| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| ln Vitro |
Wnt/β-catenin-IN-6 (compound B10) (72 h) showed potent cytotoxic activity against the human non-small cell lung cancer cell line A549 (IC50 = 1.28 μM), with IC50 values of 3.74, 3.22 and 5.68 μM in SKOV3, MDAMB-231 and BEAS-2B cells, respectively [1]. Wnt/β-catenin-IN-6 (2, 4 μM, 48 h) showed potent antiproliferative activity by inhibiting the EGFR/Erk signaling pathway in A549 cells [1]. Wnt/β-catenin-IN-6 (4 μM, 72 h) induced only 10% apoptosis in A549 cells, which was not significantly different from the control group [1]. Wnt/β-catenin-IN-6 (2, 4 μM, 48 h) inhibited the Wnt/β-catenin signaling pathway in A549 cells through the AKT/GSK-3β/β-catenin axis [1]. Wnt/β-catenin-IN-6 (2, 4 μM, 48 h) downregulated the expression of IL-8 mRNA, c-Myc and c-Jun in A549 cells, indicating that it has anti-inflammatory effects [1].
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| ln Vivo |
Wnt/β-catenin-IN-6 (compound B10) (25 mg/kg, by gavage, every other day) showed significant anti-non-small cell lung cancer activity and good biocompatibility in an A549 xenograft model established in male BALB/C nude mice [1]. No significant toxicity was observed in ICR mice at doses up to 50 mg/kg with Wnt/β-catenin-IN-6 (12.5–50 mg/kg, by gavage, once). [1]
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| Cell Assay |
Western Blot Analysis [1]
Cell Types: A549 cells Tested Concentrations: 2, 4 μM Incubation Duration: 48 hours Experimental Results: Under basal conditions (without exogenous EGF), the phosphorylation levels of EGFR and Erk in A549 cells were reduced. In the presence of EGF, the expression of phosphorylated EGFR was significantly reduced, while the inhibitory effect on Erk phosphorylation was less significant. Western Blot Analysis [1] Cell Types: A549 cells Tested Concentrations: 2, 4 μM Incubation Duration: 48 hours Experimental Results: Significantly reduced COX2 expression in A549 cells. This led to a significant decrease in p-AKT levels and its ratio to AKT. It also significantly reduced p-GSK-3β levels and its ratio to GSK-3β, resulting in downregulation of active (non-phosphorylated) β-catenin. Real-time quantitative PCR[1] Cell Types: A549 cells Tested Concentrations: 2, 4 μM Incubation Duration: 48 h Experimental Results: Downregulation of IL-8 mRNA expression in A549 cells indicates its anti-inflammatory effect. Downregulation of c-Myc and c-Jun expression. |
| Animal Protocol |
Animal/Disease Models:A549 xenograft model established in male BALB/c nude mice (6 weeks old) [1]
Doses: 25 mg/kg Route of Administration: Intragastric instillation (ig) every other day Experimental Results: No significant changes in body weight were observed, indicating good systemic tolerability. No obvious pathological abnormalities were observed. Tumor growth was inhibited, and its tumor-suppressive effect was significantly stronger than that of gefitinib. Ki67 expression was significantly reduced, indicating effective inhibition of tumor cell proliferation. No obvious histopathological abnormalities were found. Animal/Disease Models:ICR mice (20 males, 20 females, 5-6 weeks old)[1] Doses: 12.5, 25, 50 mg/kg Route of Administration: Gavage (ig) Experimental Results: No significant weight loss was observed. No significant pathological abnormalities were observed. |
| References |
| Molecular Formula |
C25H22N4O3
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|---|---|
| Molecular Weight |
426.47
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| Appearance |
Light yellow to yellow solid
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| SMILES |
COC1=C(OCC2=CC=CC=C2)C=C(N=CN=C3NC4=CC=C(NC(C=C)=O)C=C4)C3=C1
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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 : ~5.83 mg/mL (~13.67 mM; ultrasonic and warming and heat to 60°C)
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3448 mL | 11.7242 mL | 23.4483 mL | |
| 5 mM | 0.4690 mL | 2.3448 mL | 4.6897 mL | |
| 10 mM | 0.2345 mL | 1.1724 mL | 2.3448 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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