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 0.57 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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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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Choose Selective PARP Inhibitors

Biological Activity

Description Talazoparib (BMN 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.
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 NGLGUVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\NcJUxNjFvMUCwJI5O M13xOFI1NzR6L{eyJIg> MULpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36g[I9{\SCmZYDlcoRmdnSueR?= MnTPNlYxPDd4OUe=
BR5FVB1-Akt NYfjbZJKSXCxcITvd4l{KEG|c3H5 M1TsNVAvOS1zMECgcm0> NEjHU2k4OiCq NFPDbIlqdmS3Y3XzJIFxd3C2b4Ppdy=> MXKyOlA1PzZ7Nx?=
Capan-1 NWfVV3BYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3XB[2lEPTB;MU[uNQKBkcLz4pEJOU416oDLwsXNxsA> NXPNeGplOjV6NkS1PVA>
MIA PaCa-2 NEnhOHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXH[2lKSzVyPUW4MlI{6oDLwsJihKk5NjIkgJpCuW3DqA>? NFXqW4QzPTh4NEW5NC=>
RD MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRThwNzDuUS=> NW[4SlBbOjV{NkO1N|k>
Rh41 NF[zdm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHn1W4ZKSzVyPUiuNUBvVQ>? NILsc|kzPTJ4M{WzPS=>
Rh18 M37IWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnkXXBKSzVyPUSuPUBvVQ>? MoXINlUzPjN3M{m=
CHLA-266 NEXqTpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDkbVJbUUN3ME9ihKkyNDByMDDuUS=> MYOyOVI3OzV|OR?=
TC-71 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmf5TWM2OD1|Lkegcm0> MV[yOVI3OzV|OR?=
CHLA-9 M{nucWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRThwMjDuUS=> MXqyOVI3OzV|OR?=
CHLA-10 NGXTR2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\2PXNpUUN3ME22O{45KG6P MUiyOVI3OzV|OR?=
CHLA-258 NFrud4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjzTWM2OD12Lk[gcm0> MWGyOVI3OzV|OR?=
SJ-GBM2 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVLJR|UxRTF4LkKgcm0> MnvLNlUzPjN3M{m=
NB-1643 NUHKT5VWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfzTWM2OD1zOD60JI5O MX2yOVI3OzV|OR?=
NB-EBc1 MknkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvGTWM2OD1{NT64JI5O MmTqNlUzPjN3M{m=
CHLA-136 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTF2LkKgcm0> MkPQNlUzPjN3M{m=
NALM-6 MmfCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HNRWlEPTB;NEmgcm0> NVXXbHB7OjV{NkO1N|k>
COG-LL-317 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4PM[2lEPTB;OT60JI5O NXTi[IJWOjV{NkO1N|k>
RS4;11 NUfBXYtKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGCw[FBKSzVyPUWyMlYhdk1? M1\x[lI2OjZ|NUO5
MOLT-4 NG\ESnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVO1UlZCUUN3ME2xOk43KG6P NWC2ZZZqOjV{NkO1N|k>
CCRF-CEM NWHtNlBVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3frdGlEPTB;Nkm3MlMhdk1? M2n4PFI2OjZ|NUO5
Kasumi-1 NFrCS|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zPXGlEPTB;N{i2MlIhdk1? MYGyOVI3OzV|OR?=
Karpas-299 MlHXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33BbWlEPTB;N{WuO{BvVQ>? MVGyOVI3OzV|OR?=
Ramos-RA1 MkfWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHXRppKSzVyPU[4MlMhdk1? MnXvNlUzPjN3M{m=
DT40 M{G0dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTlVJFvUUN3ME20JI5O NWDveIZmOjR|NU[4NVM>
DU145 M372emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTFzIH7N NHSwZY4zPDN3NkixNy=>
H209 NHzC[G1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;t[ItKSzVyPUGuO{BvVQ>? NITR[40zPDB5N{O1NC=>
H1048 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzNR3FKSzVyPUKuNkBvVQ>? M1i2V|I1ODd5M{Ww
H524 M37JW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUS5boRyUUN3ME2zMlEhdk1? MoHYNlQxPzd|NUC=
H1930 NX7Idm45T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTRwMTDuUS=> Mn3NNlQxPzd|NUC=
H69 M372fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFq0dGtKSzVyPUWuNkBvVQ>? NVzxS4h4OjRyN{ezOVA>
H2081 NGqzVINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkO4TWM2OD14LkOgcm0> MmfNNlQxPzd|NUC=
H2107 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\ue|BKSzVyPUeuN{BvVQ>? M2\4UVI1ODd5M{Ww
H1092 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIK3c4tKSzVyPUiuPUBvVQ>? MWqyOFA4PzN3MB?=
DMS-79 NVnLdo06T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLpSVhKSzVyPUmuN{BvVQ>? NXTGR3lsOjRyN{ezOVA>
H446 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LYPWlEPTB;MUOgcm0> NXv5OpA{OjRyN{ezOVA>
COR-L279 M4rnNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYm0[FBnUUN3ME2xOUBvVQ>? NXLXUFFKOjRyN{ezOVA>

... 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]


Animal Research:


+ 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


CAS No. 1207456-01-6
Storage powder
in solvent
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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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