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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Notes:

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.
Targets
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 NEH6elNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fYZlAvOS1zMECgcm0> MnXqNlQwPDhxN{KgbC=> Ml;jbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViZHXw[Y5l\W62bIm= M1HhfFI3ODR5Nkm3
BR5FVB1-Akt MoXURZBweHSxc3nzJGF{e2G7 MmTCNE4yNTFyMDDuUS=> NIXsTXA4OiCq Moq0bY5lfWOnczDhdI9xfG:|aYO= MmHwNlYxPDd4OUe=
Capan-1 NH:0fVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzUeWVKSzVyPUG2MlDjiIoEsfMAjVUvPOLCidM1UeKh M{XlNlI2QDZ2NUmw
MIA PaCa-2 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PzZmlEPTB;NUiuNlPjiIoEsfMAjVgvOeLCidM1UeKh NXXBU5RDOjV6NkS1PVA>
RD MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWrUdol4UUN3ME24Mlchdk1? M1[3VVI2OjZ|NUO5
Rh41 NIrneZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXTWGZKSzVyPUiuNUBvVQ>? MUWyOVI3OzV|OR?=
Rh18 NEDhbFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPoRoRKSzVyPUSuPUBvVQ>? NUXofFZSOjV{NkO1N|k>
Rh30 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXDRZJwUUN3ME2zNU4yKG6P NIKxSokzPTJ4M{WzPS=>
BT-12 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXLJR|UxRuLCiUGsNFAxKG6P NX7ydWJIOjV{NkO1N|k>
CHLA-266 MlvRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRuLCiUGsNFAxKG6P MXuyOVI3OzV|OR?=
TC-71 M4TNdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTNwNzDuUS=> MmjsNlUzPjN3M{m=
CHLA-9 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDpTWM2OD16LkKgcm0> NFXqN2UzPTJ4M{WzPS=>
CHLA-10 M{HUOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{PIU2lEPTB;NkeuPEBvVQ>? MYWyOVI3OzV|OR?=
CHLA-258 M374fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnnqTWM2OD12Lk[gcm0> NGPBN3IzPTJ4M{WzPS=>
SJ-GBM2 NVzFWFJ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nKV2lEPTB;MU[uNkBvVQ>? MkjiNlUzPjN3M{m=
NB-1643 MlvkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2T3SGlEPTB;MUiuOEBvVQ>? MWWyOVI3OzV|OR?=
NB-EBc1 NFOwRXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTJ3Lkigcm0> M1fCWVI2OjZ|NUO5
CHLA-90 MnvmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRuLCiUGsNFAxKG6P M4TjRlI2OjZ|NUO5
CHLA-136 NH\HcY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYX3WW52UUN3ME2xOE4zKG6P MlLrNlUzPjN3M{m=
NALM-6 NXLRcIdLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TnRmlEPTB;NEmgcm0> MXyyOVI3OzV|OR?=
COG-LL-317 M{\XTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\EV4hKSzVyPUmuOEBvVQ>? MkPjNlUzPjN3M{m=
RS4;11 NFLnOIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3v0fmlEPTB;NUKuOkBvVQ>? Mn\xNlUzPjN3M{m=
MOLT-4 MoPBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPiTWM2OD1zNj62JI5O Mke0NlUzPjN3M{m=
CCRF-CEM NEHqUXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX24fWJDUUN3ME22PVcvOyCwTR?= NYHYVmFROjV{NkO1N|k>
Kasumi-1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXpTYJKSzVyPUe4Ok4zKG6P NXLLRoROOjV{NkO1N|k>
Karpas-299 M13yUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HrW2lEPTB;N{WuO{BvVQ>? NIjMfW0zPTJ4M{WzPS=>
Ramos-RA1 MlX1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7XTWM2OD14OD6zJI5O M3jRS|I2OjZ|NUO5
DT40 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvUSpAzUUN3ME20JI5O NGnGXZozPDN3NkixNy=>
DU145 NEO1T5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXixOZlFUUN3ME2xNUBvVQ>? MkXnNlQ{PTZ6MUO=
H209 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV7He2xHUUN3ME2xMlchdk1? MlzSNlQxPzd|NUC=
H1048 NFy5fYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGH1cGhKSzVyPUKuNkBvVQ>? MnPDNlQxPzd|NUC=
H524 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGK2fHhKSzVyPUOuNUBvVQ>? MX:yOFA4PzN3MB?=
H1930 M4nMOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVX4N29YUUN3ME20MlEhdk1? M2fBblI1ODd5M{Ww
H69 M1:zWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTVwMjDuUS=> MkXFNlQxPzd|NUC=
H2081 MnX3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3MNWxKSzVyPU[uN{BvVQ>? NIXPU|QzPDB5N{O1NC=>
H2107 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoraTWM2OD15LkOgcm0> MXWyOFA4PzN3MB?=
H1092 NG[5RoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\u[WlEPTB;OD65JI5O NXXJcW1ROjRyN{ezOVA>
DMS-79 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXEOlZKSzVyPUmuN{BvVQ>? MXWyOFA4PzN3MB?=
H446 NEPMcoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3UcGNKSzVyPUGzJI5O NWDsT2NlOjRyN{ezOVA>
COR-L279 NVHtNVIyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofkTWM2OD1zNTDuUS=> MmnlNlQxPzd|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]

Protocol

Solubility (25°C)

In vitro DMSO 38 mg/mL warmed (99.9 mM)
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
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
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