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.
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 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-90 NVzXe2pLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRuLCiUGsNFAxKG6P M2\JcFI2OjZ|NUO5
CHLA-136 NWTLbHRqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTF2LkKgcm0> MV6yOVI3OzV|OR?=
NALM-6 NUTLVYJ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHWydI1KSzVyPUS5JI5O NGXEVZkzPTJ4M{WzPS=>
COG-LL-317 MlXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTlwNDDuUS=> MnzuNlUzPjN3M{m=
RS4;11 NHTDNoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnKTWM2OD13Mj62JI5O MmDuNlUzPjN3M{m=
MOLT-4 MlPtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXkUJpGUUN3ME2xOk43KG6P M{TZTFI2OjZ|NUO5
CCRF-CEM NUPzU2JlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTZ7Nz6zJI5O M13BTFI2OjZ|NUO5
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

Assay
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. 

PD-L1; 

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. 

p-ATM; 

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.

29158830
Immunofluorescence
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.

RAD51; 

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]

Protocol

Animal Research:

[2]

- Collapse
  • 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
Formula

 

C19H14F2N6O
 
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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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