Talazoparib (BMN 673)

For research use only.

Catalog No.S7048 Synonyms: LT-673

92 publications

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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Selleck's Talazoparib (BMN 673) has been cited by 92 publications

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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.
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 M4j3cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGGz[HYxNjFvMUCwJI5O MWGyOE81QC95MjDo MojubY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViZHXw[Y5l\W62bIm= M{T5bVI3ODR5Nkm3
BR5FVB1-Akt MUfBdI9xfG:|aYOgRZN{[Xl? NUKzTmhbOC5zLUGwNEBvVQ>? M1m3SFczKGh? NFzje2pqdmS3Y3XzJIFxd3C2b4Ppdy=> MYOyOlA1PzZ7Nx?=
Capan-1 MlG3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGH5WnRKSzVyPUG2MlDjiIoEsfMAjVUvPOLCidM1UeKh NGHTUYczPTh4NEW5NC=>
MIA PaCa-2 M3LidGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYnRWoxKUUN3ME21PE4zO+LCidMx5qCKQC5z4pEJxtVOyqB? M4Pq[lI2QDZ2NUmw
RD NXHNdlY2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFn6XmxKSzVyPUiuO{BvVQ>? NH3HZlgzPTJ4M{WzPS=>
Rh41 NVnNeVNFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HQ[mlEPTB;OD6xJI5O MkjpNlUzPjN3M{m=
Rh30 NUDGUmJwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnWyTWM2OD1|MT6xJI5O MYqyOVI3OzV|OR?=
BT-12 NIDiO4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRuLCiUGsNFAxKG6P NE\uPYszPTJ4M{WzPS=>
CHLA-266 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmnETWM2OD8kgJmxMFAxOCCwTR?= NGnheIUzPTJ4M{WzPS=>
TC-71 NHLIcnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3CTWM2OD1|Lkegcm0> MYOyOVI3OzV|OR?=
CHLA-9 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVH4eYFmUUN3ME24MlIhdk1? NXnqPHVUOjV{NkO1N|k>
CHLA-10 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fmWWlEPTB;NkeuPEBvVQ>? NVzjSI9sOjV{NkO1N|k>
CHLA-258 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXmepFvUUN3ME20MlYhdk1? NILxeoEzPTJ4M{WzPS=>
SJ-GBM2 NGTDcmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfXVnJKSzVyPUG2MlIhdk1? NHTtco8zPTJ4M{WzPS=>
NB-1643 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|UxRTF6LkSgcm0> MXeyOVI3OzV|OR?=
NB-EBc1 MlqwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4[xXWlEPTB;MkWuPEBvVQ>? MXWyOVI3OzV|OR?=
CHLA-90 NG\3R3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVP1SHJ5UUN3ME9ihKkyNDByMDDuUS=> M1vZdVI2OjZ|NUO5
CHLA-136 M2DwZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTF2LkKgcm0> NV;CUop5OjV{NkO1N|k>
NALM-6 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTR7IH7N MVqyOVI3OzV|OR?=
COG-LL-317 NFj1VXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\YXoVKSzVyPUmuOEBvVQ>? M17uPFI2OjZ|NUO5
RS4;11 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTV{Lk[gcm0> NXzIcog3OjV{NkO1N|k>
Kasumi-1 NWTpWYZbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTd6Nj6yJI5O NEDk[GUzPTJ4M{WzPS=>
Karpas-299 NYK5eI43T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTd3Lkegcm0> MUWyOVI3OzV|OR?=
Ramos-RA1 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF64U4xKSzVyPU[4MlMhdk1? M3zLZlI2OjZ|NUO5
DT40 M4rNUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHraepJKSzVyPUSgcm0> MmnqNlQ{PTZ6MUO=
DU145 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXn5XFlEUUN3ME2xNUBvVQ>? MW[yOFM2PjhzMx?=
H209 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\tboVKSzVyPUGuO{BvVQ>? NHPudoQzPDB5N{O1NC=>
H1048 Mmq0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFX1cGFKSzVyPUKuNkBvVQ>? MWeyOFA4PzN3MB?=
H524 M37ZVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfrW5RKSzVyPUOuNUBvVQ>? MXWyOFA4PzN3MB?=
H1930 NUjlRYFuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnvTWM2OD12LkGgcm0> MWGyOFA4PzN3MB?=
H69 M4TXOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXJW2dKSzVyPUWuNkBvVQ>? NFP3[VczPDB5N{O1NC=>
H2081 MojrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXNZ4ZyUUN3ME22MlMhdk1? Mof6NlQxPzd|NUC=
H2107 M{HD[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPjXHd1UUN3ME23MlMhdk1? MYmyOFA4PzN3MB?=
H1092 MnfSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnOOmZ5UUN3ME24Mlkhdk1? NX6zdFZbOjRyN{ezOVA>
DMS-79 NF7TbVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3r2VWlEPTB;OT6zJI5O NHTRVoczPDB5N{O1NC=>
H446 NYi0V4xxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI[wdVVKSzVyPUGzJI5O MXGyOFA4PzN3MB?=
COR-L279 M3HwW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXUeFBFUUN3ME2xOUBvVQ>? NIKwWGIzPDB5N{O1NC=>

