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 29 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 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LQV|AvOS1zMECgcm0> NIfxXpMzPC92OD:3NkBp MXHpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36g[I9{\SCmZYDlcoRmdnSueR?= M1flUFI3ODR5Nkm3
BR5FVB1-Akt NW\OPHlPSXCxcITvd4l{KEG|c3H5 Mmf2NE4yNTFyMDDuUS=> M1LZ[lczKGh? MWTpcoR2[2W|IHHwc5B1d3Orcx?= MYqyOlA1PzZ7Nx?=
Capan-1 NY\3dplvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTF4LkFihKnDueLCiUWuOQKBkcL3TdMg MXKyOVg3PDV7MB?=
MIA PaCa-2 NVK2N4hwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TZWGlEPTB;NUiuNlPjiIoEsfMAjVgvOeLCidM1UeKh NX3tXoRnOjV6NkS1PVA>
RD NF3Nd5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\UWldKSzVyPUiuO{BvVQ>? NEP1bYozPTJ4M{WzPS=>
Rh41 M2XGfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTReopEUUN3ME24MlEhdk1? M4[3OlI2OjZ|NUO5
Rh18 Mn3VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13lUWlEPTB;ND65JI5O MUOyOVI3OzV|OR?=
Rh30 NV[5VVB2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Moe5TWM2OD1|MT6xJI5O MmLvNlUzPjN3M{m=
BT-12 NVPRRWtMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1rue2lEPTB-4pEJNUwxODBibl2= NEPiRo4zPTJ4M{WzPS=>
CHLA-266 NIrFN5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRuLCiUGsNFAxKG6P NX3iV5JlOjV{NkO1N|k>
TC-71 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVLJR|UxRTNwNzDuUS=> MXOyOVI3OzV|OR?=
CHLA-9 NIDv[4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF3We4FKSzVyPUiuNkBvVQ>? M2[zOVI2OjZ|NUO5
CHLA-10 NEHkR25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\4Z2lEPTB;NkeuPEBvVQ>? MonDNlUzPjN3M{m=
CHLA-258 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTRwNjDuUS=> M2rjXFI2OjZ|NUO5
SJ-GBM2 M2nXfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTF4LkKgcm0> NWf5TW4{OjV{NkO1N|k>
NB-1643 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3KwVWlEPTB;MUiuOEBvVQ>? M3zyXVI2OjZ|NUO5
NB-EBc1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTJ3Lkigcm0> NFf1SHgzPTJ4M{WzPS=>
CHLA-90 M4P3eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRuLCiUGsNFAxKG6P NFLGbIQzPTJ4M{WzPS=>
CHLA-136 MmLkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4K0W2lEPTB;MUSuNkBvVQ>? NITTeGkzPTJ4M{WzPS=>
NALM-6 NFzlW5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTR7IH7N MnHhNlUzPjN3M{m=
COG-LL-317 MkXNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonhTWM2OD17LkSgcm0> MkXnNlUzPjN3M{m=
RS4;11 NHfndZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LPZ2lEPTB;NUKuOkBvVQ>? MmTjNlUzPjN3M{m=
MOLT-4 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7tT4F{UUN3ME2xOk43KG6P M{TXSVI2OjZ|NUO5
CCRF-CEM MlGyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTZ7Nz6zJI5O MlTzNlUzPjN3M{m=
Kasumi-1 MnPLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M160e2lEPTB;N{i2MlIhdk1? NHrXVZgzPTJ4M{WzPS=>
Karpas-299 NEfjd4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjiTVVKSzVyPUe1Mlchdk1? MlvzNlUzPjN3M{m=
Ramos-RA1 NI\kcXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH[1UXJKSzVyPU[4MlMhdk1? MVuyOVI3OzV|OR?=
DT40 M2CyXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHr0fG9KSzVyPUSgcm0> MYSyOFM2PjhzMx?=
DU145 Mlj6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTFzIH7N NIDXTVUzPDN3NkixNy=>
H209 NXTDRZRHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4e0OmlEPTB;MT63JI5O NX7qSWJPOjRyN{ezOVA>
H1048 M{fDbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFrKTVFKSzVyPUKuNkBvVQ>? MWWyOFA4PzN3MB?=
H524 NYDpXFRxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlznTWM2OD1|LkGgcm0> MkjrNlQxPzd|NUC=
H1930 NEXEO5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWO4em1xUUN3ME20MlEhdk1? Mn3JNlQxPzd|NUC=
H69 M3HPR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1HRNWlEPTB;NT6yJI5O M3\jOFI1ODd5M{Ww
H2081 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1XkNmlEPTB;Nj6zJI5O NXvCXogyOjRyN{ezOVA>
H2107 NV7TbZdGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPjTnFKSzVyPUeuN{BvVQ>? NG\oSGEzPDB5N{O1NC=>
H1092 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTHTWM2OD16Lkmgcm0> NGjhTIszPDB5N{O1NC=>
DMS-79 NY\Zdo1YT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUHVe5BiUUN3ME25MlMhdk1? NXrQOW97OjRyN{ezOVA>
H446 MmfXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2r3VWlEPTB;MUOgcm0> NX\Q[lR1OjRyN{ezOVA>
COR-L279 NILCOVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nNSWlEPTB;MUWgcm0> M{CyRVI1ODd5M{Ww

... 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 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

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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"

selleck catalog

PARP Signaling Pathway Map

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  • PARP Inhibitor in Clinical Trial

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID