| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 10mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
FiVe1 targets vimentin, an intermediate filament protein that is a key component of the cytoskeleton and is involved in cell migration, adhesion, and signaling. FiVe1 binds to vimentin and promotes its disorganization and phosphorylation during metaphase. This leads to mitotic catastrophe, multinucleation, and loss of cancer cell stemness, ultimately inhibiting the growth of mesenchymal cancer cells.
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|---|---|
| ln Vitro |
FiVe1 selectively and irreversibly inhibits the growth of mesenchymally transformed breast cancer cells, with an IC₅₀ of 234 nM in FOXC2-HMLER cells. It also inhibits the growth of soft tissue sarcomas of diverse histological subtypes. The compound inhibits the migration of mesenchymally transformed cells and may also inhibit VEGFR2 and FGFR family kinases.
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| ln Vivo |
FiVe1 has been shown to have anticancer activity against soft tissue sarcomas. By targeting vimentin and disrupting the cytoskeleton of mesenchymal cancer cells, FiVe1 induces mitotic catastrophe and inhibits tumor growth. Its effects on cancer cell stemness suggest that it may have potential for preventing tumor recurrence and metastasis.
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| Enzyme Assay |
For non-cellular assays, FiVe1's binding to vimentin can be evaluated using surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC) to measure the affinity of the interaction. The compound's effect on vimentin polymerization can be assessed using a turbidity assay, where purified vimentin is incubated with varying concentrations of FiVe1, and the extent of filament formation is monitored by absorbance at 350 nm.
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| Cell Assay |
In vitro cellular assays for FiVe1 involve treating mesenchymal cancer cell lines (e.g., FOXC2-HMLER breast cancer cells) with the compound and assessing cell viability, proliferation, and morphology. Cell viability is measured using MTT or CellTiter-Glo® assays. The effects on vimentin organization and phosphorylation are assessed by immunofluorescence microscopy and Western blotting. Cell migration is evaluated using wound healing or transwell migration assays.
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| Animal Protocol |
In vivo animal experiments with FiVe1 involve administering the compound to mouse xenograft models of mesenchymal breast cancer or soft tissue sarcoma. Tumor-bearing mice are treated with FiVe1 via intraperitoneal injection or oral gavage, and tumor growth inhibition is monitored. Endpoints include tumor volume measurements, histopathological analysis, and assessment of vimentin phosphorylation and organization in tumor tissue.
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| ADME/Pharmacokinetics |
FiVe1 has a molecular weight of 359.25 and a molecular formula of C₁₈H₁₆Cl₂N₄. It is a solid at room temperature and is typically stored at -20°C. Purity is typically 99%. The compound is soluble in DMSO and other organic solvents. It is stable under recommended storage conditions and is protected from light and moisture.
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| Toxicity/Toxicokinetics |
Toxicological data for FiVe1 are limited as it is a research compound. Standard laboratory safety precautions should be followed when handling the compound. It may cause skin, eye, and respiratory irritation. The compound is not intended for human therapeutic use.
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| References | |
| Additional Infomation |
FiVe1 is a novel vimentin-binding small molecule that selectively inhibits the growth of mesenchymally transformed cancer cells. It promotes vimentin disorganization and phosphorylation during metaphase, leading to mitotic catastrophe. The compound is a valuable research tool for studying the role of vimentin in cancer biology and for validating vimentin as a therapeutic target.
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| Molecular Formula |
C18H16CL2N4
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|---|---|
| Molecular Weight |
359.25244140625
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| Exact Mass |
358.075
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| CAS # |
932359-76-7
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| Related CAS # |
932359-76-7;
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| PubChem CID |
20922966
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| Appearance |
Light yellow to light brown solid powder
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| LogP |
4.2
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
24
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| Complexity |
416
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1=CC=CC(=C1)N1CCN(C2=CN=NC3C(=CC=CC2=3)Cl)CC1
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| InChi Key |
DZGXRHIQXADSDH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H16Cl2N4/c19-13-3-1-4-14(11-13)23-7-9-24(10-8-23)17-12-21-22-18-15(17)5-2-6-16(18)20/h1-6,11-12H,7-10H2
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| Chemical Name |
8-Chloro-4-(4-(3-chlorophenyl)piperazin-1-yl)cinnoline
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| Synonyms |
FiVe1 FiVe 1 FiVe-1
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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 | 2.7836 mL | 13.9179 mL | 27.8358 mL | |
| 5 mM | 0.5567 mL | 2.7836 mL | 5.5672 mL | |
| 10 mM | 0.2784 mL | 1.3918 mL | 2.7836 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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