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

Talazoparib tosylate (Synonyms: BMN 673ts)

Cat. No.: HY-108413 Purity: 99.74%
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

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10 mM * 1 mL in DMSO USD 85 In-stock
Estimated Time of Arrival: December 31
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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
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Customer Review

Based on 15 publication(s) in Google Scholar

Other Forms of Talazoparib tosylate:

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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].

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].

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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Talazoparib tosylate
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