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.

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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 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVKwMlEuOTByIH7N NVvaTW55OjRxNEivO|IhcA>? MX3pcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36g[I9{\SCmZYDlcoRmdnSueR?= MY[yOlA1PzZ7Nx?=
BR5FVB1-Akt NIrIUJRCeG:ydH;zbZMhSXO|YYm= M3jHdlAvOS1zMECgcm0> M4jZb|czKGh? NV\RfIJNcW6mdXPld{BieG:ydH;zbZM> MVWyOlA1PzZ7Nx?=
Capan-1 NUS1fVZ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTF4LkFihKnDueLCiUWuOQKBkcL3TdMg MoDlNlU5PjR3OUC=
MIA PaCa-2 M2PKNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3K3RmlEPTB;NUiuNlPjiIoEsfMAjVgvOeLCidM1UeKh MoPRNlU5PjR3OUC=
RD MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\UTWM2OD16Lkegcm0> NUPE[I1bOjV{NkO1N|k>
Rh41 NXP5dZdQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXLJR|UxRThwMTDuUS=> NG\GZXIzPTJ4M{WzPS=>
Rh18 M1jVUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1O1WmlEPTB;ND65JI5O M2jYS|I2OjZ|NUO5
Rh30 M4DpOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvzZZNFUUN3ME2zNU4yKG6P NVO2PXg4OjV{NkO1N|k>
BT-12 NInGN5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\Yc2tKSzVyPvMAjVEtODByIH7N NHzUVJYzPTJ4M{WzPS=>
CHLA-266 NVjYfmNkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfn[3d4UUN3ME9ihKkyNDByMDDuUS=> MXOyOVI3OzV|OR?=
TC-71 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV20TotUUUN3ME2zMlchdk1? NFrlTG4zPTJ4M{WzPS=>
CHLA-9 M2G2SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPUWGZKSzVyPUiuNkBvVQ>? NXHrSJk6OjV{NkO1N|k>
CHLA-10 M1Pofmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTZ5Lkigcm0> M3;NO|I2OjZ|NUO5
CHLA-258 NVXNdHp6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnUTWM2OD12Lk[gcm0> NGLoNZQzPTJ4M{WzPS=>
SJ-GBM2 NF\OdVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnjETWM2OD1zNj6yJI5O MYiyOVI3OzV|OR?=
NB-1643 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\GSFFZUUN3ME2xPE41KG6P M2fETVI2OjZ|NUO5
NB-EBc1 NV22d5FtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fKW2lEPTB;MkWuPEBvVQ>? M2XPVFI2OjZ|NUO5
CHLA-90 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjXcZVrUUN3ME9ihKkyNDByMDDuUS=> MYmyOVI3OzV|OR?=
CHLA-136 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjGU29lUUN3ME2xOE4zKG6P MkPPNlUzPjN3M{m=
NALM-6 M{GzZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHMZWlDUUN3ME20PUBvVQ>? NX30VYtrOjV{NkO1N|k>
COG-LL-317 NH7nW25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTlwNDDuUS=> NVL5V|ByOjV{NkO1N|k>
RS4;11 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTV{Lk[gcm0> MUSyOVI3OzV|OR?=
MOLT-4 M1viOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7FV5RKSzVyPUG2MlYhdk1? NYO0O4RFOjV{NkO1N|k>
CCRF-CEM MofQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTZ7Nz6zJI5O NUCz[5l4OjV{NkO1N|k>
Kasumi-1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{TsbWlEPTB;N{i2MlIhdk1? NI\aXGczPTJ4M{WzPS=>
Karpas-299 M3r6Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTd3Lkegcm0> NHXPTXAzPTJ4M{WzPS=>
Ramos-RA1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTzTWM2OD14OD6zJI5O M{LHSlI2OjZ|NUO5
DT40 NV71OZkyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzPTXN[UUN3ME20JI5O NIfMVIozPDN3NkixNy=>
DU145 M4TPNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXPTWM2OD1zMTDuUS=> MUeyOFM2PjhzMx?=
H209 M2LZSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mon3TWM2OD1zLkegcm0> M4TRZ|I1ODd5M{Ww
H1048 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HLfWlEPTB;Mj6yJI5O NH;rV2wzPDB5N{O1NC=>
H524 M3vkdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVznW45rUUN3ME2zMlEhdk1? NFzzZpEzPDB5N{O1NC=>
H1930 Mn7ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPwWFBtUUN3ME20MlEhdk1? NETYWmkzPDB5N{O1NC=>
H69 M37nXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTVwMjDuUS=> MYWyOFA4PzN3MB?=
H2081 NEnvVI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HXU2lEPTB;Nj6zJI5O MUCyOFA4PzN3MB?=
H2107 MlHHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7ITWM2OD15LkOgcm0> NF36R2czPDB5N{O1NC=>
H1092 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLG[nQ1UUN3ME24Mlkhdk1? NETkfm8zPDB5N{O1NC=>
DMS-79 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTlwMzDuUS=> MonHNlQxPzd|NUC=
H446 NUTKRotyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTF|IH7N NHnGV3kzPDB5N{O1NC=>
COR-L279 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvqVopKSzVyPUG1JI5O NUflO|dROjRyN{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]

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
NCT03426254 Enrolling by invitation Advanced or Recurrent Solid Tumors|Breast Neoplasm Center Trials & Treatment|BioGene Pharmaceutical February 8 2018 Phase 1
NCT02997163 Recruiting Advanced Solid Tumors Pfizer|Medivation Inc. February 8 2017 Phase 1
NCT02921919 Recruiting Cancer Pfizer|Medivation Inc. November 8 2016 Phase 2
NCT03377556 Recruiting ATM Gene Mutation|ATR Gene Mutation|BARD1 Gene Mutation|BRCA1 Gene Mutation|BRCA2 Gene Mutation|BRIP1 Gene Mutation|CHEK1 Gene Mutation|CHEK2 Gene Mutation|FANCA Gene Mutation|FANCC Gene Mutation|FANCD2 Gene Mutation|FANCF Gene Mutation|FANCM Gene Mutation|NBN Gene Mutation|PALB2 Gene Mutation|RAD51 Gene Mutation|RAD51B Gene Mutation|RAD54L Gene Mutation|Recurrent Squamous Cell Lung Carcinoma|RPA1 Gene Mutation|Stage IV Squamous Cell Lung Carcinoma AJCC v7 Southwest Oncology Group|National Cancer Institute (NCI) February 7 2017 Phase 2
NCT03077607 Completed Advanced Solid Tumors Pfizer|Medivation Inc. November 7 2016 Phase 1
NCT03148795 Recruiting Prostate Cancer Pfizer|Medivation Inc. July 4 2017 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