| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| Targets |
Fz7-21 primarily targets Frizzled 7 (FZD7) receptors, which are involved in Wnt/β-catenin signaling pathways. FZD7 receptors play crucial roles in cellular communication and developmental processes. By selectively binding to the FZD7 CRD subclass, Fz7-21 alters the receptor's conformation and its lipid-binding groove. This modulates Wnt/β-catenin signaling, making it a valuable tool for studying cancer stem cell regulation, tumor progression, and Wnt-driven malignancies.
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|---|---|
| ln Vitro |
Fz7-21 (Ac-LPSDDLEFWCHVMY-NH2) inhibits Wnt signaling with an IC50 value of 100 nM (0-100μM; 6 hours; HEK293-TB cells) [1]. With an IC50 value of 50 nM, Fz7-21 (Ac-LPSDDLEFWCHVMY-NH2) (1 µM) inhibits WNT3A-mediated β-catenin stability in mouse L cells [1]. The function of LGR5+ stem cells is disrupted by Fz7-21 (Ac-LPSDDLEFWCHVMY-NH2) (200 µM; 48 hours; LGR5–GFP+ stem cells) [1].
In vitro, Fz7-21 modulates Wnt/β-catenin signaling in HEK293 cells stimulated with exogenous WNT3A (IC50 = 100 nM) or transfected with a construct expressing WNT3A or WNT1. It selectively binds to the FZD7 CRD subclass. Its activity is typically evaluated using luciferase reporter assays measuring β-catenin-dependent transcription, as well as receptor binding assays. The compound's ability to block WNT3A-mediated β-catenin stabilization is assessed. |
| ln Vivo |
In vivo, Fz7-21 has been studied for its role in modulating Wnt/β-catenin signaling. It is used to study cancer stem cell regulation, tumor progression, and therapeutic targeting of Wnt-driven malignancies. However, specific in vivo efficacy data, including dosing regimens and animal models, are not extensively detailed in the available literature. Further studies are needed to fully characterize its in vivo pharmacological profile. The compound is a research tool for studying Wnt signaling.
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| Enzyme Assay |
Cell-free assays for Fz7-21 involve evaluating its binding affinity to FZD7 CRD. Binding assays such as surface plasmon resonance (SPR) or fluorescence polarization are used to determine binding affinity. The compound's ability to alter the conformation of the CRD and its lipid-binding groove can be assessed using biophysical techniques. The compound's chemical purity and identity are confirmed by HPLC and mass spectrometry. It is typically dissolved in DMSO or appropriate buffers for assay preparation.
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| Cell Assay |
In vitro cellular assays for Fz7-21 typically involve treating HEK293 cells with the compound. Cells are stimulated with exogenous WNT3A or transfected with WNT3A or WNT1 expression constructs. Wnt/β-catenin signaling is assessed using luciferase reporter assays. IC50 values (100 nM) are determined from dose-response curves. The compound's ability to block β-catenin stabilization is assessed by western blotting. Cytotoxicity is evaluated using standard cell viability assays.
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| Animal Protocol |
In vivo animal studies for Fz7-21 are conducted in models of cancer, particularly Wnt-driven malignancies. The compound is administered via various routes including intraperitoneal or intravenous injection. Tumor growth is monitored. Wnt/β-catenin signaling activity in tumor tissues is assessed. However, specific dosing regimens and experimental protocols are not extensively documented in the available literature. Standard protocols for evaluating Wnt pathway inhibitors would typically be employed.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Fz7-21 include a molecular weight of 1796.05 g/mol, molecular formula C83H114N18O23S2, and sequence Ac-LPSDDLEFWCHVMY-NH2. As a peptide, it has limited oral bioavailability and is typically administered parenterally. The compound is typically stored as a lyophilized powder and reconstituted in appropriate buffers before use. Detailed ADME parameters such as half-life, Cmax, and AUC are not extensively reported.
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| Toxicity/Toxicokinetics |
The toxicity profile of Fz7-21 has not been extensively characterized in published literature. As a peptide antagonist of FZD7, potential toxicities may include effects on Wnt signaling in normal tissues. Standard preclinical safety studies would include acute and sub-chronic toxicity assessments in rodent models. The compound is intended for research use only and not for therapeutic applications in humans.
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| References | |
| Additional Infomation |
Fz7-21 is a synthetic peptide antagonist of Frizzled 7 (FZD7) receptors that modulates Wnt/β-catenin signaling. It selectively binds to FZD7 CRD and has an IC50 of 100 nM in HEK293 cells. Its sequence is Ac-LPSDDLEFWCHVMY-NH2 with a molecular weight of 1796.05 g/mol. Fz7-21 is a research tool for studying Wnt signaling, cancer stem cells, and tumor progression. It is not for therapeutic use.
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| Molecular Formula |
C83H114N18O23S2
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|---|---|
| Molecular Weight |
1796.03007745743
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| CAS # |
2247635-23-8
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| Related CAS # |
Fz7-21 TFA
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| PubChem CID |
155977635
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| Sequence |
Ac-LPSDDLEFWCHVMY-NH2
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
22
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| Hydrogen Bond Acceptor Count |
26
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| Rotatable Bond Count |
52
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| Heavy Atom Count |
126
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| Complexity |
3740
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| Defined Atom Stereocenter Count |
14
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| SMILES |
SC[C@@H](C(N[C@@H](CC1=CNC=N1)C(N[C@H](C(N[C@H](C(N[C@H](C(N)=O)CC1C=CC(=CC=1)O)=O)CCSC)=O)C(C)C)=O)=O)NC([C@H](CC1=CNC2C=CC=CC1=2)NC([C@H](CC1C=CC=CC=1)NC([C@H](CCC(=O)O)NC([C@H](CC(C)C)NC([C@H](CC(=O)O)NC([C@H](CC(=O)O)NC([C@H](CO)NC([C@@H]1CCCN1C([C@H](CC(C)C)NC(C)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 (~55.68 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 | 0.5568 mL | 2.7839 mL | 5.5678 mL | |
| 5 mM | 0.1114 mL | 0.5568 mL | 1.1136 mL | |
| 10 mM | 0.0557 mL | 0.2784 mL | 0.5568 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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