xl? MonqNE4yKHWP NXK5O4k{PCCqcoO= MUHJcohq[mm2aX;uJI9nKFCDUmCxJIlvKEKUQ1GyJIRm\mmlaXXueEBpfW2jbjDDZZBidjFiY3XscJMh[XO|ZYPz[YQh[XNiaX7jdoVie2ViaX6gVGFTWDFvRF7BJJRz[XCyaX7nJIF1KDBwMTD1UUBi\nSncjC0JIhzeyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM> NVvwXoVrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki2PVI6OTZpPkK4OlkzQTF4PD;hQi=>
MDA-MB-436 MXrGeY5kfGmxbjDhd5NigQ>? M{DVSVEhfU1? NEXsN4I1KGi{cx?= NHrENXlKdmirYnn0bY9vKG:oIGDBVnAyKGmwIFLSR2EyKGSnZnnjbYVvfCCqdX3hckBOTEFvTVKtOFM3KGOnbHzzJIF{e2W|c3XkJIF{KGmwY4LlZZNmKGmwIGDBVnAyNUSQQTD0doFxeGmwZzDheEAyKHWPIHHmeIVzKDRiaILzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?= M4LvT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NkmyPVE3Lz5{OE[5NlkyPjxxYU6=
Assay
Methods Test Index PMID
Western blot cleaved-PARP / cleaved-caspase3 / γ-H2AX ; pKAP1 / pChk2 / pChk1 ; PD-L1 ; p-ATM 29158830 28947502 28167507 30472087
Growth inhibition assay Cell viability 29158830
Immunofluorescence cleaved PARP / 53BP1 ; RAD51 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 (from reference)

Animal Research:

[2]

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

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 380.35
Formula

 

C19H14F2N6O
 
CAS No. 1207456-01-6
Storage 3 years -20°C powder
2 years -80°C in solvent
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)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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

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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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