| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg | |||
| Other Sizes |
| Targets |
TNKS1 (tankyrase 1) and TNKS2 (tankyrase 2), members of the poly(ADP-ribose) polymerase (PARP) family. Tankyrase-IN-2 is a selective, potent, and orally active inhibitor of tankyrase with IC50s of 10 nM for TNKS1 and 7 nM for TNKS2. It also inhibits PARP1 with an IC50 of 710 nM. Tankyrases are involved in Wnt/beta-catenin signaling, telomere maintenance, and mitotic progression.
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| ln Vitro |
Tankyrase-IN-2 (1-10000 nM; 24 hours) generates a dose-dependent increase in Tankyrase protein abundance in DLD1 cells with an EC50 of 320 nM. This is in the same potency range as the increase in axin2 (EC50=319 nM) [1].
In vitro, Tankyrase-IN-2 leads to a dose-dependent increase of tankyrase protein abundance in DLD1 colorectal cancer cells with an EC50 of 320 nM. This is in the same potency range as the value for axin2 increase with an EC50 of 319 nM. The compound exhibits nanomolar inhibitory activity and strong selectivity over other PARP enzymes. It is widely used in cancer and stem cell research to study Wnt pathway regulation, telomere dynamics, and therapeutic strategies targeting tankyrase-dependent oncogenic signaling. |
| ln Vivo |
In vivo, Tankyrase-IN-2 has been studied in animal models for its anticancer activity. The compound is orally active and has favorable physicochemical and pharmacokinetic properties that modulate pathway activity in colorectal cancer xenograft models. It is used to study the role of tankyrase in Wnt/beta-catenin signaling and its potential as a therapeutic target in cancer. The compound's in vivo efficacy supports its potential as a therapeutic agent for tankyrase-dependent cancers.
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| Enzyme Assay |
In vitro tankyrase inhibition assays for Tankyrase-IN-2 measure inhibition of tankyrase PARsylation activity. The assay uses recombinant human TNKS1 or TNKS2 enzyme and a substrate (e.g., auto-PARsylation or a peptide substrate) in the presence of NAD+. The compound is serially diluted in assay buffer and pre-incubated with the enzyme. The reaction is initiated by adding NAD+ and substrate, and after incubation, PARsylation is detected using either radiometric (32P-NAD+) or non-radiometric (HTRF, AlphaScreen, or ELISA) methods. IC50 values are calculated from dose-response curves.
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| Cell Assay |
In vitro cell-based assays for Tankyrase-IN-2 use DLD-1 colorectal cancer cells or other cell lines expressing tankyrase. Cells are cultured in appropriate media and treated with varying concentrations of the compound (1-10000 nM) for 24 hours. Tankyrase protein abundance and Axin2 accumulation are measured by Western blotting. EC50 values are calculated from dose-response curves. The compound's effect on Wnt/beta-catenin signaling can be assessed by measuring beta-catenin levels and downstream target gene expression.
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| Animal Protocol |
In vivo animal studies for Tankyrase-IN-2 are conducted in colorectal cancer xenograft models. Immunodeficient mice are implanted subcutaneously with DLD-1 or other colorectal cancer cells. When tumors reach a certain size, animals are randomized to receive vehicle control or Tankyrase-IN-2 at various doses (typically 1-30 mg/kg) via oral administration, daily or twice daily. Tumor volumes are measured with calipers every 2-3 days, and tumor growth inhibition is calculated. Tumor tissues are analyzed for tankyrase, Axin2, and beta-catenin levels by Western blotting or immunohistochemistry.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Tankyrase-IN-2 have been characterized in preclinical species. With a molecular weight of 316.30 and a molecular formula of C17H14F2N2O2, the compound is orally active and has favorable physicochemical properties. It is soluble in DMSO. The compound is stored as a powder at -20degC for up to 3 years or in solution at -80degC for up to 1 year. Standard pharmacokinetic parameters (Cmax, Tmax, AUC, oral bioavailability) have been determined in preclinical species.
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| Toxicity/Toxicokinetics |
Tankyrase-IN-2 is intended for research use only and is not for human therapeutic use. Standard safety precautions for handling chemical compounds apply. The compound is not approved for clinical use.
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| References | |
| Additional Infomation |
Tankyrase-IN-2 is a research-grade selective, potent, and orally active tankyrase inhibitor. It has a molecular formula of C17H14F2N2O2 and a molecular weight of 316.30. The compound inhibits TNKS1, TNKS2, and PARP1 with IC50s of 10, 7, and 710 nM, respectively. It is widely used in cancer and stem cell research to study Wnt pathway regulation, telomere dynamics, and therapeutic strategies targeting tankyrase-dependent oncogenic signaling. Not approved for clinical use.
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| Molecular Formula |
C17H14F2N2O2
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|---|---|
| Molecular Weight |
316.302071094513
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| Exact Mass |
316.102
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| CAS # |
1588870-36-3
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| PubChem CID |
136236981
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| Appearance |
White to off-white solid powder
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| LogP |
2.3
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
23
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| Complexity |
501
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1=CC(=CC2C(NC(C3C=CC(=CC=3)C(C)(C)O)=NC=21)=O)F
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| InChi Key |
FHBYLOWAINBPRJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H14F2N2O2/c1-17(2,23)10-5-3-9(4-6-10)15-20-14-12(16(22)21-15)7-11(18)8-13(14)19/h3-8,23H,1-2H3,(H,20,21,22)
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| Chemical Name |
6,8-difluoro-2-[4-(2-hydroxypropan-2-yl)phenyl]-3H-quinazolin-4-one
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~83.33 mg/mL (~263.45 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.58 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1616 mL | 15.8078 mL | 31.6156 mL | |
| 5 mM | 0.6323 mL | 3.1616 mL | 6.3231 mL | |
| 10 mM | 0.3162 mL | 1.5808 mL | 3.1616 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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