FOXM1-IN-3
Based on 1 Customer Validation
FOXM1-IN-3 is a potent FOXM1 inhibitor. FOXM1-IN-3 downregulates FOXM1 expression at protein and mRNA levels, suppressing downstream effectors CCNB1 and CDC25. FOXM1-IN-3 induces G2/M cell cycle arrest and apoptosis in colorectal cancer cells. FOXM1-IN-3 inhibits colony formation and cell migration in colorectal cancer cells. FOXM1-IN-3 targets the cancer stem cell phenotype in colorectal cancer cells, reducing cancer stem cell marker expression. FOXM1-IN-3 reduces tumor growth in a zebrafish xenograft model. FOXM1-IN-3 can be used for the research of colorectal cancer.
For research use only. We do not sell to patients.
- Purity : 99.59%
- Formula: C29H38ClN9O
- Molecular Weight:564.12
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Biological Activity
Description
IC50 & Target
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FOXM1 |
PI3Kγ 3.5 μM (IC50) |
In Vitro
FOXM1-IN-3 (compound 14) (6.25-100 μM; 24 h) potently inhibits proliferation in SW620 and SW480 colorectal cancer cells with IC50 values of 14.9 μM and 17.5 μM, respectively, and shows favorable selectivity over normal CCD841 cells (IC50 of 36.65 μM)[1].
FOXM1-IN-3 (0.75-3 μM; 7 days) almost completely inhibits colony formation in SW480 and SW620 cells at 3 μM, reflecting long-term antiproliferative effects[1].
FOXM1-IN-3 (6.25-25 μM; 48 h) suppresses cell migration in SW480 cells at 6.25 μM and in SW620 cells at 12.5 μM over 48 h[1].
FOXM1-IN-3 shows measurable inhibition of PI3Kβ, γ, and δ[1].
FOXM1-IN-3 (6.25-25 μM; 24 h) downregulates 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) causes G2/M phase arrest in SW480 and SW620 cells, correlating with FOXM1 downregulation[1].
FOXM1-IN-3 (6.25-25 μM; 24 h) induces apoptosis in SW480 and SW620 cells at 12.5 μM and 25 μM[1].
FOXM1-IN-3 (10 μM; 24 h, 48 h) selectively targets cancer stem cell (CSC) phenotypes in SW480 and SW620 cells at 10 μM, with mild and reversible effects on normal CCD841 cells[1].
FOXM1-IN-3 has high passive permeability, low CYP interference, notable hepatotoxicity (IC50 ~5.6 μM in HepG2), and lower neurotoxicity (IC50 ~17 μM in SH-SY5Y)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SW620, SW480, CCD841
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Concentration:100 μM, 50 μM, 25 μM, 12.5 μM, 6.25 μM
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Incubation Time:24 h
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Result:Demonstrated antiproliferative effects with IC₅₀ values of 14.9 μM (SW620), 17.5 μM (SW480), and 36.7 μM (CCD841), yielding selectivity indices of 2.1-2.5.
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Cell Line:SW480, SW620
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Concentration:25 μM, 12.5 μM, 6.25 μM
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Incubation Time:48 h
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Result:Significantly impaired migration ability, with inhibition observed at 6.25 μM in SW480 cells and at 12.5 μM in SW620 cells.
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Cell Line:SW480, SW620
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Concentration:25 μM, 12.5 μM, 6.25 μM
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Incubation Time:24 h
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Result:Induced a dose-dependent accumulation of cells in the G2/M phase along with a significant reduction in the S phase population in both cell lines.
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Cell Line:SW480, SW620
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Concentration:25 μM, 12.5 μM, 6.25 μM
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Incubation Time:24 h
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Result:Increased levels of both early and late apoptotic cells in a dose-dependent manner, particularly at 12.5 μM and 25 μM.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Zebrafish species Danio rerio (wild-type AB)[1]
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Dosage:5, 10 μM
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Administration:immersion; 72 hours
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Result:For SW620 xenografts, showed 85.06% tumor growth relative to control at 5 μM and 80.95% at 10 μM at 3 days post-injection (dpi).
For SW480 xenografts, showed 92.65% tumor growth relative to control at 5 μM and 90.05% at 10 μM at 3 dpi.
- RNA extraction experimental
- Cell migration
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Zigmond Chamber Chemotaxis Assay
- Under-Agarose Cell Migration Assay
- Transwell/Boyden Chamber Migration Assay
- Apoptosis Solutions
- 3D Collagen/Hydrogel Matrix Migration Assay
- Soft Agar Colony Formation Assay
- Cell-Exclusion Zone Migration Assay
- Dunn/Insall Chamber Chemotaxis Assay
- Scratch/Wound-Healing Migration Assay
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Neural Crest/Neuronal Cell Migration Explant Assay
- Patient-Derived Orthotopic Xenograft (PDOX)
- Protocol for Cell Cycle
- Colony Formation (Clonogenic) Assay
- Patient-Derived Xenograft (PDX)
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Intraperitoneal/Peritoneal Dissemination Xenograft
Chemical Information
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Appearance Solid
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Molecular Weight 564.12
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Formula C29H38ClN9O
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Color White to off-white
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SMILES
C1(NCCC2=CNC3=C2C=CC=C3)=NC(NCCN4CCN(C5=CC=CC=C5)CC4)=NC(N6CCOCC6)=N1.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro:
DMSO : 33.33 mg/mL (59.08 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.43 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.43 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7727 mL | 8.8634 mL | 17.7267 mL | 44.3168 mL |
| 5 mM | 0.3545 mL | 1.7727 mL | 3.5453 mL | 8.8634 mL | |
| 10 mM | 0.1773 mL | 0.8863 mL | 1.7727 mL | 4.4317 mL | |
| 15 mM | 0.1182 mL | 0.5909 mL | 1.1818 mL | 2.9545 mL | |
| 20 mM | 0.0886 mL | 0.4432 mL | 0.8863 mL | 2.2158 mL | |
| 25 mM | 0.0709 mL | 0.3545 mL | 0.7091 mL | 1.7727 mL | |
| 30 mM | 0.0591 mL | 0.2954 mL | 0.5909 mL | 1.4772 mL | |
| 40 mM | 0.0443 mL | 0.2216 mL | 0.4432 mL | 1.1079 mL | |
| 50 mM | 0.0355 mL | 0.1773 mL | 0.3545 mL | 0.8863 mL |