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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Targets |
FzM1 targets Frizzled (FZD) receptors, which are the cell surface receptors for Wnt proteins. Wnt signaling is a critical pathway involved in embryonic development, cell proliferation, and differentiation. By inhibiting FZD receptors, FzM1 blocks the activation of downstream signaling cascades, including the β-catenin-dependent canonical pathway. This inhibition can reduce cell proliferation and induce apoptosis in cancer cells that depend on Wnt signaling.
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| ln Vitro |
In vitro, FzM1 has been shown to inhibit Wnt/β-catenin signaling in various cancer cell lines. The compound reduces the expression of Wnt target genes and inhibits cell proliferation. Its activity has been characterized in cell-based reporter assays and functional studies. Its selectivity for FZD receptors over other receptors has been assessed. The compound's effects on cell viability and signaling pathways have been studied.
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| ln Vivo |
In vivo, FzM1 has demonstrated efficacy in preclinical models of Wnt-dependent cancers. The compound has been shown to inhibit tumor growth in xenograft models. Its ability to block Wnt signaling and reduce tumor cell proliferation underlies its in vivo efficacy. Specific dosing regimens and detailed efficacy data are available in the scientific literature.
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| Enzyme Assay |
In vitro receptor binding assays for FzM1 involve measuring its binding affinity to Frizzled receptors using radioligand binding or surface plasmon resonance. Its ability to inhibit Wnt signaling is assessed using reporter gene assays, where cells are transfected with a Wnt-responsive luciferase reporter and treated with the compound. The IC50 value is determined from dose-response curves. Selectivity against other receptors is assessed using screening panels.
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| Cell Assay |
In vitro cell-based assays for FzM1 involve treating cancer cell lines with the compound to assess its effects on Wnt signaling, cell proliferation, and apoptosis. Wnt target gene expression is measured by qPCR. Cell proliferation is measured using MTT or similar assays. Apoptosis is quantified by flow cytometry or caspase activity assays. These assays characterize the compound's cellular activity and mechanism of action.
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| Animal Protocol |
In vivo animal experiments for FzM1 have been conducted in mouse xenograft models of Wnt-dependent cancers. Tumor-bearing mice are treated with FzM1, and tumor growth inhibition is monitored. Effects on Wnt signaling in tumor tissues are assessed by measuring target gene expression. Pharmacokinetic studies are performed to establish exposure-response relationships. These studies support the compound's potential as an anticancer agent.
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| ADME/Pharmacokinetics |
FzM1 has a molecular weight and formula consistent with small-molecule FZD inhibitors. It is a research compound. The compound is typically dissolved in DMSO for in vitro studies and formulated for in vivo administration. Its pharmacokinetic properties have been characterized in preclinical studies. It is typically stored under recommended conditions for research compounds.
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| Toxicity/Toxicokinetics |
Specific toxicity data for FzM1 is not extensively reported. As a Wnt signaling inhibitor, its safety profile is related to its effects on this pathway, which is important for normal tissue homeostasis. The compound is generally well-tolerated in preclinical studies at therapeutic doses. Comprehensive toxicological studies would be required for therapeutic development. Standard safety precautions should be taken when handling the compound.
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| References | |
| Additional Infomation |
FzM1 is a research compound that targets Frizzled (FZD) receptors and inhibits Wnt/β-catenin signaling. It has been studied for its potential in cancer research. The compound has demonstrated efficacy in preclinical models of Wnt-dependent cancers. FzM1 is a tool for studying Wnt pathway biology and has potential therapeutic applications.
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| Molecular Formula |
C21H16N2O2S
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|---|---|
| Molecular Weight |
360.43
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| Exact Mass |
360.093
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| CAS # |
1680196-54-6
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| PubChem CID |
90478321
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| Appearance |
White to light brown solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
518.3±50.0 °C at 760 mmHg
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| Flash Point |
267.2±30.1 °C
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| Vapour Pressure |
0.0±1.4 mmHg at 25°C
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| Index of Refraction |
1.779
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| LogP |
5.29
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
26
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| Complexity |
489
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C2C=C(C=CC2=C1)NC(=O)NC3=CC(=CC(=C3)C4=CC=CS4)O
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| InChi Key |
OBTSACXGWYGCPK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H16N2O2S/c24-19-12-16(20-6-3-9-26-20)11-18(13-19)23-21(25)22-17-8-7-14-4-1-2-5-15(14)10-17/h1-13,24H,(H2,22,23,25)
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| Chemical Name |
1-(3-hydroxy-5-thiophen-2-ylphenyl)-3-naphthalen-2-ylurea
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| Synonyms |
FzM 1 FzM-1 FzM1
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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 : ~62.5 mg/mL (~173.40 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (5.77 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 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. Solubility in Formulation 2: 2.08 mg/mL (5.77 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline 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 | 2.7745 mL | 13.8723 mL | 27.7446 mL | |
| 5 mM | 0.5549 mL | 2.7745 mL | 5.5489 mL | |
| 10 mM | 0.2774 mL | 1.3872 mL | 2.7745 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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