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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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 Mom2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PoeFAvOS1zMECgcm0> M4TadlI1NzR6L{eyJIg> MWDpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36g[I9{\SCmZYDlcoRmdnSueR?= NIXBRXIzPjB2N{[5Oy=>
BR5FVB1-Akt MV3BdI9xfG:|aYOgRZN{[Xl? NFjmTZgxNjFvMUCwJI5O MYi3NkBp M{HN[olv\HWlZYOgZZBweHSxc3nz MnXGNlYxPDd4OUe=
Capan-1 NWHiZYZmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTF4LkFihKnDueLCiUWuOQKBkcL3TdMg NETiSI4zPTh4NEW5NC=>
MIA PaCa-2 Mk\DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\HTWM2OD13OD6yN-KBkcLz4pEJPE4y6oDLwsXNxsA> Mn3RNlU5PjR3OUC=
RD MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoO5TWM2OD16Lkegcm0> NEfDcVYzPTJ4M{WzPS=>
Rh41 M1r3TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1yyeGlEPTB;OD6xJI5O M2jleVI2OjZ|NUO5
Rh18 NHGyRo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1e0ZWlEPTB;ND65JI5O NHLkNIIzPTJ4M{WzPS=>
Rh30 NHLUbmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULMbJFUUUN3ME2zNU4yKG6P NYO2VYhUOjV{NkO1N|k>
BT-12 NH7EbYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2X0UGlEPTB-4pEJNUwxODBibl2= NUiyPZRSOjV{NkO1N|k>
CHLA-266 M2rVeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXx[plKSzVyPvMAjVEtODByIH7N NFn4Z5kzPTJ4M{WzPS=>
TC-71 MnLRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zv[GlEPTB;Mz63JI5O M3v5PVI2OjZ|NUO5
CHLA-9 MkP5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mom0TWM2OD16LkKgcm0> NH7UOGszPTJ4M{WzPS=>
CHLA-10 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjaTWM2OD14Nz64JI5O Ml\oNlUzPjN3M{m=
CHLA-258 MlfnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXCTWM2OD12Lk[gcm0> MoKwNlUzPjN3M{m=
SJ-GBM2 MmjYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXkTWM2OD1zNj6yJI5O NYj5O|hzOjV{NkO1N|k>
NB-1643 NHfGV41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjPPGNKSzVyPUG4MlQhdk1? NXPkfGNUOjV{NkO1N|k>
NB-EBc1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37y[WlEPTB;MkWuPEBvVQ>? NYjabJlxOjV{NkO1N|k>
CHLA-90 M1HHdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRuLCiUGsNFAxKG6P MYqyOVI3OzV|OR?=
CHLA-136 M1vIVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmriTWM2OD1zND6yJI5O MX:yOVI3OzV|OR?=
NALM-6 NYCwfXZtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTR7IH7N NXviWm9sOjV{NkO1N|k>
COG-LL-317 M3zJTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTlwNDDuUS=> MY[yOVI3OzV|OR?=
RS4;11 NUfURYpUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTJNYNRUUN3ME21Nk43KG6P NV:zO|ZCOjV{NkO1N|k>
MOLT-4 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3ewbmlEPTB;MU[uOkBvVQ>? MX2yOVI3OzV|OR?=
CCRF-CEM NV\EcZNtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\JTWM2OD14OUeuN{BvVQ>? M3nuN|I2OjZ|NUO5
Kasumi-1 M3qzRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTd6Nj6yJI5O MoHSNlUzPjN3M{m=
Karpas-299 M1HDUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHrhSnZKSzVyPUe1Mlchdk1? M3PXNFI2OjZ|NUO5
Ramos-RA1 Mor6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nsUmlEPTB;NkiuN{BvVQ>? M1SwW|I2OjZ|NUO5
DT40 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLGTWM2OD12IH7N NYfxVJFzOjR|NU[4NVM>
DU145 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fU[WlEPTB;MUGgcm0> M4LzdVI1OzV4OEGz
H209 M3fXb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfJfoJKSzVyPUGuO{BvVQ>? MnLENlQxPzd|NUC=
H1048 M{\6bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3T3ZmlEPTB;Mj6yJI5O MXGyOFA4PzN3MB?=
H524 NGrXPIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfLVVRGUUN3ME2zMlEhdk1? NFXscHozPDB5N{O1NC=>
H1930 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnmxTWM2OD12LkGgcm0> MWKyOFA4PzN3MB?=
H69 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DWVGlEPTB;NT6yJI5O MUeyOFA4PzN3MB?=
H2081 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoT0TWM2OD14LkOgcm0> MUiyOFA4PzN3MB?=
H2107 M2[4fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTdwMzDuUS=> NXrEfI9zOjRyN{ezOVA>
H1092 M1Wzbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGnXOWlKSzVyPUiuPUBvVQ>? M17YWVI1ODd5M{Ww
DMS-79 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1jNRmlEPTB;OT6zJI5O MVeyOFA4PzN3MB?=
H446 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fUNGlEPTB;MUOgcm0> NInad2szPDB5N{O1NC=>
COR-L279 NH6xSVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnVcJpsUUN3ME2xOUBvVQ>? M1W2UlI1ODd5M{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]

- Collapse
  • 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