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
cleaved-PARP / cleaved-caspase3 / γ-H2AX; 

PubMed: 29158830     

Western Blot data testing protein expression after treatment with Olaparib, Niraparib, and Talazoparib on Brca1-deficient cell line in W0069 cells.

pKAP1 / pChk2 / pChk1; 

PubMed: 28947502     

Western blot images (representative from 3 independent experiments) showing the impact of a 24 hour pre-treatment with TAL ± TMZ on DNA damage signaling in U251 (MGMT-low) and T98G (MGMT-high) cells. 


PubMed: 28167507     

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. 


PubMed: 30472087     

Western blot analysis of the DNA damage sensors ATM, p-ATM (Ser1981), CHK1, p-CHK1 (Ser317), CHK2 and p-CHK2 (Thr68) in MV4-11 and HL-60 cells. GAPDH served as a loading control.

29158830 28947502 28167507 30472087
Growth inhibition assay
Cell viability; 

PubMed: 29158830     

Measured dose response curve and IC50 of Talazoparib in W780 and W0069 cells.

cleaved PARP / 53BP1; 

PubMed: 28958991     

Cleaved-PARP and 53BP1 expression. Representative images with 10× objective from high-content imaging of control cells in the left column, and cells treated with veliparib, olaparib, and talazoparib in three right columns. 53BP1 expression is seen in: A, HCC1143; B, MDAMB231; and C, HCC1806. Blue represents nuclear staining and pink foci represent 53BP1 foci. Cleaved-PARP expression is seen in D, HCC1143 and E, HCC1806. Blue represents nuclear staining and green represents cleaved-PARP expression.


PubMed: 30621214     

(A) MCF7 and (B) MCF7-T cells were treated with either 100 nM tamoxifen (Tamox) or 1 nM talazoparib (Talaz) for 72 h, alone and in combination. 24 h post treatment RAD51 foci formation assay was performed. Scale bar: 20 µm.

28958991 30621214
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:


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  • Animal Models: MX-1 model (BRCA-1 deficient)
  • 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 interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04337970 Recruiting Drug: Talazoparib|Drug: Axitinib Kidney Cancer|Renal Cell Carcinoma|Unresectable Renal Cell Carcinoma|Metastatic Renal Cell Carcinoma Memorial Sloan Kettering Cancer Center April 6 2020 Phase 1|Phase 2
NCT04134884 Recruiting Drug: Talazoparib|Drug: ASTX727 Metastatic Breast Cancer|Triple Negative Breast Cancer|Hormone Receptor Positive Tumor Kathy Miller|Pfizer|Astex Pharmaceuticals Inc.|Van Andel Institute Stand Up to Cancer Team|Indiana University March 30 2020 Phase 1
NCT03974217 Recruiting Drug: Talazoparib Leukemia Dana-Farber Cancer Institute|Pfizer August 1 2019 Phase 1
NCT03901469 Recruiting Drug: ZEN003694|Drug: Talazoparib Triple Negative Breast Cancer Zenith Epigenetics|Pfizer June 26 2019 Phase 2

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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