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Tankyrase Inhibitors (TNKS) 22

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Catalog No. T23420

Tankyrase Inhibitors 22 is a potent, selective, and orally bioavailable inhibitor of tankyrase (IC50: 0.1nM).

Tankyrase Inhibitors (TNKS) 22

Tankyrase Inhibitors (TNKS) 22

😃Good
Catalog No. T23420
Tankyrase Inhibitors 22 is a potent, selective, and orally bioavailable inhibitor of tankyrase (IC50: 0.1nM).
Pack SizePriceAvailabilityQuantity
5 mg$189Backorder
10 mg$329Backorder
50 mg$888Backorder
100 mg$1,400Backorder
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Product Introduction

Bioactivity
Description
Tankyrase Inhibitors 22 is a potent, selective, and orally bioavailable inhibitor of tankyrase (IC50: 0.1nM).
In vitro
Tankyrase inhibitors 22 is an optimization of the previous hit compound inhibitor 8 with improved potency and selectivity. It has excellent effects in both tankyrase assay and cellular assay (IC50: 0.1nM and 3.7nM, respectively). In addition, it is found to be a dual binder with both the nicotinamide pocket and the induced pocket of the enzymes [1].
In vivo
In the in vivo studies in rodents, tankyrase inhibitors 22 is found to potently inhibit TNKS2 autoparsylation (IC50: 4.1nM). It also causes stabilization and accumulation of axin protein in SW480 cells (EC50: 3.9nM). In DLD-1 cells with truncated APC, the inhibitor inhibits the STF reporter transcription (IC50: 0.6nM) suggesting its downstream inhibitory activity on Wnt-associated transcription [1].
Chemical Properties
Molecular Weight475.56
FormulaC25H25N5O3S
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: <1 mg/mL

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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
For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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