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 79 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 MoW5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYKwMlEuOTByIH7N NHPZfpMzPC92OD:3NkBp MmGzbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViZHXw[Y5l\W62bIm= NWH1ZYh5OjZyNEe2PVc>
BR5FVB1-Akt M2\KUmFxd3C2b4Ppd{BCe3OjeR?= MYSwMlEuOTByIH7N NWHBWHJiPzJiaB?= MXrpcoR2[2W|IHHwc5B1d3Orcx?= NVy2[|lHOjZyNEe2PVc>
Capan-1 M2LtXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfjXpZKUUN3ME2xOk4x6oDLwsJihKk2NjUkgJpCuW3DqA>? Mn3CNlU5PjR3OUC=
MIA PaCa-2 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTV6LkKz5qCKyrIkgJm4MlHjiIoEtV5CpC=> MVeyOVg3PDV7MB?=
RD NXPZU5hmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLJR|UxRThwNzDuUS=> Mlz0NlUzPjN3M{m=
Rh41 MorpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrRTG9KSzVyPUiuNUBvVQ>? MlHRNlUzPjN3M{m=
Rh18 MnqzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDwfItKSzVyPUSuPUBvVQ>? NWHuOWNxOjV{NkO1N|k>
Rh30 NYHXcpc6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX64bI9WUUN3ME2zNU4yKG6P MWSyOVI3OzV|OR?=
BT-12 NWLsOoJmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4q3eGlEPTB-4pEJNUwxODBibl2= MV2yOVI3OzV|OR?=
CHLA-266 MlO3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorBTWM2OD8kgJmxMFAxOCCwTR?= M3G4RVI2OjZ|NUO5
TC-71 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TvUWlEPTB;Mz63JI5O NUHj[JE6OjV{NkO1N|k>
CHLA-9 NVTPRnF[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\5NHVKSzVyPUiuNkBvVQ>? NIHTdoYzPTJ4M{WzPS=>
CHLA-10 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4L6[GlEPTB;NkeuPEBvVQ>? NYPkbodLOjV{NkO1N|k>
CHLA-258 M1TQ[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\GcIlKSzVyPUSuOkBvVQ>? Mni0NlUzPjN3M{m=
SJ-GBM2 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fOUmlEPTB;MU[uNkBvVQ>? MVGyOVI3OzV|OR?=
NB-1643 M17RO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUXY[ZRZUUN3ME2xPE41KG6P M3PvRVI2OjZ|NUO5
NB-EBc1 NWDMV2lkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnvTWM2OD1{NT64JI5O NX24eGtNOjV{NkO1N|k>
CHLA-90 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnGR5VLUUN3ME9ihKkyNDByMDDuUS=> NX\MR4pUOjV{NkO1N|k>
CHLA-136 M4jVNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XxZWlEPTB;MUSuNkBvVQ>? MVGyOVI3OzV|OR?=
NALM-6 NIL0TXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTR7IH7N MlHENlUzPjN3M{m=
COG-LL-317 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoSxTWM2OD17LkSgcm0> MUmyOVI3OzV|OR?=
RS4;11 NIG0U5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVe1bW17UUN3ME21Nk43KG6P NGD5UYczPTJ4M{WzPS=>
MOLT-4 NHTrOXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTF4Lk[gcm0> MYiyOVI3OzV|OR?=
CCRF-CEM NVHsdJAzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnO1TWM2OD14OUeuN{BvVQ>? MmHyNlUzPjN3M{m=
Kasumi-1 M{ntWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG[wZmFKSzVyPUe4Ok4zKG6P MljLNlUzPjN3M{m=
Karpas-299 M2rlSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDFWWtKSzVyPUe1Mlchdk1? NX[2dlZFOjV{NkO1N|k>
Ramos-RA1 MnnoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDhTWM2OD14OD6zJI5O M3;ZSVI2OjZ|NUO5
DT40 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHnnWZNKSzVyPUSgcm0> MUSyOFM2PjhzMx?=
DU145 NY\meHhpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXLJR|UxRTFzIH7N M1O1N|I1OzV4OEGz
H209 MlrTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDifGtKSzVyPUGuO{BvVQ>? Mn[2NlQxPzd|NUC=
H1048 NFLaVVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4D0NGlEPTB;Mj6yJI5O NIrxR|MzPDB5N{O1NC=>
H524 Mn3XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTrTmpGUUN3ME2zMlEhdk1? MXuyOFA4PzN3MB?=
H1930 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTRwMTDuUS=> MUeyOFA4PzN3MB?=
H69 NELROGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPTcXVKSzVyPUWuNkBvVQ>? NF3aNZYzPDB5N{O1NC=>
H2081 MojtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYGweo1tUUN3ME22MlMhdk1? M2D6e|I1ODd5M{Ww
H2107 M3fhN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;r[GRGUUN3ME23MlMhdk1? NX2y[XhHOjRyN{ezOVA>
H1092 NWrqSmtkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVHsTY5nUUN3ME24Mlkhdk1? M3TqclI1ODd5M{Ww
DMS-79 NVHKdoxOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTlwMzDuUS=> M1LhbFI1ODd5M{Ww
H446 NVvBPXVLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLkNXVKSzVyPUGzJI5O M4GyOlI1ODd5M{Ww
COR-L279 MlW5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEe4T3RKSzVyPUG1JI5O Mo\vNlQxPzd|NUC=

... 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