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, 23(13):3405-3415. 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.

Purity & Quality Control

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.
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 MnLVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXuNE4yNTFyMDDuUS=> M{W0SFI1NzR6L{eyJIg> NVnlO2NGcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> M2ixdFI3ODR5Nkm3
BR5FVB1-Akt NVfPSotjSXCxcITvd4l{KEG|c3H5 M1LsT|AvOS1zMECgcm0> M{DyfFczKGh? M1TafYlv\HWlZYOgZZBweHSxc3nz NHzyO2EzPjB2N{[5Oy=>
Capan-1 NYjKZWhbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHHTWM2OD1zNj6w5qCKyrIkgJm1MlTjiIoEtV5CpC=> MlvRNlU5PjR3OUC=
MIA PaCa-2 NWHHU2xUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnrvTWM2OD13OD6yN-KBkcLz4pEJPE4y6oDLwsXNxsA> NYns[41EOjV6NkS1PVA>
RD NUXHNHFsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3nNSWlEPTB;OD63JI5O NWPCRlhWOjV{NkO1N|k>
Rh41 NWrPU4xxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3HR5hKSzVyPUiuNUBvVQ>? NHfx[lUzPTJ4M{WzPS=>
Rh18 MomyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nUVmlEPTB;ND65JI5O NULSZmdTOjV{NkO1N|k>
Rh30 NWTnPZNoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUe3R3Q{UUN3ME2zNU4yKG6P M3viTVI2OjZ|NUO5
BT-12 M{ewPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjnbVk4UUN3ME9ihKkyNDByMDDuUS=> M3XIXlI2OjZ|NUO5
CHLA-266 NILGPZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLlSpJKSzVyPvMAjVEtODByIH7N NX64fYVqOjV{NkO1N|k>
TC-71 NXn2[4dXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrXbHd6UUN3ME2zMlchdk1? MY[yOVI3OzV|OR?=
CHLA-9 NYPJOlZOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlTLTWM2OD16LkKgcm0> M3uyd|I2OjZ|NUO5
CHLA-10 MnHTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzWV2RRUUN3ME22O{45KG6P MWSyOVI3OzV|OR?=
CHLA-258 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGSxVphKSzVyPUSuOkBvVQ>? NUHTW3lROjV{NkO1N|k>
SJ-GBM2 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEP3NXNKSzVyPUG2MlIhdk1? Mn;PNlUzPjN3M{m=
NB-1643 Ml\jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY[xWnJ4UUN3ME2xPE41KG6P MXWyOVI3OzV|OR?=
NB-EBc1 NELnc3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTJ3Lkigcm0> MVyyOVI3OzV|OR?=
CHLA-90 NGjLUoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDmRphKSzVyPvMAjVEtODByIH7N NVz3TVNmOjV{NkO1N|k>
CHLA-136 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVj0O41vUUN3ME2xOE4zKG6P MVWyOVI3OzV|OR?=
NALM-6 M3;yeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXL4VFRRUUN3ME20PUBvVQ>? M1XIZlI2OjZ|NUO5
COG-LL-317 MnLqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn71TWM2OD17LkSgcm0> NXjFNlBnOjV{NkO1N|k>
RS4;11 M{noV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPj[4FKSzVyPUWyMlYhdk1? MmPmNlUzPjN3M{m=
MOLT-4 NHrneW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37MU2lEPTB;MU[uOkBvVQ>? NF:yT4UzPTJ4M{WzPS=>
CCRF-CEM MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDITWM2OD14OUeuN{BvVQ>? MWGyOVI3OzV|OR?=
Kasumi-1 NHL3eZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnH2TWM2OD15OE[uNkBvVQ>? M2rCdVI2OjZ|NUO5
Karpas-299 NYfYTpdpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLQTWM2OD15NT63JI5O MlfJNlUzPjN3M{m=
Ramos-RA1 M4\HcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjNTWM2OD14OD6zJI5O NUfGOYsxOjV{NkO1N|k>
DT40 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{[3UGlEPTB;NDDuUS=> MlXDNlQ{PTZ6MUO=
DU145 MonnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPqNXdvUUN3ME2xNUBvVQ>? NWKwSGd7OjR|NU[4NVM>
H209 NX;YVnYxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1PPW2lEPTB;MT63JI5O Mlr4NlQxPzd|NUC=
H1048 NY[4bXMzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfYdJBOUUN3ME2yMlIhdk1? M{fCOFI1ODd5M{Ww
H524 Mn;0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTNwMTDuUS=> NHHKO|QzPDB5N{O1NC=>
H1930 NWDqc2JwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTRwMTDuUS=> NES0T3QzPDB5N{O1NC=>
H69 NYj1cXJ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDLRY03UUN3ME21MlIhdk1? NFnhOVgzPDB5N{O1NC=>
H2081 NEW5ZnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlruTWM2OD14LkOgcm0> M{\aPFI1ODd5M{Ww
H2107 M4fYRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTyTWM2OD15LkOgcm0> Ml3MNlQxPzd|NUC=
H1092 NUDHSlBFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRThwOTDuUS=> M1e1eVI1ODd5M{Ww
DMS-79 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TRfGlEPTB;OT6zJI5O Ml3xNlQxPzd|NUC=
H446 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3f2XmlEPTB;MUOgcm0> MYSyOFA4PzN3MB?=
COR-L279 NUnzXVVXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfWdZczUUN3ME2xOUBvVQ>? NHPuTJYzPDB5N{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
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.

Handling Instructions

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