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

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

Cat. No.: HY-16106 Purity: 99.64%
COA Handling Instructions

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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, orally active PARP1/2 inhibitor.Talazoparib inhibits PARP1 and PARP2 enzyme activity with Kis of 1.2 nM and 0.87 nM, respectively. Talazoparib has antitumor activity.

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
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 77 In-stock
Solution
10 mM * 1 mL in DMSO USD 77 In-stock
Solid
1 mg USD 28 In-stock
5 mg USD 70 In-stock
10 mg USD 100 In-stock
50 mg USD 250 In-stock
100 mg USD 400 In-stock
200 mg USD 550 In-stock
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Customer Review

Based on 70 publication(s) in Google Scholar

Other Forms of Talazoparib:

Talazoparib Related Antibodies

Top Publications Citing Use of Products

69 Publications Citing Use of MCE Talazoparib

WB

    Talazoparib purchased from MedChemExpress. Usage Cited in: EBioMedicine. 2020 Sep;59:102923.  [Abstract]

    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.

    View All PARP Isoform Specific Products:

    View All Isoforms
    PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Talazoparib (BMN-673) is a highly potent, orally active PARP1/2 inhibitor.Talazoparib inhibits PARP1 and PARP2 enzyme activity with Kis of 1.2 nM and 0.87 nM, respectively. Talazoparib has antitumor activity[1].

    IC50 & Target[1]

    PARP2

    0.87 nM (Ki)

    PARP1

    1.2 nM (Ki)

    In Vitro

    Talazoparib shows an EC50 of 2.51 nM in cellular PARylation assay[1].
    Talazoparib shows EC50s of 0.3 nM, 5 nM and 0.31 for MX-1 cells (BRCA1 mutant), Capan-1 cells (BRCA2 mutant) and MRC-5 cells (normal)[1].

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

    Talazoparib Related Antibodies
    In Vivo

    Talazoparib (0.33 mg/kg; i.g.; once daily; for 28 days) exhibits antitumor activity against BRCA1 mutant breast cancer model in mice[1].
    Talazoparib exhibits moderate oral bioavailability (rat 56%) and Cmax (rat 7948 ng/mL) following oral administration (rat 10 mg/kg)[1]. Talazoparib exhibits the terminal elimination half-life (rat 2.25 h) due to plasma clearance (2 mL/min/kg) following intravenous administration (rat 5 mg/kg)[1].

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

    Animal Model: Female athymic nu/nu mice (8-10 weeks old), with MX-1 xenograft-bearing mice[1]
    Dosage: 0.33 mg/kg
    Administration: Oral gavage, once daily, for 28 days
    Result: Significantly inhibited xenograft MX-1 tumor growth.
    Animal Model: Sprague-Dawley rats[1]
    Dosage: 5mg/kg for i.v.; 10 mg/kg for oral (Pharmacokinetic Analysis)
    Administration: Intravenous administration and oral administration
    Result: Oral bioavailability (56%), Cmax (7948 ng/mL), T1/2 (2.25 h).
    Clinical Trial
    Molecular Weight

    380.35

    Formula

    C19H14F2N6O
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C1NN=C2C3=C1C=C(F)C=C3N[C@H](C4=CC=C(F)C=C4)[C@H]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 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 25 mg/mL (65.73 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 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

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in Saline)

      Solubility: 1.25 mg/mL (3.29 mM); Suspended solution; Need ultrasonic

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMAc    6% Solutol HS-15    84% PBS

      Solubility: 5 mg/mL (13.15 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.89%

    COA (254 KB) LCMS (125 KB) Elemental Analysis Report (112 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.6292 mL 13.1458 mL 26.2916 mL 65.7289 mL
    5 mM 0.5258 mL 2.6292 mL 5.2583 mL 13.1458 mL
    10 mM 0.2629 mL 1.3146 mL 2.6292 mL 6.5729 mL
    15 mM 0.1753 mL 0.8764 mL 1.7528 mL 4.3819 mL
    20 mM 0.1315 mL 0.6573 mL 1.3146 mL 3.2864 mL
    25 mM 0.1052 mL 0.5258 mL 1.0517 mL 2.6292 mL
    30 mM 0.0876 mL 0.4382 mL 0.8764 mL 2.1910 mL
    40 mM 0.0657 mL 0.3286 mL 0.6573 mL 1.6432 mL
    50 mM 0.0526 mL 0.2629 mL 0.5258 mL 1.3146 mL
    60 mM 0.0438 mL 0.2191 mL 0.4382 mL 1.0955 mL
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    Talazoparib Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Talazoparib1207456-01-6BMN-673 LT-673BMN673BMN 673LT673LT 673LT-673PARPpoly ADP ribose polymeraseanticancerPARP-mediated PARylationBRCA1/2MX-1breast cancerInhibitorinhibitorinhibit

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