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 36 Publications

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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 NH:3VZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fqelAvOS1zMECgcm0> NGjIb|gzPC92OD:3NkBp NYrCbVA2cW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> NVXFZnZZOjZyNEe2PVc>
BR5FVB1-Akt MVjBdI9xfG:|aYOgRZN{[Xl? NFO5V2UxNjFvMUCwJI5O MVW3NkBp MYXpcoR2[2W|IHHwc5B1d3Orcx?= NHrXOYMzPjB2N{[5Oy=>
Capan-1 MoLRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7VTWM2OD1zNj6w5qCKyrIkgJm1MlTjiIoEtV5CpC=> MUWyOVg3PDV7MB?=
MIA PaCa-2 NUDz[XNKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfjW3RKSzVyPUW4MlI{6oDLwsJihKk5NjIkgJpCuW3DqA>? NFLUb4wzPTh4NEW5NC=>
RD MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRThwNzDuUS=> MkHsNlUzPjN3M{m=
Rh41 NWftU3BYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MonQTWM2OD16LkGgcm0> NEWyZoYzPTJ4M{WzPS=>
Rh18 M1\n[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;5T2lEPTB;ND65JI5O MVqyOVI3OzV|OR?=
Rh30 NHPYeGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmi5TWM2OD1|MT6xJI5O MnzxNlUzPjN3M{m=
BT-12 NETRTG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{LUNmlEPTB-4pEJNUwxODBibl2= MljDNlUzPjN3M{m=
CHLA-266 NFHKTZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXyxe5RUUUN3ME9ihKkyNDByMDDuUS=> NXjYd2VQOjV{NkO1N|k>
TC-71 M{HidWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHvSYc{UUN3ME2zMlchdk1? M3XPU|I2OjZ|NUO5
CHLA-9 NIrUO41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRThwMjDuUS=> NHTPOXAzPTJ4M{WzPS=>
CHLA-10 MoTCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHETWM2OD14Nz64JI5O MkfBNlUzPjN3M{m=
CHLA-258 M{O1[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFrZVZlKSzVyPUSuOkBvVQ>? MY[yOVI3OzV|OR?=
SJ-GBM2 MlfOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYK3eYNqUUN3ME2xOk4zKG6P MVuyOVI3OzV|OR?=
NB-1643 NWjPe|lQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jDNGlEPTB;MUiuOEBvVQ>? Mke5NlUzPjN3M{m=
NB-EBc1 NVnVOZd3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fGPWlEPTB;MkWuPEBvVQ>? MoDpNlUzPjN3M{m=
CHLA-90 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vZOWlEPTB-4pEJNUwxODBibl2= NWXJNXl[OjV{NkO1N|k>
CHLA-136 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXzTWM2OD1zND6yJI5O M4LYeVI2OjZ|NUO5
NALM-6 NG[1OXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXkTWM2OD12OTDuUS=> MYGyOVI3OzV|OR?=
COG-LL-317 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHTTWM2OD17LkSgcm0> MofTNlUzPjN3M{m=
RS4;11 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW[yW4hPUUN3ME21Nk43KG6P MVWyOVI3OzV|OR?=
MOLT-4 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEDxVotKSzVyPUG2MlYhdk1? MYeyOVI3OzV|OR?=
CCRF-CEM M1H4eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3lNYhKSzVyPU[5O{4{KG6P NITMV4kzPTJ4M{WzPS=>
Kasumi-1 NH\K[VFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTd6Nj6yJI5O MkjFNlUzPjN3M{m=
Karpas-299 M{S0NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XOXWlEPTB;N{WuO{BvVQ>? MXyyOVI3OzV|OR?=
Ramos-RA1 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjLVWJKSzVyPU[4MlMhdk1? MXqyOVI3OzV|OR?=
DT40 M1rwcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTRibl2= MnvNNlQ{PTZ6MUO=
DU145 M3:xNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVK5PW5qUUN3ME2xNUBvVQ>? M1HQbVI1OzV4OEGz
H209 NV3WbZpwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUO1WpZEUUN3ME2xMlchdk1? NUL1NoxIOjRyN{ezOVA>
H1048 NYP5SWVvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2C4WWlEPTB;Mj6yJI5O MmCwNlQxPzd|NUC=
H524 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzD[WlKSzVyPUOuNUBvVQ>? MnnxNlQxPzd|NUC=
H1930 M2ryZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DoXmlEPTB;ND6xJI5O NYXVOnMzOjRyN{ezOVA>
H69 NHv0d4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MorETWM2OD13LkKgcm0> NX3MXpp2OjRyN{ezOVA>
H2081 Mk\RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPMTWM2OD14LkOgcm0> MknUNlQxPzd|NUC=
H2107 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fRbGlEPTB;Nz6zJI5O NE\SWFAzPDB5N{O1NC=>
H1092 NUOxVHdiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\CdndtUUN3ME24Mlkhdk1? NUfydYh7OjRyN{ezOVA>
DMS-79 NInoSmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPsTWM2OD17LkOgcm0> M1PUXFI1ODd5M{Ww
H446 NWLQepQ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY[2bGN6UUN3ME2xN{BvVQ>? NY\yWYVjOjRyN{ezOVA>
COR-L279 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfYPY1KSzVyPUG1JI5O MYGyOFA4PzN3MB?=

... 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]

+ 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 interventions Conditions Sponsor/Collaborators Start Date Phases
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
NCT03911973 Recruiting Drug: Gedatolisib|Drug: Talazoparib TNBC - Triple-Negative Breast Cancer Kari Wisinski|Pfizer|Big Ten Cancer Research Consortium April 17 2019 Phase 1|Phase 2
NCT03875313 Recruiting Drug: CB-839|Drug: Talazoparib Solid Tumor|Clear Cell Renal Cell Carcinoma|TNBC - Triple-Negative Breast Cancer|Colorectal Cancer|CRC|RCC|ccRCC Calithera Biosciences Inc March 22 2019 Phase 1|Phase 2
NCT03672773 Recruiting Drug: Talazoparib|Drug: Temozolomide 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

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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