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

Talazoparib tosylate (BMN 673ts) is a novel, potent and orally available PARP1/2 inhibitor with an IC50 of 0.57 nM for PARP1.

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CAS No. : 1373431-65-2

Size Prix Stock Quantité
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 En stock
Solution
10 mM * 1 mL in DMSO En stock
Solid
5 mg En stock
10 mg En stock
50 mg En stock
100 mg En stock
200 mg En stock
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Based on 98 publication(s) in Google Scholar

Other Forms of Talazoparib tosylate:

Talazoparib tosylate Related Antibodies

Top Publications Citing Use of Products

98 Publications Citing Use of MCE Talazoparib tosylate

2D/3D Cell Culture and Differentiation
Cell Proliferation/Viability Assay
Cell Imaging/Staining
In Vivo Efficacy Study
WB

    Talazoparib tosylate purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2022 Aug 5;12(8):1904-1921.  [Abstract]

    Talazoparib (0.33 mg/kg, p.o., 70 days) diminished ascites accumulation and extended survival by ~30% in mice bearing ATX-sufficient OvCa.

    Talazoparib tosylate purchased from MedChemExpress. Usage Cited in: Nat Cancer. 2022 Oct;3(10):1211-1227.  [Abstract]

    Representative images of clonogenic assay results in PARP inhibitor (PARPi)-resistant OVCA433 cell in the presence of the indicated inhibitor for 12 d. ALKi, ALK inhibitor; LOR, Lorlatinib (250-500 nM); TALA, Talazoparib (100-200 nM); Comb, combination of Lorlatinib and Talazoparib.

    Talazoparib tosylate purchased from MedChemExpress. Usage Cited in: Nat Cancer. 2022 Oct;3(10):1211-1227.  [Abstract]

    Representative images of RAD51 with EdU/DAPI staining in OVCA433 cell treated with 0.25 μM PARP inhibitor (PARPi; Talazoparib) or 0.5 μM ALK inhibitor (ALKi; Lorlatinib), either alone or in combination, for 48 h.

    Talazoparib tosylate purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2020 Dec 14;38(6):844-856.e7.  [Abstract]

    Talazoparib (0.1–1250 nM, 5 days) suppressed the viability of CXorf67-WT and -KO Daoy C67 cells.

    Talazoparib tosylate purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2020 Dec 14;38(6):844-856.e7.  [Abstract]

    Talazoparib (5 nM, 0.5 or 24 h) combined with IR (2 Gy) resulted in further increases in γ-H2AX foci.

    Talazoparib tosylate purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2020 Dec 14;38(6):844-856.e7.  [Abstract]

    Talazoparib (0.33 mg/kg, p.o., once a day for 5 days per week for 84 days) inhibited tumor growth in C67-KO and C67-re-expressing Daoy cells xenograft tumor models.

    Talazoparib tosylate 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.

    Voir tous les produits spécifiques à Isoform PARP:

    Voir toutes les isoformes
    PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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    Description

    Talazoparib tosylate (BMN 673ts) is a novel, potent and orally available PARP1/2 inhibitor with an IC50 of 0.57 nM for PARP1.

    IC50 & Target

    IC50: 0.57 nM (PARP1)[1]
    In Vitro

    Talazoparib is a potent PARP1/2 inhibitor (PARP1 IC50=0.57 nM), it has no effect on PARG activity at concentrations up to 1 μM. Talazoparib binds to PARP1 with a dissociation constant (KD) of 0.29 nM. Talazoparib inhibits PARP1 and -2 to a similar extent, with Kis of 1.20 and 0.85 nM, respectively. Talazoparib selectively targets tumor cells with BRCA1, BRCA2, or PTEN gene defects with 20- to more than 200-fold greater potency than existing PARP1/2 inhibitors. Talazoparib targets tumor cells with homologous recombination gene defects. Tumor models that are either BRCA1-deficient (MX-1 and SUM149) or BRCA2-deficient (Capan-1) are profoundly sensitive to Talazoparib. Talazoparib induces nuclear γ-H2AX foci at concentrations as low as 100 pM[1].

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

    Talazoparib tosylate Related Antibodies
    In Vivo

    Talazoparib 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. Synergistic or additive antitumor effects are also found when Talazoparib is combined with temozolomide, SN38, or platinum drugs[1].

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

    552.55

    Formule

    C26H22F2N6O4S
    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.O=S(C6=CC=C(C)C=C6)(O)=O
    Livraison

    Room temperature in continental US; may vary elsewhere.
    Stockage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvant et solubilité
    In Vitro: 

    DMSO : ≥ 108 mg/mL (195.46 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8098 mL 9.0490 mL 18.0979 mL
    5 mM 0.3620 mL 1.8098 mL 3.6196 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Calculateur de molarité

    • Calculateur de dilution

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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 (4.52 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:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (4.52 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    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).

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    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.
    Pureté et documentation

    Purity: 99.92%

    SDS (644 KB)

    COA (259 KB) HNMR (268 KB) LCMS (92 KB)

    Instruction de manipulation (2659 KB)
    Références
    Test cellulaire
    [1]

    LoVo cells are treated with Talazoparib (10, 40 nM) and temozolomide (TMZ) either alone or in combination for 5 days. Surviving fraction is determined using CellTiter-Glo assay.[1]

    MCE n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.
    Administration animale
    [1]

    Mice[1]

    In single-agent studies, olaparib (100 mg/kg), Talazoparib (0.33 or 0.1 mg/kg/d), or vehicle (10% DMAc, 6% Solutol, and 84% PBS) is administered by oral gavage (per os), once daily or Talazoparib (0.165 mg/kg) twice daily for 28 consecutive days. Mice are continuously monitored for 10 more days after last day of dosing[1].

    MCE n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.
    Références

    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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.8098 mL 9.0490 mL 18.0979 mL 45.2448 mL
    5 mM 0.3620 mL 1.8098 mL 3.6196 mL 9.0490 mL
    10 mM 0.1810 mL 0.9049 mL 1.8098 mL 4.5245 mL
    15 mM 0.1207 mL 0.6033 mL 1.2065 mL 3.0163 mL
    20 mM 0.0905 mL 0.4524 mL 0.9049 mL 2.2622 mL
    25 mM 0.0724 mL 0.3620 mL 0.7239 mL 1.8098 mL
    30 mM 0.0603 mL 0.3016 mL 0.6033 mL 1.5082 mL
    40 mM 0.0452 mL 0.2262 mL 0.4524 mL 1.1311 mL
    50 mM 0.0362 mL 0.1810 mL 0.3620 mL 0.9049 mL
    60 mM 0.0302 mL 0.1508 mL 0.3016 mL 0.7541 mL
    80 mM 0.0226 mL 0.1131 mL 0.2262 mL 0.5656 mL
    100 mM 0.0181 mL 0.0905 mL 0.1810 mL 0.4524 mL
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    Talazoparib tosylate 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:

    Talazoparib1373431-65-2BMN 673tsPARPpoly ADP ribose polymeraseInhibitorinhibitorinhibit

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