Talazoparib (BMN 673)

For research use only.

Catalog No.S7048 Synonyms: LT-673

106 publications

Talazoparib (BMN 673) Chemical Structure

CAS No. 1207456-01-6

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 106 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 MkLyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW[wMlEuOTByIH7N MWiyOE81QC95MjDo NF3tcVhqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDk[ZBmdmSnboTsfS=> MoDKNlYxPDd4OUe=
BR5FVB1-Akt MoHiRZBweHSxc3nzJGF{e2G7 MWewMlEuOTByIH7N M2TYTFczKGh? MV3pcoR2[2W|IHHwc5B1d3Orcx?= MnvQNlYxPDd4OUe=
Capan-1 Ml\NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjnNGtyUUN3ME2xOk4x6oDLwsJihKk2NjUkgJpCuW3DqA>? MnvCNlU5PjR3OUC=
MIA PaCa-2 NF\TWYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXqyXm16UUN3ME21PE4zO+LCidMx5qCKQC5z4pEJxtVOyqB? MkfnNlU5PjR3OUC=
RD MoLGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPkfYVKSzVyPUiuO{BvVQ>? M4S4dlI2OjZ|NUO5
Rh41 NUe2S4syT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGnIdHhKSzVyPUiuNUBvVQ>? NGe5T5AzPTJ4M{WzPS=>
Rh18 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml7GTWM2OD12Lkmgcm0> NHvoTIczPTJ4M{WzPS=>
Rh30 M3nONWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrkfVhMUUN3ME2zNU4yKG6P NHqxe|gzPTJ4M{WzPS=>
BT-12 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHNZ4ptUUN3ME9ihKkyNDByMDDuUS=> MnLHNlUzPjN3M{m=
CHLA-266 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HEeWlEPTB-4pEJNUwxODBibl2= MVuyOVI3OzV|OR?=
TC-71 MnXUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTNwNzDuUS=> M1jKTVI2OjZ|NUO5
CHLA-9 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFq1cHhKSzVyPUiuNkBvVQ>? NUWzNGE4OjV{NkO1N|k>
CHLA-10 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTZ5Lkigcm0> NGfhdXYzPTJ4M{WzPS=>
CHLA-258 M1HHcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI[w[HBKSzVyPUSuOkBvVQ>? M4PVOVI2OjZ|NUO5
SJ-GBM2 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzhR2piUUN3ME2xOk4zKG6P NGPsRmQzPTJ4M{WzPS=>
NB-1643 NHXLRWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{D5XGlEPTB;MUiuOEBvVQ>? MkjINlUzPjN3M{m=
NB-EBc1 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTJ3Lkigcm0> Mn\3NlUzPjN3M{m=
CHLA-136 NWTLbHRqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTF2LkKgcm0> MV6yOVI3OzV|OR?=
COG-LL-317 MlXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTlwNDDuUS=> MnzuNlUzPjN3M{m=
RS4;11 NHTDNoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnKTWM2OD13Mj62JI5O MmDuNlUzPjN3M{m=
Kasumi-1 M3vNUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;kT2R[UUN3ME23PFYvOiCwTR?= NVnmfWh{OjV{NkO1N|k>
Karpas-299 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HKb2lEPTB;N{WuO{BvVQ>? MmjLNlUzPjN3M{m=
Ramos-RA1 M4LUUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TPZ2lEPTB;NkiuN{BvVQ>? Mo\LNlUzPjN3M{m=
DT40 M2DJNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjscpBKSzVyPUSgcm0> NU\EZZkzOjR|NU[4NVM>
DU145 NHj6TIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoTPTWM2OD1zMTDuUS=> MWCyOFM2PjhzMx?=
H209 MnXlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLsTWM2OD1zLkegcm0> Ml3nNlQxPzd|NUC=
H1048 MmnKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTJwMjDuUS=> M3ziO|I1ODd5M{Ww
H524 MljhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTNwMTDuUS=> M4LjXFI1ODd5M{Ww
H1930 NHrEc|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\JR|UxRTRwMTDuUS=> NGTWe|EzPDB5N{O1NC=>
H69 NYXhd|FRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2LxXWlEPTB;NT6yJI5O M{HvdlI1ODd5M{Ww
H2081 M3ywPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTZwMzDuUS=> M3jPO|I1ODd5M{Ww
H2107 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjwWZFKSzVyPUeuN{BvVQ>? MkXTNlQxPzd|NUC=
H1092 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUTNOWF{UUN3ME24Mlkhdk1? MY[yOFA4PzN3MB?=
DMS-79 NUfBZ3NrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDJTWM2OD17LkOgcm0> MkP0NlQxPzd|NUC=
H446 Mlm5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4H5W2lEPTB;MUOgcm0> MojsNlQxPzd|NUC=
COR-L279 MlfMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTF3IH7N NEX5eoszPDB5N{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
Smiles CN1C(=NC=N1)C2C(NC3=CC(=CC4=C3C2=NNC4=O)F)C5=CC=C(C=C5)F

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04497116 Recruiting Drug: RP-3500|Drug: Talazoparib: oral PARP inhibitor Advanced Solid Tumor Adult Repare Therapeutics July 22 2020 Phase 1|Phase 2
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

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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