| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 50mg | |||
| Other Sizes |
| Targets |
The primary target of SRI37892 is Frizzled protein 7 (Fzd7), a seven-pass transmembrane receptor that functions as a receptor for Wnt ligands. Fzd7 is a key component of the Wnt/β-catenin signaling pathway, which regulates cell proliferation, differentiation, and migration. SRI37892 targets the transmembrane domain of FZD7, blocking the interaction between Wnt ligands and the receptor and thereby inhibiting downstream signaling. The compound inhibits Wnt/β-catenin signaling with an IC50 of 0.66 μM in reporter assays and inhibits cancer cell proliferation with an IC50 of 2 μM.
|
|---|---|
| ln Vitro |
In vitro, SRI37892 demonstrates potent inhibition of Wnt/Fzd7 signaling and cancer cell proliferation. It inhibits Wnt/β-catenin signaling with an IC50 of 0.66 μM in reporter assays and inhibits cancer cell proliferation with an IC50 of 2 μM. The compound's activity is mediated through its binding to the transmembrane domain of FZD7. However, detailed cellular activity data, including effects on specific cancer cell lines, are not extensively reported in the available literature.
|
| ln Vivo |
In vivo data for SRI37892 are not extensively reported in the available literature. As an inhibitor of Fzd7, the compound has potential for in vivo applications in cancer models. However, specific in vivo efficacy data, including animal models, dosing regimens, and pharmacokinetic-pharmacodynamic relationships, are not detailed in the available sources. The compound is classified as a research-use-only chemical.
|
| Enzyme Assay |
In vitro enzyme/receptor binding assays for SRI37892 typically involve measuring its binding to Fzd7 or its inhibition of Wnt/β-catenin signaling. In binding assays, the compound's affinity for Fzd7 is measured using surface plasmon resonance or other biophysical techniques. In functional assays, the compound's ability to inhibit Wnt/β-catenin signaling is assessed using reporter gene assays, such as TOPFlash/FOPFlash assays, in cells expressing Fzd7.
|
| Cell Assay |
Cellular assays for SRI37892 are performed in cancer cell lines to assess its effects on Wnt signaling and cell proliferation. Cells are treated with SRI37892, and Wnt/β-catenin signaling is measured using reporter gene assays or by measuring the expression of Wnt target genes. Cell proliferation is assessed using assays such as MTT or cell counting. The compound's effects on cell cycle and apoptosis may also be assessed.
|
| Animal Protocol |
In vivo animal studies with SRI37892 are not extensively documented in the available literature. Based on its inhibition of Fzd7-mediated Wnt signaling, potential in vivo models could include xenograft models for cancer. In such studies, SRI37892 would be administered orally or intraperitoneally, and tumor growth would be monitored. However, specific protocols are not detailed in the available sources.
|
| ADME/Pharmacokinetics |
Pharmacokinetic data for SRI37892 are not extensively reported. The compound is a small molecule with a molecular weight that is not specified in the available literature. It is typically dissolved in DMSO for in vitro studies. However, detailed pharmacokinetic parameters such as absorption, distribution, metabolism, excretion, half-life, and bioavailability are not available in the literature for this research compound.
|
| Toxicity/Toxicokinetics |
SRI37892 has been shown to inhibit cancer cell proliferation, indicating potential anticancer activity. However, comprehensive toxicology data for this compound are not extensively reported. As an inhibitor of Wnt signaling, it may have effects on normal stem cell populations that could contribute to toxicity. The compound is classified as a research-use-only chemical and is not intended for human consumption. Specific toxicological data, including acute toxicity, genotoxicity, and target organ effects, are not reported in the available literature.
|
| References |
Zhang W, Lu W, Ananthan S, Suto MJ, Li Y. Discovery of novel frizzled-7 inhibitors by targeting the receptor's transmembrane domain. Oncotarget. 2017 Sep 6;8(53):91459-91470. doi: 10.18632/oncotarget.20665. eCollection 2017 Oct 31. PubMed PMID: 29207657; PubMed Central PMCID: PMC5710937.
|
| Additional Infomation |
SRI37892 is a research-grade compound not approved for clinical use. Its primary application is as a pharmacological tool for studying the role of Fzd7 and Wnt signaling in cancer. The compound is used to investigate the mechanisms of Wnt/Fzd7 signaling in tumorigenesis and to develop cancer therapeutic agents that target this pathway. It is also used to study the potential of Fzd7 as a therapeutic target in cancer.
|
| Molecular Formula |
C26H19N5O2S
|
|---|---|
| Molecular Weight |
465.526363611221
|
| Exact Mass |
465.125
|
| CAS # |
1030769-75-5
|
| Related CAS # |
1030769-75-5;
|
| PubChem CID |
41550022
|
| Appearance |
Light yellow to brown solid powder
|
| LogP |
4.1
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
34
|
| Complexity |
760
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1CC(=O)NC2=C1C=C(C=C2)C3=CSC(=N3)NC(=O)C4=CC=C(C=C4)N5C=NC6=CC=CC=C65
|
| InChi Key |
DXSMYUKZPWJQFM-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C26H19N5O2S/c32-24-12-8-17-13-18(7-11-20(17)28-24)22-14-34-26(29-22)30-25(33)16-5-9-19(10-6-16)31-15-27-21-3-1-2-4-23(21)31/h1-7,9-11,13-15H,8,12H2,(H,28,32)(H,29,30,33)
|
| Chemical Name |
4-(1H-Benzo[d]imidazol-1-yl)-N-(4-(2-oxo-1,2,3,4-tetrahydroquinolin-6-yl)thiazol-2-yl)benzamide
|
| Synonyms |
SRI-37892 SRI 37892 SRI37892
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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
|
|---|---|
| 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 | 2.1481 mL | 10.7404 mL | 21.4809 mL | |
| 5 mM | 0.4296 mL | 2.1481 mL | 4.2962 mL | |
| 10 mM | 0.2148 mL | 1.0740 mL | 2.1481 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
