| ln Vitro |
β-catenin-IN-10 (10 μM; 24 hours) can regulate the expression of Wnt and AR target genes in LNCaP-abl and LNCaP-95 prostate cancer cells, reduce the level of oncogenic target transcripts, and upregulate E-cadherin [1]. β-catenin-IN-10 (0.195-0.782 μM; 5 days) can effectively inhibit the proliferation of castration-resistant prostate cancer cells LNCaP-abl and LNCaP-95 in a two-dimensional culture system, with IC50 values of 0.195 μM and 0.782 μM for the two cell lines, respectively, but has no effect on non-prostate cancer cells, and this effect is independent of the Wnt signaling pathway [1]. β-catenin-IN-10 (0.694–1.34 μM; 17–22 d) inhibited the proliferation of LNCaP-abl prostate cancer spheroids in a 3D culture system; its IC50 was 0.694 μM when added at the time of inoculation and 1.34 μM when added to pre-formed spheroids[1].
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| ln Vivo |
β-catenin-IN-10 (compound 13) (10 μM; single dose) effectively inhibited the overactivated Wnt signaling pathway in zebrafish embryos, resulting in complete recovery of eye development in 100% of the treated embryos [1].
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| Cell Assay |
Real-time quantitative PCR[1]
Cell Types: LNCaP-abl and LNCaP-95 castration-resistant prostate cancer cells Tested Concentrations: 10 μM Incubation Duration: 24 hours Experimental Results: The mRNA levels of Wnt target genes (AR, cMYC, Cyclin D1), AR target genes (PSA, FKBP5), and constitutively active AR splice variant AR-V7 were decreased; the mRNA level of E-cadherin (a gene inhibited by Wnt signaling) was increased. Cell viability assay [1] Cell Types: LNCaP-abl, LNCaP-95, U2OS and A549 cells Tested Concentrations: 0.195 μM IC50 (LNCaP-abl); 0.782 μM IC50 (LNCaP-95); 0.001 to 100 μM (dose range) Incubation Duration: 5 days Experimental Results: The IC50 for inhibiting the proliferation of LNCaP-abl cells was 0.195 μM, and the IC50 for inhibiting the proliferation of LNCaP-95 cells was 0.782 μM; there was no effect on the proliferation of Wnt-independent U2OS (osteosarcoma) and A549 (lung adenocarcinoma) cells. Cell viability assay [1] Cell Types: LNCaP-abl prostate cancer cells Tested Concentrations: 0.694 μM IC50 (added on day 0); 1.34 μM IC50 (added on day 5); 0.001 to 100 μM (dose range); ≥1 μM (inhibits spheroid formation/growth arrest) Incubation Duration: 22 days in total (added on day 0, medium changed every 3-4 days); 17 days in total (added on day 5, medium changed every 3-4 days) Experimental Results: When added on day 0, the IC50 was 0.694 μM, which inhibited spheroid proliferation; when added to pre-formed spheroids on day 5, proliferation was inhibited, with an IC50 of 1.34 μM. A concentration ≥1 μM could prevent spheroid formation or inhibit the growth of pre-formed spheroids. |
| Animal Protocol |
Animal/Disease Models:Wild type (embryo) [1]
Doses: 10 μM Route of Administration: Immersion; Single administration 5.5 hours after fertilization Experimental Results: Eye development was saved in 100% of the embryos (8/8 embryos in each of the 3 independent experiments). |
| References |
| Molecular Formula |
C74H97N11O17
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|---|---|
| Molecular Weight |
1412.63
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| Appearance |
Typically exists as solids at room temperature
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.7079 mL | 3.5395 mL | 7.0790 mL | |
| 5 mM | 0.1416 mL | 0.7079 mL | 1.4158 mL | |
| 10 mM | 0.0708 mL | 0.3539 mL | 0.7079 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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