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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4 Customer Reviews

  • Western blot assessment of effects on PAR, PARP, and dsDNA breaks mediated by IMMU-132 plus PARPi in TNBC tumor lines. Cells were plated overnight in 6-well plates before the addition of chemotherapeutics. After a 24-hour incubation, cells were harvested and cell lysates resolved and transferred for Western analysis as described in Materials and Methods. PAR and FL-PARP levels were determined on the same gel. Assessment of dsDNA breaks (p-H2A.X) was calculated as ratios relative to untreated control (Unt) normalized to b-actin protein loading control (Dp-H2A.X). B, HCC1806 cells exposed to rucaparib (Ruc) and IMMU-132 or to (C) talazoparib (Tala) and IMMU-132.

    Clin Cancer Res, 2017. Talazoparib (BMN 673) purchased from Selleck.

    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.

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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 NWW2blJ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEGwcYcxNjFvMUCwJI5O MWiyOE81QC95MjDo MnXvbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViZHXw[Y5l\W62bIm= MW[yOlA1PzZ7Nx?=
BR5FVB1-Akt NEH1RWNCeG:ydH;zbZMhSXO|YYm= NGjORWMxNjFvMUCwJI5O MVe3NkBp M2m3d4lv\HWlZYOgZZBweHSxc3nz M2jpVFI3ODR5Nkm3
Capan-1 NYnZS5BYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlm4TWM2OD1zNj6w5qCKyrIkgJm1MlTjiIoEtV5CpC=> MYqyOVg3PDV7MB?=
MIA PaCa-2 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rjR2lEPTB;NUiuNlPjiIoEsfMAjVgvOeLCidM1UeKh NUC0NG53OjV6NkS1PVA>
RD NFvCTWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRThwNzDuUS=> Mk\kNlUzPjN3M{m=
Rh41 M3m0TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXwV4ZKSzVyPUiuNUBvVQ>? NF7yTpozPTJ4M{WzPS=>
Rh18 NX7hXIFJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYW1N|YzUUN3ME20Mlkhdk1? NG\QUXAzPTJ4M{WzPS=>
Rh30 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVX0bIV1UUN3ME2zNU4yKG6P M1;yeFI2OjZ|NUO5
BT-12 MkjsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHvafohKSzVyPvMAjVEtODByIH7N M1XOdlI2OjZ|NUO5
CHLA-266 Ml7BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\MeWhKSzVyPvMAjVEtODByIH7N NYC2S3NVOjV{NkO1N|k>
TC-71 NHXMeXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjuTWM2OD1|Lkegcm0> NF6zTXAzPTJ4M{WzPS=>
CHLA-9 NEHhfppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Moi1TWM2OD16LkKgcm0> M1fFUFI2OjZ|NUO5
CHLA-10 NGLiSHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIX1b5hKSzVyPU[3Mlghdk1? NXjqfGJsOjV{NkO1N|k>
CHLA-258 NUf4c|hyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUC1dWRHUUN3ME20MlYhdk1? NWXmeIlyOjV{NkO1N|k>
SJ-GBM2 NFvIXIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\NWWlEPTB;MU[uNkBvVQ>? MUCyOVI3OzV|OR?=
NB-1643 NVPIb5BYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXTVXBKSzVyPUG4MlQhdk1? NUTt[YlJOjV{NkO1N|k>
NB-EBc1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXPWFBKSzVyPUK1Mlghdk1? MV[yOVI3OzV|OR?=
CHLA-90 MlfaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk[yTWM2OD8kgJmxMFAxOCCwTR?= NV;WPY9wOjV{NkO1N|k>
CHLA-136 MojKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTUbFVKSzVyPUG0MlIhdk1? MlzYNlUzPjN3M{m=
NALM-6 NYnxU2Y6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHvxbVhKSzVyPUS5JI5O MnLONlUzPjN3M{m=
COG-LL-317 NILPTWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmTITWM2OD17LkSgcm0> MVmyOVI3OzV|OR?=
RS4;11 NEDJdGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nXcWlEPTB;NUKuOkBvVQ>? NHHyTJIzPTJ4M{WzPS=>
MOLT-4 MoHZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTF4Lk[gcm0> M{D0dlI2OjZ|NUO5
CCRF-CEM NGPpOY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFPre2RKSzVyPU[5O{4{KG6P Ml\wNlUzPjN3M{m=
Kasumi-1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTd6Nj6yJI5O MV2yOVI3OzV|OR?=
Karpas-299 NWXlUXVmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4Xzb2lEPTB;N{WuO{BvVQ>? NGTxTmEzPTJ4M{WzPS=>
Ramos-RA1 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\YNIVKSzVyPU[4MlMhdk1? M{XLeFI2OjZ|NUO5
DT40 NISyTHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXVSW5HUUN3ME20JI5O M3KyOVI1OzV4OEGz
DU145 NWPTfIVST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDMTWM2OD1zMTDuUS=> Mn32NlQ{PTZ6MUO=
H209 MmrsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTFwNzDuUS=> MnHzNlQxPzd|NUC=
H1048 NUXzPJk1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\odGlEPTB;Mj6yJI5O MWGyOFA4PzN3MB?=
H524 M4TscGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXITY1KSzVyPUOuNUBvVQ>? NGjhbVUzPDB5N{O1NC=>
H1930 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\CW2lEPTB;ND6xJI5O M2HCc|I1ODd5M{Ww
H69 NEnrfI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTVwMjDuUS=> MX:yOFA4PzN3MB?=
H2081 Ml:zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmH5TWM2OD14LkOgcm0> M2fX[lI1ODd5M{Ww
H2107 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTmdHBKSzVyPUeuN{BvVQ>? M{ezflI1ODd5M{Ww
H1092 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFrMenhKSzVyPUiuPUBvVQ>? NF20clIzPDB5N{O1NC=>
DMS-79 Ml\FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jzPGlEPTB;OT6zJI5O MWOyOFA4PzN3MB?=
H446 M{XCWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDxPJV7UUN3ME2xN{BvVQ>? M{PheVI1ODd5M{Ww
COR-L279 NUDJb|V5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIryeW1KSzVyPUG1JI5O MUiyOFA4PzN3MB?=

... 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