Talazoparib (BMN 673)

Catalog No.S7048 Synonyms: LT-673

Talazoparib (BMN 673) Chemical Structure

Molecular Weight(MW): 380.35

Talazoparib (BMN 673) is a novel PARP inhibitor with IC50 of 0.58 nM 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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4 Customer Reviews

  • Western blot assessment of effects on PAR, PARP, and dsDNA breaks mediated by IMMU-132 plus PARPi in TNBC tumor lines. Cells were plated overnight in 6-well plates before the addition of chemotherapeutics. After a 24-hour incubation, cells were harvested and cell lysates resolved and transferred for Western analysis as described in Materials and Methods. PAR and FL-PARP levels were determined on the same gel. Assessment of dsDNA breaks (p-H2A.X) was calculated as ratios relative to untreated control (Unt) normalized to b-actin protein loading control (Dp-H2A.X). B, HCC1806 cells exposed to rucaparib (Ruc) and IMMU-132 or to (C) talazoparib (Tala) and IMMU-132.

    Clin Cancer Res, 2017. Talazoparib (BMN 673) purchased from Selleck.

    PARP inhibition prevents adhesion to and migration of monocytes across BMVEC monolayers preserving the barrier. Primary human monocytes were treated for 24 h with PARPi (AIQ, olaparib, EB47, talazoparib), calcein-labeled, washed, and then added to BMVEC monolayers (untreated or treated for 24 h with TNFα). Treatments were removed prior to the addition of monocytes. Adhesion to (a) and migration of (b) monocytes across blood-brain barrier models were measured and are presented as fold difference compared to TNFα-only control (mean ± SEM) for each treatment from at least quadruplicate determinations, which was assigned a value of 1 (7600 relative fluorescent units for adhesion or equivalent to 37 migrated cells). *P < 0.05, **P < 0.01 indicate significance vs. non-treated. TEER, an indicator of barrier integrity, was continuously measured in BMVEC monolayers treated with or without TNFα following the addition of primary human monocytes that had been treated with PARPi.

    J Neuroinflammation, 2016, 13(1):254.. Talazoparib (BMN 673) purchased from Selleck.

  • BT-549 cells reconstituted with Vet, WT, 336* or PTEN WT HP1aKD were treated with BMN673. Relative cell viability was determined by MTT assay. The results were presented as mean of 3 independent experiments. Error bars indicate s.d.

    Cell Cycle, 2015, 14(14): 2323-32. Talazoparib (BMN 673) purchased from Selleck.

    We treated the FA defective and control lung cancer cell lines H1299D2-down/H1299E and A549D2 down/A549E with BMN673 (0.5 µM). MTT assay was used for the cell viability analysis and an averaged absorbance was recorded 24, 48 and 72 h post treatment.

    Front Oncol, 2014, 4: 368. Talazoparib (BMN 673) purchased from Selleck.

