| Size | Price | Stock | Qty |
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| 10mg |
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| Targets |
β-catenin-IN-2 directly targets β-catenin, a key transcriptional co-activator in the Wnt signaling pathway that plays a crucial role in cell adhesion, gene transcription, and regulation of cell growth and differentiation.
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| ln Vitro |
In HCT116 cells, β-catenin/Tcf-4 transcriptional activity is dose-dependently inhibited by β-catenin-IN-2 (10–40 μM) [1].
In HCT116 colorectal cancer cells, β-catenin-IN-2 (10-40 μM) dose-dependently suppresses the transcriptional activity of the β-catenin/Tcf-4 complex, demonstrating its potent inhibitory effect on β-catenin-mediated transcription. |
| ln Vivo |
In vivo efficacy studies for β-catenin-IN-2 have shown potential in relevant cancer models, particularly in colorectal cancer research. The compound demonstrates significant biological activity in various cancer models characterized by dysregulated Wnt signaling.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for β-catenin-IN-2 typically involve cell-free systems to assess direct binding to β-catenin or its interaction with Tcf-4. Surface plasmon resonance or fluorescence polarization-based binding assays can be employed to determine the binding affinity (Kd) of the compound to purified β-catenin protein.
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| Cell Assay |
For in vitro cellular experiments, β-catenin-IN-2 is dissolved in DMSO and diluted in cell culture medium. HCT116 or other colorectal cancer cell lines are treated with the compound at concentrations ranging from 10-40 μM. Transcriptional activity is measured using luciferase reporter assays with β-catenin/Tcf-4 responsive elements. Cell viability and proliferation can be assessed using standard MTT or CCK-8 assays.
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| Animal Protocol |
For in vivo animal experiments, β-catenin-IN-2 is typically formulated in suitable vehicles such as PBS, carboxymethyl cellulose, or PEG400 for administration to mouse xenograft models. Tumor-bearing mice are dosed orally or intraperitoneally, and tumor growth inhibition, body weight, and survival are monitored. Tumor tissues are collected for immunohistochemical analysis of β-catenin pathway biomarkers.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of β-catenin-IN-2 have not been extensively reported in the public domain. The compound has a molecular weight of 255.29 g/mol and a molecular formula of C₁₅H₁₄FN₃. Standard PK studies would typically assess parameters such as half-life, clearance, volume of distribution, and bioavailability in rodent models.
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| Toxicity/Toxicokinetics |
The compound has a molecular weight of 255.29, a molecular formula of C₁₅H₁₄FN₃, and a CAS number of 1458664-10-2. Toxicological data for β-catenin-IN-2 is limited to research applications. As an experimental compound, it is not intended for human therapeutic use. Standard laboratory safety practices should be observed during handling.
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| References | |
| Additional Infomation |
β-catenin-IN-2 is a potent inhibitor of β-catenin that can be used in colorectal cancer research. It is a valuable tool compound for studying the Wnt/β-catenin signaling pathway and its role in cancer biology. The compound has not entered clinical trials or received regulatory approval for any therapeutic indication.
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| Molecular Formula |
C15H14FN3
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|---|---|
| Molecular Weight |
255.290166378021
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| Exact Mass |
255.117
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| CAS # |
1458664-10-2
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| PubChem CID |
60979451
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| Appearance |
Pink to red solid powder
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| LogP |
3.5
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
19
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| Complexity |
302
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1C=CC2=C(C=1)NC(C1C=CC(=CC=1)N(C)C)=N2
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| InChi Key |
ALWZHAOGGMSYPG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H14FN3/c1-19(2)12-6-3-10(4-7-12)15-17-13-8-5-11(16)9-14(13)18-15/h3-9H,1-2H3,(H,17,18)
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| Chemical Name |
4-(6-fluoro-1H-benzimidazol-2-yl)-N,N-dimethylaniline
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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 (326.41 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.15 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 | 3.9171 mL | 19.5856 mL | 39.1711 mL | |
| 5 mM | 0.7834 mL | 3.9171 mL | 7.8342 mL | |
| 10 mM | 0.3917 mL | 1.9586 mL | 3.9171 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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