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

Talazoparib tosylate (Synonyms: BMN 673ts)

Cat. No.: HY-108413 Purity: 99.72%
Handling Instructions

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

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

Talazoparib tosylate Chemical Structure

Talazoparib tosylate Chemical Structure

CAS No. : 1373431-65-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 85 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  

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Customer Review

Based on 30 publication(s) in Google Scholar

Other Forms of Talazoparib tosylate:

Top Publications Citing Use of Products

    Talazoparib tosylate purchased from MCE. Usage Cited in: EBioMedicine. 2020 Sep;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 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].

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

    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].

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

    Clinical Trial
    Molecular Weight

    552.55

    Formula

    C₂₆H₂₂F₂N₆O₄S

    CAS No.

    1373431-65-2

    SMILES

    O=C1NN=C2C3=C1C=C(F)C=C3N[[email protected]](C4=CC=C(F)C=C4)[[email protected]]2C5=NC=NN5C.O=S(C6=CC=C(C)C=C6)(O)=O

    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 : ≥ 108 mg/mL (195.46 mM)

    *"≥" 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
    10 mM 0.1810 mL 0.9049 mL 1.8098 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 (4.52 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

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

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [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 has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [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 has not independently confirmed the accuracy of these methods. They are for reference only.

    References
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    Keywords:

    TalazoparibBMN 673tsPARPpoly ADP ribose polymeraseInhibitorinhibitorinhibit

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    Product Name:
    Talazoparib tosylate
    Cat. No.:
    HY-108413
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