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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Cited by 12 Publications

6 Customer Reviews

  • DNA damage persists on withdrawal of PARPi in RNASEH2AKO cells. Wild-type and RNASEH2AKO HeLa cells were treated with talazoparib and released into fresh medium for the indicated times before being processed for γ-H2AX immunofluorescence and propidium iodide (PI) staining. The γ-H2AX immunofluorescence (pseudocolor plots) and cell cycle (histograms) FACS profiles shown are representative of three biologically independent experiments.

    Nature, 2018, 559(7713):285-289. Talazoparib (BMN 673) purchased from Selleck.

    MDA-MDA-MB-231 and BT549 cells were treated with 10 μM olaparib or 10 nM talazoparib for 24 hours, and subjected to immunoblotting with the indicated antibodies. PD-L1 knockout (K/O) cells were included as a negative control.

    Clin Cancer Res, 2017, 23(14):3711-3720. Talazoparib (BMN 673) purchased from Selleck.

  • 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 NHy5OXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\wVYIxNjFvMUCwJI5O MmjONlQwPDhxN{KgbC=> NIf3O45qdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDk[ZBmdmSnboTsfS=> MUOyOlA1PzZ7Nx?=
BR5FVB1-Akt Mo\mRZBweHSxc3nzJGF{e2G7 M3jzcFAvOS1zMECgcm0> MYm3NkBp NYfpcW9OcW6mdXPld{BieG:ydH;zbZM> NXvNfoR5OjZyNEe2PVc>
Capan-1 NXLuN4hnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDkWZF[UUN3ME2xOk4x6oDLwsJihKk2NjUkgJpCuW3DqA>? M1f5N|I2QDZ2NUmw
MIA PaCa-2 NWLEN3JWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTV6LkKz5qCKyrIkgJm4MlHjiIoEtV5CpC=> M1[2OlI2QDZ2NUmw
RD Mo\3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmT6TWM2OD16Lkegcm0> M1e4elI2OjZ|NUO5
Rh41 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRThwMTDuUS=> NFPidZEzPTJ4M{WzPS=>
Rh18 MlPKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTRwOTDuUS=> NUXpRZRMOjV{NkO1N|k>
Rh30 NEDPRnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHQTWM2OD1|MT6xJI5O Mm\UNlUzPjN3M{m=
BT-12 NVjQSHlsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGTBVIRKSzVyPvMAjVEtODByIH7N NHvzXnczPTJ4M{WzPS=>
CHLA-266 M4r3PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLyTWM2OD8kgJmxMFAxOCCwTR?= NEnaV3IzPTJ4M{WzPS=>
TC-71 M4LoNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\Bc3lKSzVyPUOuO{BvVQ>? M1rkS|I2OjZ|NUO5
CHLA-9 NVewSGFKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nyRmlEPTB;OD6yJI5O MU[yOVI3OzV|OR?=
CHLA-10 NHHZWHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTZ5Lkigcm0> MlzmNlUzPjN3M{m=
CHLA-258 NFPJco1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfqTWM2OD12Lk[gcm0> M1PqWFI2OjZ|NUO5
SJ-GBM2 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYK5cJNHUUN3ME2xOk4zKG6P MUKyOVI3OzV|OR?=
NB-1643 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHaNWhmUUN3ME2xPE41KG6P NUnKdHdzOjV{NkO1N|k>
NB-EBc1 NH7WOFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWSze4hHUUN3ME2yOU45KG6P M2XtbVI2OjZ|NUO5
CHLA-90 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXLJR|UxRuLCiUGsNFAxKG6P NHT0UVkzPTJ4M{WzPS=>
CHLA-136 M{f2NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLyTWM2OD1zND6yJI5O M1;PR|I2OjZ|NUO5
NALM-6 Mo\iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXr5TnhuUUN3ME20PUBvVQ>? M{PMTlI2OjZ|NUO5
COG-LL-317 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HqNmlEPTB;OT60JI5O MUKyOVI3OzV|OR?=
RS4;11 M3q5TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HiXGlEPTB;NUKuOkBvVQ>? NY[wUnZzOjV{NkO1N|k>
MOLT-4 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzDTWM2OD1zNj62JI5O NX;N[IROOjV{NkO1N|k>
CCRF-CEM M3;BeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XETGlEPTB;Nkm3MlMhdk1? NEHmcnkzPTJ4M{WzPS=>
Kasumi-1 MmXuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXQOotsUUN3ME23PFYvOiCwTR?= MYCyOVI3OzV|OR?=
Karpas-299 NWXKW4dXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTd3Lkegcm0> NFLxTJEzPTJ4M{WzPS=>
Ramos-RA1 M4npc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHUTWM2OD14OD6zJI5O NYS4N5Z7OjV{NkO1N|k>
DT40 MmXCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfGOGFKSzVyPUSgcm0> NFLodYgzPDN3NkixNy=>
DU145 M4XvWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTFzIH7N NVr1UFFoOjR|NU[4NVM>
H209 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn71TWM2OD1zLkegcm0> M{DDOlI1ODd5M{Ww
H1048 M33OO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nlcGlEPTB;Mj6yJI5O NGHYZ24zPDB5N{O1NC=>
H524 M3\Ucmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HGXWlEPTB;Mz6xJI5O MmDGNlQxPzd|NUC=
H1930 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzHTWM2OD12LkGgcm0> MVuyOFA4PzN3MB?=
H69 Mmn1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTVwMjDuUS=> MYGyOFA4PzN3MB?=
H2081 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2X4b2lEPTB;Nj6zJI5O NXP6WJB3OjRyN{ezOVA>
H2107 M2fvPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\ON2VKSzVyPUeuN{BvVQ>? NGPzelIzPDB5N{O1NC=>
H1092 M1jZe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nrWmlEPTB;OD65JI5O M4DkUlI1ODd5M{Ww
DMS-79 NV\DeWVCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHG3OJVKSzVyPUmuN{BvVQ>? NWfoW4ZIOjRyN{ezOVA>
H446 MmW2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3T2dGlEPTB;MUOgcm0> MV[yOFA4PzN3MB?=
COR-L279 NIrPU4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHKwSJVKSzVyPUG1JI5O MUOyOFA4PzN3MB?=

... 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
NCT03875313 Recruiting Solid Tumor|Clear Cell Renal Cell Carcinoma|TNBC - Triple-Negative Breast Cancer|Colorectal Cancer|CRC|RCC|ccRCC Calithera Biosciences Inc March 2019 Phase 1|Phase 2
NCT03875313 Recruiting Solid Tumor|Clear Cell Renal Cell Carcinoma|TNBC - Triple-Negative Breast Cancer|Colorectal Cancer|CRC|RCC|ccRCC Calithera Biosciences Inc March 2019 Phase 1|Phase 2
NCT03672773 Recruiting Recurrent Extensive Stage Small Cell Lung Carcinoma|Refractory Extensive Stage Small Cell Lung Carcinoma Jonsson Comprehensive Cancer Center|Translational Research in Oncology|National Cancer Institute (NCI) October 31 2018 Phase 2
NCT03672773 Recruiting Recurrent Extensive Stage Small Cell Lung Carcinoma|Refractory Extensive Stage Small Cell Lung Carcinoma Jonsson Comprehensive Cancer Center|Translational Research in Oncology|National Cancer Institute (NCI) October 31 2018 Phase 2
NCT03637491 Recruiting Pancreatic Cancer|Non-Small Cell Lung Cancer|Cancer Pfizer|Array BioPharma August 15 2018 Phase 2
NCT03499353 Recruiting Early Breast Cancer Pfizer August 27 2018 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

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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