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Biological Activity

Description Talazoparib (BMN 673) is a novel PARP inhibitor with IC50 of 0.58 nM 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
PARP [1]
(Cell-free assay)
0.58 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 M2PjTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\LdlUxNjFvMUCwJI5O MljtNlQwPDhxN{KgbC=> M2nJ[IlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvckBld3OnIHTldIVv\GWwdHz5 MViyOlA1PzZ7Nx?=
BR5FVB1-Akt M3XSWWFxd3C2b4Ppd{BCe3OjeR?= M2XqclAvOS1zMECgcm0> NXHJPJcyPzJiaB?= MVTpcoR2[2W|IHHwc5B1d3Orcx?= NH61WlAzPjB2N{[5Oy=>
Capan-1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;zRWlEPTB;MU[uNQKBkcLz4pEJOU416oDLwsXNxsA> NWi2fFNwOjV6NkS1PVA>
MIA PaCa-2 MkPyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;vTXhsUUN3ME21PE4zO+LCidMx5qCKQC5z4pEJxtVOyqB? NXO2UJFYOjV6NkS1PVA>
RD NF3KS|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRThwNzDuUS=> Mmn0NlUzPjN3M{m=
Rh41 NHHvdIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTVOXZNUUN3ME24MlEhdk1? Mn3ONlUzPjN3M{m=
Rh18 NFP1OIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;ZTWM2OD12Lkmgcm0> MV2yOVI3OzV|OR?=
Rh30 NXrRUWVyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTNzLkGgcm0> NWPkZ5JGOjV{NkO1N|k>
BT-12 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjkS3VSUUN3ME9ihKkyNDByMDDuUS=> MV[yOVI3OzV|OR?=
CHLA-266 NEL6V2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH[3V3lKSzVyPvMAjVEtODByIH7N M1\ndFI2OjZ|NUO5
TC-71 NVPZSYhrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3y2e2lEPTB;Mz63JI5O NHfTSWgzPTJ4M{WzPS=>
CHLA-9 NFjlc4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH64[pdKSzVyPUiuNkBvVQ>? NGPrXnIzPTJ4M{WzPS=>
CHLA-10 MoXPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTZ5Lkigcm0> NWPFeIxoOjV{NkO1N|k>
CHLA-258 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTRwNjDuUS=> M1TmeVI2OjZ|NUO5
SJ-GBM2 NUfqRnN{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFnwemdKSzVyPUG2MlIhdk1? NVPnV21FOjV{NkO1N|k>
NB-1643 NXjIVnBrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTOPXVKSzVyPUG4MlQhdk1? MXSyOVI3OzV|OR?=
NB-EBc1 M3m1Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlv5TWM2OD1{NT64JI5O MWKyOVI3OzV|OR?=
CHLA-90 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTZeIFKSzVyPvMAjVEtODByIH7N NHXTdG8zPTJ4M{WzPS=>
CHLA-136 NF7aSo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTF2LkKgcm0> MWKyOVI3OzV|OR?=
NALM-6 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2Tzd2lEPTB;NEmgcm0> MXeyOVI3OzV|OR?=
COG-LL-317 NWXSWZY{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmL0TWM2OD17LkSgcm0> NHviUJEzPTJ4M{WzPS=>
RS4;11 Mn3OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXETWM2OD13Mj62JI5O MX6yOVI3OzV|OR?=
MOLT-4 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTF4Lk[gcm0> MoXCNlUzPjN3M{m=
CCRF-CEM NHm4XmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTZ7Nz6zJI5O NHXEVoszPTJ4M{WzPS=>
Kasumi-1 M4\1[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfNR4JKSzVyPUe4Ok4zKG6P MnzlNlUzPjN3M{m=
Karpas-299 NVfSNpB6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELOXm9KSzVyPUe1Mlchdk1? MonlNlUzPjN3M{m=
Ramos-RA1 NHriW5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{H3ZmlEPTB;NkiuN{BvVQ>? NVq2fJk{OjV{NkO1N|k>
DT40 NHHBXG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XvcGlEPTB;NDDuUS=> NU[4Vm5YOjR|NU[4NVM>
DU145 MlLvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTFzIH7N M3u1UVI1OzV4OEGz
H209 NHjFOZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3ntWGlEPTB;MT63JI5O M1K0fFI1ODd5M{Ww
H1048 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1i1WGlEPTB;Mj6yJI5O NXqzd3lNOjRyN{ezOVA>
H524 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1:2Z2lEPTB;Mz6xJI5O MUSyOFA4PzN3MB?=
H1930 NXv2eJVlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHMZoFFUUN3ME20MlEhdk1? NIrQR2szPDB5N{O1NC=>
H69 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTIV4dKSzVyPUWuNkBvVQ>? NIC2N3UzPDB5N{O1NC=>
H2081 NWnRU2pzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIX2ZWNKSzVyPU[uN{BvVQ>? NHPQSVkzPDB5N{O1NC=>
H2107 MkjDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHr6XHpKSzVyPUeuN{BvVQ>? Mmq0NlQxPzd|NUC=
H1092 MoDlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13Ke2lEPTB;OD65JI5O Mm\uNlQxPzd|NUC=
DMS-79 M3XYcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4Hi[2lEPTB;OT6zJI5O MUSyOFA4PzN3MB?=
H446 NF;1XHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIfvV|BKSzVyPUGzJI5O NWH1dphzOjRyN{ezOVA>
COR-L279 NGX4ZndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\CdWZXUUN3ME2xOUBvVQ>? NGmzPWgzPDB5N{O1NC=>

... Click to View More Cell Line Experimental Data

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]

+ Expand
  • Animal Models: MX-1 model (BRCA-1 deficient)
  • Formulation: --
  • 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
Synonyms LT-673

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01989546 Active, not recruiting Advanced Ovarian Cancer|Primary Peritoneal Cancer|Advanced Breast Cancer|Advanced Solid Tumors National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) November 8, 2013 Phase 1|Phase 2
NCT02286687 Active, not recruiting Advanced Cancers M.D. Anderson Cancer Center|BioMarin Pharmaceutical December 22, 2014 Phase 2
NCT02997163 Not yet recruiting Advanced Solid Tumors Medivation, Inc. January 2017 Phase 1
NCT02997176 Recruiting Advanced Solid Tumors Medivation, Inc. November 2016 Phase 1
NCT03042910 Recruiting Solid Tumor Medivation, Inc. October 2016 Phase 1
NCT02836028 Withdrawn Ovarian Cancer Medivation, Inc.|Myriad Genetic Laboratories, Inc. October 2016 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.

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

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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