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.

Size Price Stock Quantity  
USD 470 In stock
USD 970 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

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, 23(13):3405-3415. 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.

Purity & Quality Control

Choose Selective PARP Inhibitors

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 NGnwPHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWGwMlEuOTByIH7N M{joVFI1NzR6L{eyJIg> NYjHfph7cW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> M{XXPVI3ODR5Nkm3
BR5FVB1-Akt NXO5VGZHSXCxcITvd4l{KEG|c3H5 MkewNE4yNTFyMDDuUS=> M2qzW|czKGh? M{TzbYlv\HWlZYOgZZBweHSxc3nz M4GxZlI3ODR5Nkm3
Capan-1 M2Kyemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fsd2lEPTB;MU[uNQKBkcLz4pEJOU416oDLwsXNxsA> NIH5VJczPTh4NEW5NC=>
MIA PaCa-2 M3TUN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrEVoZmUUN3ME21PE4zO+LCidMx5qCKQC5z4pEJxtVOyqB? MmPkNlU5PjR3OUC=
RD NH[zOIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\6TWM2OD16Lkegcm0> MmnqNlUzPjN3M{m=
Rh41 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRThwMTDuUS=> MkDDNlUzPjN3M{m=
Rh18 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\xT2FKSzVyPUSuPUBvVQ>? MX6yOVI3OzV|OR?=
Rh30 Mn7hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTNzLkGgcm0> MXWyOVI3OzV|OR?=
BT-12 NYTpOm9ZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MonaTWM2OD8kgJmxMFAxOCCwTR?= MnjTNlUzPjN3M{m=
CHLA-266 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33JZ2lEPTB-4pEJNUwxODBibl2= NFGzWJgzPTJ4M{WzPS=>
TC-71 NWewWHprT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzmVFhKSzVyPUOuO{BvVQ>? MlL2NlUzPjN3M{m=
CHLA-9 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnWwTWM2OD16LkKgcm0> MmTBNlUzPjN3M{m=
CHLA-10 NYPQVIFvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUToSFh6UUN3ME22O{45KG6P MYqyOVI3OzV|OR?=
CHLA-258 NETjVnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTRwNjDuUS=> MmnpNlUzPjN3M{m=
SJ-GBM2 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHKUXduUUN3ME2xOk4zKG6P MWmyOVI3OzV|OR?=
NB-1643 M{i2Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTF6LkSgcm0> M{XyWFI2OjZ|NUO5
NB-EBc1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVWx[JY{UUN3ME2yOU45KG6P M{HOSVI2OjZ|NUO5
CHLA-90 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjlVGRJUUN3ME9ihKkyNDByMDDuUS=> NHfrdIMzPTJ4M{WzPS=>
CHLA-136 Mo\RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrhTWM2OD1zND6yJI5O MVOyOVI3OzV|OR?=
NALM-6 NX;QZmhHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTR7IH7N NV\OOXM6OjV{NkO1N|k>
COG-LL-317 M1PZ[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGewS2lKSzVyPUmuOEBvVQ>? MUSyOVI3OzV|OR?=
RS4;11 M1HZZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HKRmlEPTB;NUKuOkBvVQ>? NIPUWYkzPTJ4M{WzPS=>
MOLT-4 Ml3iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjITWM2OD1zNj62JI5O MmrDNlUzPjN3M{m=
CCRF-CEM MniwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4T0[GlEPTB;Nkm3MlMhdk1? M13ubVI2OjZ|NUO5
Kasumi-1 NFi1eJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTd6Nj6yJI5O MVqyOVI3OzV|OR?=
Karpas-299 MlPnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rXeGlEPTB;N{WuO{BvVQ>? M1\aRVI2OjZ|NUO5
Ramos-RA1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\FUJZKSzVyPU[4MlMhdk1? Mly5NlUzPjN3M{m=
DT40 NYnlfIZIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHHbFlKSzVyPUSgcm0> NGTYNFIzPDN3NkixNy=>
DU145 NH\wNo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XY[2lEPTB;MUGgcm0> MmjtNlQ{PTZ6MUO=
H209 Mnn2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXPRZJoUUN3ME2xMlchdk1? NYnQPIk4OjRyN{ezOVA>
H1048 MnLrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkDvTWM2OD1{LkKgcm0> M{n1RlI1ODd5M{Ww
H524 NVWzeJZHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\0cXZuUUN3ME2zMlEhdk1? NWC2[3pqOjRyN{ezOVA>
H1930 NXfJNZZiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELLcZVKSzVyPUSuNUBvVQ>? NWLpRXp3OjRyN{ezOVA>
H69 NHPrbHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHe1e4FKSzVyPUWuNkBvVQ>? NXvlWIQ2OjRyN{ezOVA>
H2081 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rETGlEPTB;Nj6zJI5O MkL3NlQxPzd|NUC=
H2107 NVHmNnoyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTdwMzDuUS=> NWPXNYZGOjRyN{ezOVA>
H1092 MkOwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInQZoZKSzVyPUiuPUBvVQ>? NUnaXJBtOjRyN{ezOVA>
DMS-79 NYXFS2liT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3j2XGlEPTB;OT6zJI5O NIrENnczPDB5N{O1NC=>
H446 MmnZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\VXWlEPTB;MUOgcm0> NUTmengxOjRyN{ezOVA>
COR-L279 M1;QW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlO2TWM2OD1zNTDuUS=> NXHuOZk5OjRyN{ezOVA>

... 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

Animal Research:

[2]

+ Expand
  • 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

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03426254 Enrolling by invitation Advanced or Recurrent Solid Tumors|Breast Neoplasm Center Trials & Treatment|BioGene Pharmaceutical February 8 2018 Phase 1
NCT02997163 Recruiting Advanced Solid Tumors Pfizer|Medivation Inc. February 8 2017 Phase 1
NCT02921919 Recruiting Cancer Pfizer|Medivation Inc. November 8 2016 Phase 2
NCT03377556 Recruiting ATM Gene Mutation|ATR Gene Mutation|BARD1 Gene Mutation|BRCA1 Gene Mutation|BRCA2 Gene Mutation|BRIP1 Gene Mutation|CHEK1 Gene Mutation|CHEK2 Gene Mutation|FANCA Gene Mutation|FANCC Gene Mutation|FANCD2 Gene Mutation|FANCF Gene Mutation|FANCM Gene Mutation|NBN Gene Mutation|PALB2 Gene Mutation|RAD51 Gene Mutation|RAD51B Gene Mutation|RAD54L Gene Mutation|Recurrent Squamous Cell Lung Carcinoma|RPA1 Gene Mutation|Stage IV Squamous Cell Lung Carcinoma AJCC v7 Southwest Oncology Group|National Cancer Institute (NCI) February 7 2017 Phase 2
NCT03077607 Completed Advanced Solid Tumors Pfizer|Medivation Inc. November 7 2016 Phase 1
NCT03148795 Recruiting Prostate Cancer Pfizer|Medivation Inc. July 4 2017 Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

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"

PARP Signaling Pathway Map

PARP Inhibitors with Unique Features

Related PARP Products5

Tags: buy Talazoparib (BMN 673) | Talazoparib (BMN 673) supplier | purchase Talazoparib (BMN 673) | Talazoparib (BMN 673) cost | Talazoparib (BMN 673) manufacturer | order Talazoparib (BMN 673) | Talazoparib (BMN 673) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID