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, orally available PARP1/2 inhibitor.Talazoparib inhibits PARP1 and PARP2 enzyme activity with Kis of 1.2 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

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10 mM * 1 mL in DMSO USD 77 In-stock
Estimated Time of Arrival: December 31
5 mg USD 70 In-stock
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10 mg USD 100 In-stock
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50 mg USD 250 In-stock
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100 mg USD 400 In-stock
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200 mg USD 550 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 26 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.
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    Description

    Talazoparib (BMN-673) is a highly potent, orally available PARP1/2 inhibitor.Talazoparib inhibits PARP1 and PARP2 enzyme activity with Kis of 1.2 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 cell (BRCA1 mutant), Capan-1 cell (BRCA2 mutant) and MRC-5 (normal )[1].

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

    In Vivo

    Talazoparib (0.33 mg/kg; i.g.; once daily; for 28 days) exhibits antitumor activity against a BRCA1 mutant breast cancer model in mice[1].
    Talazoparib (5mg/kg for i.v.; 10 mg/kg for p.o.) has oral bioactivity[1].

    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: Rat[1]
    Dosage: 5mg/kg (i.v.), 10 mg/kg (p.o.) (Pharmacokinetic Analysis)
    Administration: Intravenous injection, oral administration
    Result: T1/2=2.25 hours, Cmax=7948 ng/mL (p.o.), AUC= 56134 ng.h/mL (p.o.).
    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

    Purity: 99.89%

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    Keywords:

    TalazoparibBMN-673 LT-673BMN673BMN 673LT673LT 673LT-673PARPpoly ADP ribose polymeraseanticancerPARP-mediated PARylationBRCA1/2MX-1breast cancerInhibitorinhibitorinhibit

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