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Talazoparib tosylate

Talazoparib tosylate
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Talazoparib tosylate

Catalog No. T16979Cas No. 1373431-65-2
Talazoparib tosylate is a novel and potent PARP1/2 (n IC50: 0.57 nM for PARP1).
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Pack SizePriceAvailabilityQuantity
2 mg$447-10 days
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Product Introduction

Bioactivity
Description
Talazoparib tosylate is a novel and potent PARP1/2 (n IC50: 0.57 nM for PARP1).
In vitro
Talazoparib inhibits PARP1 and -2 to a similar extent (Kis: 1.20 and 0.85 nM, respectively). Talazoparib induces nuclear γ-H2AX foci at concentrations as low as 100 pM. Talazoparib has no effect on PARG activity at concentrations up to 1 μM. Talazoparib binds to PARP1 with a dissociation constant of 0.29 nM. 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 or BRCA2-deficient are profoundly sensitive to Talazoparib. [1].
In vivo
Talazoparib is readily orally bioavailable, with more than 40% absolute oral bioavailability in rats when dosed in carboxymethyl cellulose. Talazoparib (p.o.) 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 [1].
AliasBMN 673ts
Chemical Properties
Molecular Weight552.55
FormulaC26H22F2N6O4S
Cas No.1373431-65-2
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 108 mg/mL (195.46 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.8098 mL9.0490 mL18.0979 mL90.4895 mL
5 mM0.3620 mL1.8098 mL3.6196 mL18.0979 mL
10 mM0.1810 mL0.9049 mL1.8098 mL9.0490 mL
20 mM0.0905 mL0.4524 mL0.9049 mL4.5245 mL
50 mM0.0362 mL0.1810 mL0.3620 mL1.8098 mL
100 mM0.0181 mL0.0905 mL0.1810 mL0.9049 mL

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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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