| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg | |||
| Other Sizes |
| Targets |
IC50: 2.65 µM (FOXM1)[1]
The primary target of FOXM1-IN-1 is the transcription factor FOXM1. By inhibiting FOXM1, the compound reduces the expression of its downstream target genes, including PLK1 (Polo-like kinase 1) and CDC25B (cell division cycle 25B). These targets are critical regulators of G2/M cell cycle transition and mitotic progression. |
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| ln Vitro |
In SKOV3 cells, the expression of FOXM1, PLK1, and CDC25B proteins is decreased by FOXM1-IN-1 (0-10 μg/mL; 24 h) [1].
In vitro, FOXM1-IN-1 shows potent antiproliferative activity against several cancer cell lines. It has demonstrated antiproliferative activity with IC50s of 15.06 microM for HepG2 (liver cancer) cells and 2.69 microM for HCT116 (colorectal cancer) cells. The compound effectively decreases FOXM1 expression and the expression of its downstream targets in a dose-dependent manner. |
| ln Vivo |
Specific in vivo activity data for FOXM1-IN-1 is not available in the provided search results. Based on its mechanism as an oncogene inhibitor, it is expected to be tested in mouse xenograft models of cancer (e.g., colorectal or liver) to assess its ability to slow tumor growth and prolong survival when administered orally or intraperitoneally.
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| Enzyme Assay |
A non-cellular biochemical assay is not feasible for a transcription factor inhibitor. The mechanism is typically validated by assessing protein levels. However, a DNA-binding ELISA (TransAM assay) can be used. Nuclear extracts from cells are incubated with an oligonucleotide containing the FOXM1 consensus DNA binding site. FOXM1-IN-1 is added to the mix, and the amount of bound transcription factor is detected with a FOXM1-specific antibody, quantifying the compound‘s ability to disrupt DNA binding.
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: HepG2, HCT116 cells Tested Concentrations: 0-100 µM Incubation Duration: 24 h Experimental Results: demonstrated antiproliferative activity with IC50s of 15.06, 2.69 µM for HepG2, HCT116 cells, respectively. Western Blot Analysis[1] Cell Types: SKOV3 cells Tested Concentrations: 0-10 μg/mL Incubation Duration: 24 h Experimental Results: diminished the expression of FOXM1, PLK1, CDC25B protein in a dose dependent manner. The primary in vitro cellular assay is a Western blot. SKOV3 ovarian cancer cells are treated with FOXM1-IN-1 at concentrations ranging from 0-10 microg/mL for 24 hours. The cells are then lysed, and protein lysates are separated by SDS-PAGE. The membrane is probed with primary antibodies against FOXM1, PLK1, and CDC25B, as well as a loading control (e.g., GAPDH or beta-actin). Densitometry is used to quantify the reduction in target protein expression levels relative to the untreated control. |
| Animal Protocol |
A protocol for a cell proliferation assay (MTT or CCK-8) is also standard. HepG2 or HCT116 cells are seeded in 96-well plates (1-5 × 103 cells/well). After 24 hours, the cells are treated with FOXM1-IN-1 at a range of concentrations (0-100 uM) for 72 hours. Cell viability is measured using a colorimetric MTT/CCK-8 assay, and the IC50 value (e.g., 15.06 uM for HepG2, 2.69 uM for HCT116) is calculated by fitting a dose-response curve.
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| ADME/Pharmacokinetics |
A typical xenograft protocol for an FOXM1 inhibitor would be as follows: Female BALB/c nude mice are injected subcutaneously in the right flank with 5 × 10⁶ HCT116 cells. When tumors reach approximately 100-200 mm3, the mice are randomized into treatment groups (n=8-10/group). FOXM1-IN-1 would be administered daily at doses of 10-50 mg/kg, either orally (p.o.) or intraperitoneally (i.p.), for 14-21 days. Tumor volumes (length × width2/2) are measured every 2-3 days using calipers, and body weights are recorded. At the end of the study, tumors are excised and weighed.
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| Toxicity/Toxicokinetics |
Dedicated PK data for FOXM1-IN-1 is not available. As a small molecule with MW 403.94 (C23H30ClNO3), it is moderately lipophilic (LogP ~5.2). It is soluble in DMSO and would likely be formulated for in vivo studies using a vehicle like 10% DMSO in corn oil. The oral bioavailability and plasma half-life would need to be experimentally determined; however, based on related compounds, it is expected to be moderately stable and distributed.
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| References |
[1]. Gao Y, et al. Synthesis and antineoplastic activity of ethylene glycol phenyl aminoethyl ether derivatives as FOXM1 inhibitors. Eur J Med Chem. 2022 Dec 15;244:114877.
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| Additional Infomation |
Specific toxicity data for FOXM1-IN-1 is not provided. As an inhibitor of a cell cycle transcription factor, it is expected to be cytotoxic to proliferating cells. Its antiproliferative activity in cancer cells (IC50 as low as 2.69 uM) suggests it would be toxic to normal rapidly dividing cells (e.g., bone marrow, gut epithelium) if administered systemically. This limits its therapeutic window, which is typical for cytotoxic agents.
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| Molecular Formula |
C23H30CLNO3
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|---|---|
| Molecular Weight |
403.942205905914
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| Exact Mass |
403.191
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| CAS # |
2864407-22-5
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| PubChem CID |
166177028
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| Appearance |
White to off-white solid powder
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| LogP |
5.2
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
28
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| Complexity |
389
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1C=CC(=CC=1)COC1C=CC(=CC=1)OCCOCCNC1CCCCC1
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| InChi Key |
RKTLOUYERGLRCM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H30ClNO3/c24-20-8-6-19(7-9-20)18-28-23-12-10-22(11-13-23)27-17-16-26-15-14-25-21-4-2-1-3-5-21/h6-13,21,25H,1-5,14-18H2
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| Chemical Name |
N-[2-[2-[4-[(4-chlorophenyl)methoxy]phenoxy]ethoxy]ethyl]cyclohexanamine
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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: ~100 mg/mL (~247.6 mM; with ultrasonication and warming by heating to 160°C)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.19 mM) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (6.19 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4756 mL | 12.3781 mL | 24.7562 mL | |
| 5 mM | 0.4951 mL | 2.4756 mL | 4.9512 mL | |
| 10 mM | 0.2476 mL | 1.2378 mL | 2.4756 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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