1. Cell Cycle/DNA Damage
    Epigenetics
  2. PARP
  3. Talazoparib

Talazoparib (Synonyms: BMN-673; LT-673)

Cat. No.: HY-16106 Purity: 99.89%
Handling Instructions

Talazoparib (BMN-673) est un inhibiteur très puissant de PARP1 / 2 avec des Kis de 1,2 nM et 0,87 nM, respectivement.

Talazoparib (BMN-673) ist ein hochwirksamer PARP1/2-Inhibitor mit Kis von 1,2 nM bzw. 0,87 nM.

Talazoparib (BMN-673) is a highly potent PARP1/2 inhibitor with Kis of 1.2 nM and 0.87 nM, respectively.

For research use only. We do not sell to patients.

Talazoparib Chemical Structure

Talazoparib Chemical Structure

CAS No. : 1207456-01-6

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 77 In-stock
Estimated Time of Arrival: December 31
5 mg USD 70 In-stock
Estimated Time of Arrival: December 31
10 mg USD 100 In-stock
Estimated Time of Arrival: December 31
50 mg USD 250 In-stock
Estimated Time of Arrival: December 31
100 mg USD 400 In-stock
Estimated Time of Arrival: December 31
200 mg USD 550 In-stock
Estimated Time of Arrival: December 31
500 mg   Get quote  
1 g   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 24 publication(s) in Google Scholar

Other Forms of Talazoparib:

Top Publications Citing Use of Products

    Talazoparib purchased from MCE. Usage Cited in: EBioMedicine. 2020 Aug 13;59:102923.

    Western Blot analyses of TP53, p21 and RAD51 in PARP inhibitor sensitive (SKCO1 and LS513) and resistant cell lines (SW1222 and SNU61) after treatment with Talazoparib for 48 h. Talazoparib decreases RAD51 protein expression in the two TP53 wild-type cell lines SKCO1 and LS513.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Talazoparib (BMN-673) is a highly potent PARP1/2 inhibitor with Kis of 1.2 nM and 0.87 nM, respectively[1].

    IC50 & Target

    PARP2

    0.87 nM (Ki)

    PARP1

    1.2 nM (Ki)

    In Vitro

    Talazoparib (BMN 673) demonstrates excellent potency, inhibiting PARP1 and PARP2 enzyme activity with Ki=1.2 and 0.87 nM, respectively[1]. Talazoparib (BMN 673) exhibits selective antitumor cytotoxicity and elicits DNA repair biomarkers at much lower concentrations than earlier generation PARP1/2 inhibitors (such as AZD2281, Rucaparib, and Veliparib)[2].

    In Vivo

    Talazoparib (BMN 673; 1 mg/kg, p.o.) is orally available, displaying favorable pharmacokinetic (PK) properties and remarkable antitumor efficacy in the BRCA1 mutant MX-1 breast cancer xenograft model following oral administration as a single-agent or in combination with chemotherapy agents such as NSC 362856 and CDDP[1]. Talazoparib (BMN 673) is readily orally bioavailable, with more than 40% absolute oral bioavailability in rats when dosed in carboxylmethyl cellulose. Oral administration of Talazoparib elicits remarkable antitumor activity, xenografted tumors that carry defects in DNA repair due to BRCA mutations or PTEN deficiency are profoundly sensitive to oral Talazoparib treatment at well-tolerated doses in mice[2].

    Clinical Trial
    Molecular Weight

    380.35

    Formula

    C₁₉H₁₄F₂N₆O

    CAS No.

    1207456-01-6

    SMILES

    O=C1NN=C2C3=C1C=C(F)C=C3N[[email protected]](C4=CC=C(F)C=C4)[[email protected]]2C5=NC=NN5C

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 33.33 mg/mL (87.63 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.6292 mL 13.1458 mL 26.2916 mL
    5 mM 0.5258 mL 2.6292 mL 5.2583 mL
    10 mM 0.2629 mL 1.3146 mL 2.6292 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (6.57 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Kinase Assay
    [1]

    The ability of a test compound to inhibit PARP1 enzyme activity is assessed using PARP1 assay kit. IC50 values are calculated using GraphPad Prism5 software. For PARP inhibitor Ki determination, enzyme assays are conducted in 96-well FlashPlate with 0.5 U of PARP1 enzyme, 0.25× activated DNA, 0.2 μCi [3H]NAD, and 5 μM cold NAD in a final volume of 50 μL in reaction buffer containing 10% glycerol (v/v), 25 mM HEPES, 12.5 mM MgCl2, 50 mM KCl, 1 mM dithiothreitol (DTT), and 0.01% NP-40 (v/v), pH 7.6. Reactions are initiated by adding NAD to the PARP reaction mixture with or without inhibitors and incubated for 1 min at room temperature. Fifty microliters of ice-cold 20% trichloroacetic acid (TCA) is then added to each well to quench the reaction. The plate is sealed and shaken for a further 120 min at room temperature, followed by centrifugation. Radioactive signal bound to the FlashPlate is determined using TopCount. PARP1 Km is determined using the Michaelis-Menten equation from various substrate concentrations (1-100 μM NAD). Compound Ki is calculated from the enzyme inhibition curve according to the following formula: Ki=IC50/[1+(substrate)/Km]. Km for PARP2 enzyme and compound Ki are determined with the same assay protocol except that 30 ng of PARP2, 0.25× activated DNA, 0.2 μCi [3H]NAD, and 20 μM cold NAD are used in the reaction for 30 min at room temperature[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [1]

    In single-agent assays, Capan-1 cells (BRCA2-deficient), MX-1 (BRCA1-deficient) cells, or other cultured cells are seeded at densities that allow linear growth for 10-12 days in 96-well plates (typically 500-3000 cells/well). Cells are treated in their recommended growth media containing varying concentrations of PARP inhibitors (Veliparib, Rucaparib, Niraparib, AZD2281, and Talazoparib) for 10-12 consecutive days (media are changed with fresh compounds every 5 days). IC50 values are calculated using GraphPad Prism5[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    Mice[1]
    MX-1 tumor xenografts are prepared. When tumors reach an average volume of approximately 150 mm3, AZD2281 (100 mg/kg), Talazoparib (1 mg/kg), or vehicle is administered in a single po dose. Tumors are harvested at 2, 8, and 24 h after drug dosing and snap-frozen in liquid nitrogen. Tumor tissue is then homogenized in PBS on ice and extracted with lysis buffer (25 mM Tris, pH 8.0, 150 mM NaCl, 5 mM EDTA, 2 mM EGTA, 25 mM NaF, 2 mM Na3VO4, 1 mM Pefabloc, 1% Triton X-100, and protease inhibitor cocktail) containing 1% SDS. Levels of PAR in the tumor lysates are determined by ELISA using PARP in vivo PD assay II kit.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Purity: 99.89%

    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.
    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

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

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Keywords:

    TalazoparibBMN-673LT-673BMN673BMN 673LT673LT 673PARPpoly ADP ribose polymeraseInhibitorinhibitorinhibit

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

     

    Salutation

    Applicant Name *

     

    Email address *

    Phone number *

     

    Organization name *

    Department *

     

    Requested quantity *

    Country or Region *

         

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    Talazoparib
    Cat. No.:
    HY-16106
    Quantity:
    MCE Japan Authorized Agent: