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

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

Cat. No.: HY-16106 Purity: 98.97%
COA 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 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

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

Based on 48 publication(s) in Google Scholar

Other Forms of Talazoparib:

Top Publications Citing Use of Products

47 Publications Citing Use of MCE Talazoparib

WB

    Talazoparib purchased from MCE. 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

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    • 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].

    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 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].

    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

    Appearance

    Solid

    Formula

    C19H14F2N6O
    CAS No.
    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 : 25 mg/mL (65.73 mM; Need ultrasonic)

    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% DMAC  6% Solutol HS-15   84% PBS

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

    • 2.

      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

    • 3.

      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

    • 4.

      Add each solvent one by one:  2% DMSO    40% PEG300    5% Tween-80    53% saline

      Solubility: ≥ 0.5 mg/mL (1.31 mM); Clear solution

    • 5.

      Add each solvent one by one:  1% DMSO    99% saline

      Solubility: ≥ 0.25 mg/mL (0.66 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.89%

    COA (254 KB) LCMS (125 KB)

    Handling Instructions (2659 KB)
    References
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    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.

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    Keywords:

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

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