| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
YW2036 targets the Wnt/β-catenin signaling pathway, inhibiting β-catenin-mediated transcriptional activity.
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| ln Vitro |
YW2036 inhibits the Wnt/β-catenin signaling pathway with an IC₅₀ value of 637 nM as determined in Wnt-HEK293 luciferase reporter gene assays. It demonstrates significant biological activity in research focused on colorectal cancer.
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| ln Vivo |
YW2036 has demonstrated in vivo potential in cancer research, particularly in studies concerning colorectal cancer. The compound has shown efficacy in preclinical models and is being evaluated for its therapeutic potential.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for YW2036 are not typically performed as it is a cell-based pathway inhibitor. However, binding to β-catenin or other Wnt pathway components could be assessed using surface plasmon resonance or isothermal titration calorimetry. The compound's mechanism of action is evaluated through cell-based reporter assays rather than direct enzyme binding.
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| Cell Assay |
For in vitro cellular experiments, YW2036 is dissolved in DMSO and diluted in cell culture medium. HEK293 cells stably transfected with Wnt-responsive luciferase reporter constructs are treated with the compound at various concentrations. Wnt signaling activity is measured by luciferase activity, and IC₅₀ values are determined from dose-response curves. Colorectal cancer cell lines are treated with YW2036 to assess effects on cell proliferation, migration, and expression of Wnt target genes.
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| Animal Protocol |
For in vivo animal experiments, YW2036 is formulated in suitable vehicles such as PBS, carboxymethyl cellulose, or PEG400 for administration to mouse models. Xenograft models of colorectal cancer are established, and the compound is administered orally or intraperitoneally. Tumor growth inhibition, body weight, and survival are monitored. Tumor tissues are collected for immunohistochemical analysis of Wnt/β-catenin pathway biomarkers and assessment of target engagement.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of YW2036 have not been extensively reported. The compound has a molecular weight of 328.37 g/mol and a molecular formula of C₂₀H₁₆N₄O. Standard PK studies would assess parameters such as half-life, oral bioavailability, clearance, and tissue distribution in rodent models.
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| Toxicity/Toxicokinetics |
Toxicological data for YW2036 is limited to preclinical research settings. The compound is intended for laboratory use only and has not been evaluated for human therapeutic safety. Standard safety precautions should be observed during handling.
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| References | |
| Additional Infomation |
YW2036 (compound 2a) is a potent inhibitor of the Wnt/β-Catenin signaling pathway. It is a synthetic small molecule belonging to the pyrazole-4-carboxamide class. The compound is primarily used in research focused on colorectal cancer. No clinical trials or regulatory approvals have been reported.
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| CAS # |
2131223-92-0
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| Appearance |
White to off-white solid powder
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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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