| Size | Price | Stock | Qty |
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| 5mg |
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| 50mg |
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| Targets |
Late SV40 Factor (LSF/TFCP2). FQI1 is a selective, reversible inhibitor of the oncogenic transcription factor Late SV40 Factor (LSF/TFCP2). LSF is a ubiquitous transcription factor that is upregulated in many hepatocellular carcinomas (HCC). By inhibiting the DNA-binding activity of LSF, FQI1 blocks LSF-dependent transactivation and transcriptional activity. LSF plays a critical role in the regulation of cell growth and division, and its overexpression is associated with oncogenic transformation. FQI1 specifically targets the DNA-binding activity of LSF with an IC₅₀ of 2.1 μM.
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| ln Vitro |
FQI1 inhibits the DNA-binding activity of LSF with an IC₅₀ of 2.1 μM. It inhibits LSF-dependent luciferase reporter expression. The compound inhibits cell proliferation with IC₅₀ values of 3 μM for NIH/3T3 cells, 0.79 μM for HeLa cells, and 6.3 μM for A549 cells. FQI1 blocks proliferation in cancer cell lines and induces apoptosis in liver cancer cells but is not toxic to primary hepatocytes. The compound exhibits differential antiproliferative activity across multiple cancer cell lines.
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| ln Vivo |
FQI1 has been evaluated in vivo in mouse HCC xenograft models. At a dose of 1 mg/kg administered intraperitoneally every three days (q3d), FQI1 demonstrated tumor growth inhibition with no general cytotoxicity. The compound's ability to inhibit LSF-dependent transactivation and induce apoptosis in LSF-overexpressing cells supports its potential for cancer therapy. Further studies are needed to fully characterize its pharmacokinetic and pharmacodynamic properties.
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| Enzyme Assay |
Non-cell-based assays for FQI1 include LSF DNA-binding activity inhibition assays. The transcription factor LSF is incubated with its DNA target sequence in the presence of various concentrations of FQI1, and DNA-binding activity is measured using electrophoretic mobility shift assays (EMSA) or fluorescence polarization. The IC₅₀ value of 2.1 μM for LSF inhibition is determined from the dose-response curve. LSF-dependent luciferase reporter expression assays are used to assess transcriptional inhibition. Standard analytical methods including HPLC, NMR, and mass spectrometry are used for compound characterization.
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| Cell Assay |
Cell-based assays for FQI1 use various cancer cell lines to assess its antiproliferative activity. NIH/3T3, HeLa, and A549 cells are cultured and treated with FQI1 at various concentrations. Cell viability is measured using MTT or similar assays. Apoptosis is evaluated by flow cytometry using Annexin V/PI staining and detection of apoptotic markers. For liver cancer studies, HCC cell lines and primary hepatocytes are used to assess selective toxicity. LSF-dependent luciferase reporter expression is measured in transfected cells.
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| Animal Protocol |
In vivo studies of FQI1 have been conducted in mouse HCC xenograft models. Mice bearing hepatocellular carcinoma tumors are treated with FQI1 at 1 mg/kg via intraperitoneal injection every three days (q3d). Tumor volume is measured over time to assess growth inhibition. Tissue samples are collected for histopathological examination and biomarker analysis. The compound shows tumor growth inhibition with no general cytotoxicity. Further in vivo studies are needed to fully characterize its efficacy and safety profile.
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| ADME/Pharmacokinetics |
FQI1 has a molecular formula of C₁₈H₁₇NO₄ and a molecular weight of 311.33 g/mol. The chemical name is 8-(2-ethoxyphenyl)-7,8-dihydro-[1,3]dioxolo[4,5-g]quinolin-6(5H)-one. It appears as a solid powder with a white to beige color. The compound is soluble in DMSO (125 mg/mL, 401.50 mM). It should be stored as a powder at -20°C for up to 3 years or in solvent at -80°C for 6 months. Purity is ≥98%. It is intended for research use only.
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| Toxicity/Toxicokinetics |
Specific toxicity data for FQI1 are limited. The compound induces apoptosis in liver cancer cells but is not toxic to primary hepatocytes, suggesting some selectivity for cancer cells. In mouse HCC xenograft models, FQI1 at 1 mg/kg (i.p., q3d) showed tumor growth inhibition with no general cytotoxicity. Standard laboratory safety practices should be followed when handling this compound, including the use of personal protective equipment. It is intended for research use only.
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| References | |
| Additional Infomation |
Blocking the binding ability of late-stage SV-40 factor to the target promoter; structure as described in the first source.
FQI1 (Factor Quinolinone Inhibitor 1) is a cell-permeable dihydroquinolinone compound that functions as a selective, reversible inhibitor of the oncogenic transcription factor Late SV40 Factor (LSF/TFCP2). LSF is a ubiquitous transcription factor that is upregulated in many hepatocellular carcinomas (HCC). FQI1 inhibits LSF DNA-binding activity with an IC₅₀ of 2.1 μM and blocks LSF-dependent transactivation. The compound exhibits differential antiproliferative activity across multiple cancer cell lines and induces apoptosis in LSF-overexpressing cells including HCC cells. FQI1 has demonstrated tumor growth inhibition in mouse HCC xenograft models. It is for research use only. |
| Molecular Formula |
C18H17NO4
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|---|---|
| Molecular Weight |
311.33
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| Exact Mass |
311.116
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| CAS # |
599151-35-6
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| PubChem CID |
656346
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| Appearance |
White to light yellow solid powder
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| LogP |
3.373
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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 |
3
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| Heavy Atom Count |
23
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| Complexity |
443
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCOC1=CC=CC=C1C2CC(=O)NC3=CC4=C(C=C23)OCO4
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| InChi Key |
YKSYGLXHLSPWLB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H17NO4/c1-2-21-15-6-4-3-5-11(15)12-8-18(20)19-14-9-17-16(7-13(12)14)22-10-23-17/h3-7,9,12H,2,8,10H2,1H3,(H,19,20)
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| Chemical Name |
8-(2-ethoxyphenyl)-7,8-dihydro-5H-[1,3]dioxolo[4,5-g]quinolin-6-one
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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: 125 mg/mL (401.50 mM）
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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 | 3.2120 mL | 16.0601 mL | 32.1203 mL | |
| 5 mM | 0.6424 mL | 3.2120 mL | 6.4241 mL | |
| 10 mM | 0.3212 mL | 1.6060 mL | 3.2120 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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