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 0.58 nM 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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3 Customer Reviews

  • PARP inhibition prevents adhesion to and migration of monocytes across BMVEC monolayers preserving the barrier. Primary human monocytes were treated for 24 h with PARPi (AIQ, olaparib, EB47, talazoparib), calcein-labeled, washed, and then added to BMVEC monolayers (untreated or treated for 24 h with TNFα). Treatments were removed prior to the addition of monocytes. Adhesion to (a) and migration of (b) monocytes across blood-brain barrier models were measured and are presented as fold difference compared to TNFα-only control (mean ± SEM) for each treatment from at least quadruplicate determinations, which was assigned a value of 1 (7600 relative fluorescent units for adhesion or equivalent to 37 migrated cells). *P < 0.05, **P < 0.01 indicate significance vs. non-treated. TEER, an indicator of barrier integrity, was continuously measured in BMVEC monolayers treated with or without TNFα following the addition of primary human monocytes that had been treated with PARPi.

    J Neuroinflammation, 2016, 13(1):254.. Talazoparib (BMN 673) purchased from Selleck.

    BT-549 cells reconstituted with Vet, WT, 336* or PTEN WT HP1aKD were treated with BMN673. Relative cell viability was determined by MTT assay. The results were presented as mean of 3 independent experiments. Error bars indicate s.d.

    Cell Cycle, 2015, 14(14): 2323-32. Talazoparib (BMN 673) purchased from Selleck.

  • We treated the FA defective and control lung cancer cell lines H1299D2-down/H1299E and A549D2 down/A549E with BMN673 (0.5 µM). MTT assay was used for the cell viability analysis and an averaged absorbance was recorded 24, 48 and 72 h post treatment.

    Front Oncol, 2014, 4: 368. Talazoparib (BMN 673) purchased from Selleck.

