| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 500mg | |||
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| Targets |
F7H targets Frizzled receptor FZD7, a member of the Frizzled family of G protein-coupled receptors that serve as receptors for Wnt ligands. FZD7 plays critical roles in embryonic development, tissue homeostasis, and cancer. F7H is a potent ligand for the FZD7 transmembrane domain (TMD) with an IC50 of 1.25 μM. By antagonizing FZD7, F7H modulates Wnt/β-catenin signaling, which is implicated in various cancers and inflammatory conditions.
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| ln Vitro |
In vitro, F7H acts as a potent Frizzled receptor FZD7 antagonist with an IC50 of 1.25 μM. It is a potent ligand for the FZD7 transmembrane domain (TMD). F7H exhibits potential antitumor and bacteriostatic activities through modulation of Wnt/β-catenin signaling. These in vitro properties make F7H a valuable tool for studying FZD7-mediated Wnt signaling and its role in cancer and infectious diseases.
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| ln Vivo |
In vivo activity of F7H has not been extensively reported. As a FZD7 antagonist with potential antitumor and bacteriostatic activities, it may have applications in cancer and infectious disease research. The compound's effects on Wnt/β-catenin signaling suggest potential for treating cancers driven by aberrant Wnt signaling. However, detailed in vivo efficacy data are limited in publicly available sources.
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| Enzyme Assay |
The in vitro enzyme/receptor binding assay for F7H typically involves measuring its binding affinity to the FZD7 transmembrane domain (TMD). Surface plasmon resonance (SPR) can be used to determine the binding affinity (KD) of F7H for FZD7-TMD. Competitive binding assays with labeled FZD7 ligands can also be employed. The IC50 for FZD7 antagonism is determined using cell-based reporter assays measuring Wnt/β-catenin activity, where F7H is incubated with cells expressing FZD7 and a Wnt-responsive reporter.
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| Cell Assay |
The in vitro cell-based assay for F7H involves culturing cells expressing FZD7 and a Wnt/β-catenin-responsive reporter (e.g., TOPFlash luciferase). Cells are treated with F7H at various concentrations in the presence of Wnt ligands or activators. Luciferase activity is measured to determine the IC50 for FZD7 antagonism. Cell viability assays (MTT or CellTiter-Glo) may be used to assess cytotoxicity and distinguish specific pathway inhibition from general toxicity.
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| Animal Protocol |
In vivo animal studies for F7H have not been extensively reported. If conducted, such studies might involve mouse xenograft models of FZD7-driven cancers, where F7H is administered orally or intraperitoneally and tumor growth is monitored. Alternatively, models of bacterial infection could be used to assess bacteriostatic activity. Standard protocols for xenograft or infection models would be employed. No specific data are available from publicly accessible sources.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of F7H have not been extensively characterized. As a small molecule with a molecular weight of 463.55 and a molecular formula of C24H18FN3O2S2, it is expected to have moderate oral bioavailability. The compound is soluble in DMSO (50 mg/mL) and can be formulated for in vivo administration. Detailed PK parameters such as half-life, Cmax, and bioavailability are not available from publicly accessible sources.
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| Toxicity/Toxicokinetics |
The toxicity profile of F7H has not been systematically evaluated. As a research compound targeting FZD7, its primary safety concerns would relate to on-target effects on Wnt signaling, which is critical for tissue homeostasis. Standard toxicology assessments would include acute and sub-chronic toxicity studies in rodents, with endpoints including clinical signs, body weight, clinical pathology, and histopathology. No specific toxicity data are available from publicly accessible sources.
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| References | |
| Additional Infomation |
F7H is a research compound and has not been approved for clinical use. It is a potent small-molecule antagonist of Frizzled receptor FZD7 with an IC50 of 1.25 μM. F7H is a potent ligand for the FZD7 transmembrane domain (TMD) and exhibits potential antitumor and bacteriostatic activities through modulation of Wnt/β-catenin signaling. It is a valuable tool for studying FZD7-mediated Wnt signaling in cancer and infectious disease research.
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| Molecular Formula |
C24H18FN3O2S2
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|---|---|
| Molecular Weight |
463.547026157379
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| Exact Mass |
463.08
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| Elemental Analysis |
C, 62.19; H, 3.91; F, 4.10; N, 9.07; O, 6.90; S, 13.83
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| CAS # |
897109-93-2
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| PubChem CID |
20169956
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| Appearance |
White to off-white solid powder
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| LogP |
5.3
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
32
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| Complexity |
618
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(CC(NC1=NC(=CS1)C1C=CC=CC=1)=O)C1C=CC(=CC=1)NC(C1C=CC(=CC=1)F)=O
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| InChi Key |
GEURGPJRAOYJKC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H18FN3O2S2/c25-18-8-6-17(7-9-18)23(30)26-19-10-12-20(13-11-19)31-15-22(29)28-24-27-21(14-32-24)16-4-2-1-3-5-16/h1-14H,15H2,(H,26,30)(H,27,28,29)
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| Chemical Name |
4-fluoro-N-(4-((2-oxo-2-((4-phenylthiazol-2-yl)amino)ethyl)thio)phenyl)benzamide
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| Synonyms |
F7H inhibitor; F7-H inhibitor; F-7H inhibitor; F-7-H inhibitor; F7-H; F-7H; F-7-H; F7H
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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) |
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 | 2.1573 mL | 10.7863 mL | 21.5726 mL | |
| 5 mM | 0.4315 mL | 2.1573 mL | 4.3145 mL | |
| 10 mM | 0.2157 mL | 1.0786 mL | 2.1573 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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