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.

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

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

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

Choose Selective PARP Inhibitors

Click to view more

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 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=>
SJ-GBM2 NVzL[Zd5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPMSVd{UUN3ME2xOk4zKG6P M4TNNVI2OjZ|NUO5
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]

Protocol

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
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
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

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

PARP Signaling Pathway Map

PARP Inhibitors with Unique Features

Related PARP Products

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