Purity & Quality Control

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2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description Talazoparib (BMN 673) is a novel PARP inhibitor with IC50 of 0.58 nM 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.
PARP [1]
(Cell-free assay)
0.58 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 NGi1SnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljCNE4yNTFyMDDuUS=> M{jHN|I1NzR6L{eyJIg> MWjpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36g[I9{\SCmZYDlcoRmdnSueR?= Mm\5NlYxPDd4OUe=
BR5FVB1-Akt NH\NR|ZCeG:ydH;zbZMhSXO|YYm= MnnrNE4yNTFyMDDuUS=> NYPuZ2l7PzJiaB?= NGHQVVVqdmS3Y3XzJIFxd3C2b4Ppdy=> NWnUZpZKOjZyNEe2PVc>
Capan-1 NWHWSY1pT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MljSTWM2OD1zNj6w5qCKyrIkgJm1MlTjiIoEtV5CpC=> NYiycmtGOjV6NkS1PVA>
MIA PaCa-2 NXPt[ZZuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\LTWM2OD13OD6yN-KBkcLz4pEJPE4y6oDLwsXNxsA> NHzjfWczPTh4NEW5NC=>
RD MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRThwNzDuUS=> NYDYfnh2OjV{NkO1N|k>
Rh41 NEj4dXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2OxOmlEPTB;OD6xJI5O NIjkeVczPTJ4M{WzPS=>
Rh18 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRTRwOTDuUS=> MmHnNlUzPjN3M{m=
Rh30 MlvUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvxblBKSzVyPUOxMlEhdk1? MVOyOVI3OzV|OR?=
BT-12 MkHxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRuLCiUGsNFAxKG6P NUfUPWNKOjV{NkO1N|k>
CHLA-266 M2XYXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRuLCiUGsNFAxKG6P NUjIfIRVOjV{NkO1N|k>
TC-71 NIjzb4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTNwNzDuUS=> NXf2bGw2OjV{NkO1N|k>
CHLA-9 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3Tj[WlEPTB;OD6yJI5O MXOyOVI3OzV|OR?=
CHLA-10 M1;DcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfkSmJKSzVyPU[3Mlghdk1? MmTTNlUzPjN3M{m=
CHLA-258 M1LPR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTRwNjDuUS=> NEHHeGYzPTJ4M{WzPS=>
NB-1643 NILsU2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2L2b2lEPTB;MUiuOEBvVQ>? MoHYNlUzPjN3M{m=
NB-EBc1 M1HrWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnv4TWM2OD1{NT64JI5O M1i4[VI2OjZ|NUO5
CHLA-90 MkLrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTVfYtVUUN3ME9ihKkyNDByMDDuUS=> NFq2WpozPTJ4M{WzPS=>
CHLA-136 Mn2zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTyTWM2OD1zND6yJI5O NFz5XZYzPTJ4M{WzPS=>
NALM-6 MmOyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrHTWM2OD12OTDuUS=> M37GeFI2OjZ|NUO5
COG-LL-317 NWnHWZpUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkW0TWM2OD17LkSgcm0> NUfUNY97OjV{NkO1N|k>
RS4;11 M2DmO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jCcWlEPTB;NUKuOkBvVQ>? NFXlVoIzPTJ4M{WzPS=>
MOLT-4 NV36XIhmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3udIFVUUN3ME2xOk43KG6P MmjpNlUzPjN3M{m=
CCRF-CEM Mn20S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\4TWM2OD14OUeuN{BvVQ>? MkP6NlUzPjN3M{m=
Kasumi-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjVfVh7UUN3ME23PFYvOiCwTR?= NW[0N3hDOjV{NkO1N|k>
Karpas-299 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGezdXlKSzVyPUe1Mlchdk1? NXnDOFkxOjV{NkO1N|k>
Ramos-RA1 NWHwRZhpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTZ6LkOgcm0> NUXz[3RkOjV{NkO1N|k>
DT40 NVL4VpRHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHuwTFNKSzVyPUSgcm0> NGO5WIUzPDN3NkixNy=>
DU145 M4DkUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnqwTWM2OD1zMTDuUS=> MYOyOFM2PjhzMx?=
H209 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWrM[|k4UUN3ME2xMlchdk1? MW[yOFA4PzN3MB?=
H1048 MlzlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\p[5NKSzVyPUKuNkBvVQ>? M4i5[|I1ODd5M{Ww
H524 NWPrN2JqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M325NGlEPTB;Mz6xJI5O NXTvTXRjOjRyN{ezOVA>
H1930 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1Ls[GlEPTB;ND6xJI5O NGS3UXYzPDB5N{O1NC=>
H69 MnzOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\X[nRKSzVyPUWuNkBvVQ>? NHjCZmIzPDB5N{O1NC=>
H2081 M1zve2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTZwMzDuUS=> MmryNlQxPzd|NUC=
H2107 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDzUm9KSzVyPUeuN{BvVQ>? NVz4e3RFOjRyN{ezOVA>
H1092 NHf4U5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmm1TWM2OD16Lkmgcm0> M3;aT|I1ODd5M{Ww
DMS-79 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjUTWM2OD17LkOgcm0> NXLLdXpvOjRyN{ezOVA>
H446 MnXkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF:yXmRKSzVyPUGzJI5O NFH5eI0zPDB5N{O1NC=>
COR-L279 M1PNXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTF3IH7N MnTuNlQxPzd|NUC=

... Click to View More Cell Line Experimental Data

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]


Solubility (25°C)

In vitro DMSO 38 mg/mL (99.9 mM) warming
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo

* 1 mg/ml means slightly soluble or 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


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
NCT01989546 Active, not recruiting Advanced Ovarian Cancer|Primary Peritoneal Cancer|Advanced Breast Cancer|Advanced Solid Tumors National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) November 8, 2013 Phase 1|Phase 2
NCT02286687 Active, not recruiting Advanced Cancers M.D. Anderson Cancer Center|BioMarin Pharmaceutical December 22, 2014 Phase 2
NCT02997163 Not yet recruiting Advanced Solid Tumors Medivation, Inc. January 2017 Phase 1
NCT02997176 Recruiting Advanced Solid Tumors Medivation, Inc. November 2016 Phase 1
NCT03042910 Recruiting Solid Tumor Medivation, Inc. October 2016 Phase 1
NCT02836028 Withdrawn Ovarian Cancer Medivation, Inc.|Myriad Genetic Laboratories, Inc. October 2016 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID