| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
5F-203 targets the aryl hydrocarbon receptor (AhR), a ligand-activated transcription factor involved in xenobiotic metabolism and cell proliferation. Upon binding to AhR, 5F-203 induces CYP1A1 expression, which leads to bioactivation and formation of DNA adducts. This results in DNA damage, cell cycle arrest, and tumor-specific cytotoxicity. The compound selectively targets cancer cells expressing AhR.
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| ln Vitro |
In vitro, 5F-203 is potently cytotoxic against sensitive human breast cancer cell lines and exhibits selective toxicity, sparing nonmalignant cells. It forms DNA adducts that lead to cell death. The compound induces aryl hydrocarbon receptor signaling and elevates CYP1A1 expression. It also increases reactive oxygen species levels. 5F-203 has shown efficacy in breast, ovarian, and gastric cancer models.
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| ln Vivo |
In vivo, 5F-203 has shown efficacy in breast, ovarian, and gastric cancer models. However, specific in vivo efficacy data in animal models are not detailed in the provided literature. The compound’s unique mechanism—AhR-mediated activation followed by DNA interaction—supports its potential in developing targeted cancer therapies with minimal off-target toxicity.
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| Enzyme Assay |
The in vitro enzyme/receptor binding assay for 5F-203 involves measuring its binding affinity to the aryl hydrocarbon receptor (AhR). This is typically done using competitive binding assays with radiolabeled AhR ligands. The compound’s ability to induce CYP1A1 expression is also measured as a functional readout of AhR activation.
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| Cell Assay |
In vitro cell-based assays for 5F-203 involve treating cancer cell lines with the compound and assessing cell viability, DNA damage (comet assay, γ-H2AX foci), and oxidative stress (ROS levels). CYP1A1 induction is measured by qPCR or Western blot. The compound’s selective toxicity against cancer cells versus nonmalignant cells is a key endpoint.
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| Animal Protocol |
In vivo animal studies for 5F-203 would likely involve xenograft mouse models of breast, ovarian, or gastric cancer. Tumor-bearing mice would be treated with 5F-203, and tumor growth inhibition would be monitored. Biomarkers of AhR activation and DNA damage would be assessed in tumor tissues.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of 5F-203 are not detailed in the provided literature. As a small molecule, it is expected to be orally bioavailable.
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| Toxicity/Toxicokinetics |
No specific toxicity data for 5F-203 are available in the provided literature. As a DNA-damaging agent, potential genotoxicity and off-target effects would need to be evaluated. The compound is for research use only.
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| References |
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| Additional Infomation |
5F-203 is a research compound targeting the aryl hydrocarbon receptor for cancer therapy. It is a benzothiazole derivative. It induces CYP1A1 expression and DNA damage. It is for research use only. Its CAS number is 260443-89-8.
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| Molecular Formula |
C14H11N2FS
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|---|---|
| Molecular Weight |
258.31394
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| Exact Mass |
258.063
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| CAS # |
260443-89-8
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| PubChem CID |
396813
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
4.574
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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 |
1
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| Heavy Atom Count |
18
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| Complexity |
302
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
IFWLHIIUGSEKKE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H11FN2S/c1-8-6-9(2-4-11(8)16)14-17-12-7-10(15)3-5-13(12)18-14/h2-7H,16H2,1H3
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| Chemical Name |
4-(5-fluoro-1,3-benzothiazol-2-yl)-2-methylaniline
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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 (~387.13 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.68 mM) (saturation unknown) 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.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.8713 mL | 19.3566 mL | 38.7132 mL | |
| 5 mM | 0.7743 mL | 3.8713 mL | 7.7426 mL | |
| 10 mM | 0.3871 mL | 1.9357 mL | 3.8713 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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