| ln Vitro |
FOXM1-IN-3 (compound 14) (6.25-100 μM; 24 hours) effectively inhibited the proliferation of SW620 and SW480 colorectal cancer cells, with IC50 values of 14.9 μM and 17.5 μM, respectively, and showed good selectivity for normal CCD841 cells (IC50 of 36.65 μM) [1]. FOXM1-IN-3 (0.75-3 μM; 7 days) almost completely inhibited the colony formation of SW480 and SW620 cells at a concentration of 3 μM, indicating that it has a long-term anti-proliferative effect [1]. FOXM1-IN-3 (6.25-25 μM; 48 hours) inhibited the migration of SW480 cells at a concentration of 6.25 μM and the migration of SW620 cells at a concentration of 12.5 μM [1]. FOXM1-IN-3 significantly inhibits the activity of PI3Kβ, γ and δ[1]. FOXM1-IN-3 (6.25-25 μM; 24 h) downregulated the expression of FOXM1 and its downstream effectors CCNB1 and CDC25 in SW480 and SW620 cells at concentrations as low as 6.25 μM[1]. FOXM1-IN-3 (6.25-25 μM; 24 h) caused G2/M phase arrest in SW480 and SW620 cells, which was associated with the downregulation of FOXM1[1]. FOXM1-IN-3 (6.25-25 μM; 24 h) induced apoptosis in SW480 and SW620 cells at concentrations of 12.5 μM and 25 μM[1]. FOXM1-IN-3 (10 μM; 24 h, 48 h) selectively targets the cancer stem cell (CSC) phenotype in SW480 and SW620 cells at a concentration of 10 μM, with minimal and reversible effects on normal CCD841 cells [1]. FOXM1-IN-3 exhibits high passive permeability, low CYP interference, significant hepatotoxicity (IC50 of approximately 5.6 μM in HepG2 cells), and low neurotoxicity (IC50 of approximately 17 μM in SH-SY5Y cells) [1].
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|---|---|
| ln Vivo |
FOXM1-IN-3 (compound 14) (5-10 μM; soaking; 72 hours) can inhibit tumor growth in zebrafish xenograft models, with the most significant effect in the SW620 strain (tumor growth was reduced by 80.95% compared to the control group at 10 μM) [1].
|
| Cell Assay |
Cell viability assay [1]
Cell Types: SW620, SW480, CCD841 Test concentrations: 100 μM, 50 μM, 25 μM, 12.5 μM, 6.25 μM Incubation Duration: 24 hours Experimental Results: Showed anti-proliferative effect, with IC₅₀ values of 14.9 μM (SW620), 17.5 μM (SW480) and 36.7 μM (CCD841), and selectivity indices of 2.1-2.5. Cell migration assay [1] Cell Types: SW480, SW620 Concentrations: 25 μM, 12.5 μM, 6.25 μM Incubation Duration: 48 hours Experimental Results: Migration ability was significantly impaired. Inhibition was observed in SW480 cells at 6.25 μM and in SW620 cells at 12.5 μM. Cell cycle analysis [1] Cell Types: SW480, SW620 Tested Concentrations: 25 μM, 12.5 μM, 6.25 μM Incubation Duration: 24 hours Experimental Results: In both cell lines, dose-dependent accumulation of G2/M phase cells was induced, while the number of S phase cells was significantly reduced.
|
| Animal Protocol |
Animal/Disease Models:Zebrafish (Danio rerio, wild-type AB)[1]
Doses: 5, 10 μM Route of Administration: Immersion; 72 hours Experimental Results: SW620 xenografts showed a tumor growth rate of 85.06% in the 5 μM group and 80.95% in the 10 μM group 3 days after injection (dpi). SW480 xenografts showed a tumor growth rate of 92.65% in the 5 μM group and 90.05% in the 10 μM group 3 days after injection (dpi). |
| References |
| Molecular Formula |
C29H38CLN9O
|
|---|---|
| Molecular Weight |
564.12
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
C1(NCCC2=CNC3=C2C=CC=C3)=NC(NCCN4CCN(C5=CC=CC=C5)CC4)=NC(N6CCOCC6)=N1.Cl
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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 | 1.7727 mL | 8.8634 mL | 17.7267 mL | |
| 5 mM | 0.3545 mL | 1.7727 mL | 3.5453 mL | |
| 10 mM | 0.1773 mL | 0.8863 mL | 1.7727 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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