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| Targets |
(Z)-FeCP-oxindole targets vascular endothelial growth factor receptor 2 (VEGFR2), a receptor tyrosine kinase that is a key mediator of angiogenesis. VEGFR2 is activated by VEGF binding, leading to downstream signaling that promotes endothelial cell proliferation, migration, and survival. The compound inhibits VEGFR2 with IC50 = 200 nM (or 220 nM), demonstrating potent inhibitory activity. At 10 µM, (Z)-FeCP-oxindole significantly inhibits VEGFR1 and PDGFRα or β, indicating some selectivity for VEGFR2. The oxindole core is a common pharmacophore for kinase inhibitors, interacting with the ATP-binding pocket of the kinase domain. The ferrocenyl group enhances lipophilicity and cellular uptake, potentially improving bioavailability. By inhibiting VEGFR2, the compound blocks VEGF-mediated angiogenesis, which is a critical process in tumor growth, metastasis, and other angiogenesis-dependent diseases. The compound's anticancer activity is attributed to VEGFR2 inhibition and potentially other mechanisms including redox modulation.
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| ln Vitro |
In vitro, (Z)-FeCP-oxindole demonstrates potent VEGFR2 inhibitory activity with IC50 = 200 nM. At 10 µM, the compound significantly inhibits VEGFR1 and PDGFRα or β, indicating some selectivity for VEGFR2. The compound exhibits anticancer activity against B16 murine melanoma cells with IC50 <1 µM. The ferrocenyl group contributes to cellular uptake and potentially to redox-mediated effects. The oxindole core provides the kinase inhibitory pharmacophore. The compound's mechanism of action involves inhibition of VEGFR2-mediated signaling, leading to reduced endothelial cell proliferation and angiogenesis. The compound may also have direct effects on cancer cells through VEGFR2 inhibition and potentially through other mechanisms including interference with cellular redox balance and induction of apoptosis. These in vitro activities make (Z)-FeCP-oxindole a promising lead compound for anticancer drug development.
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| ln Vivo |
In vivo studies with (Z)-FeCP-oxindole are limited in publicly available literature. The compound's potent in vitro VEGFR2 inhibitory activity and anticancer activity against B16 melanoma cells (IC50 <1 µM) suggest potential for in vivo antitumor efficacy. As a VEGFR2 inhibitor, the compound would be expected to inhibit angiogenesis and tumor growth in vivo. However, specific in vivo studies (animal models, dosing regimens, tumor growth inhibition) have not been extensively reported. The ferrocenyl group may affect the compound's pharmacokinetic properties and tissue distribution. Researchers interested in in vivo applications should consult the primary literature for updated information and conduct appropriate studies to determine effective dosing and administration routes. The compound's mechanism as a VEGFR2 inhibitor makes it relevant for studying angiogenesis-dependent diseases including cancer.
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| Enzyme Assay |
In vitro kinase assays are used to characterize (Z)-FeCP-oxindole's inhibitory activity against VEGFR2 and other kinases. The compound is incubated with purified VEGFR2 kinase and ATP substrate, and kinase activity is measured by phosphorylation of a peptide substrate or by monitoring ATP consumption. IC50 = 200 nM (or 220 nM) is determined from dose-response curves. Selectivity is assessed by testing the compound against a panel of related kinases including VEGFR1, PDGFRα, PDGFRβ, and others at 10 µM concentration. The compound significantly inhibits VEGFR1 and PDGFRα or β at 10 µM, indicating some selectivity for VEGFR2. These kinase assays are essential for characterizing the compound's potency, selectivity, and mechanism of action. The oxindole core interacts with the ATP-binding pocket of the kinase domain, a common feature of kinase inhibitors.
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| Cell Assay |
In vitro cell-based assays for (Z)-FeCP-oxindole are conducted in cancer cell lines including B16 murine melanoma cells. Cells are treated with the compound at various concentrations (typically 0-10 µM) for defined periods (24-72 hours). Cell proliferation is assessed using MTT, CCK-8, or CellTiter-Glo assays. The compound demonstrates IC50 <1 µM against B16 cells. Apoptosis is assessed by Annexin V/PI staining, caspase activity assays, and PARP cleavage Western blot. The compound's ability to interfere with cellular redox balance can be assessed by measuring reactive oxygen species (ROS) levels using fluorescent probes such as DCFH-DA. Endothelial cell-based assays (e.g., HUVEC proliferation, migration, tube formation) can be used to assess anti-angiogenic activity. These cell-based assays characterize the compound's anticancer activity and mechanism of action.
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| Animal Protocol |
In vivo animal protocols for (Z)-FeCP-oxindole are not well-documented in publicly available literature. Based on the compound's in vitro activity as a VEGFR2 inhibitor, typical study designs for evaluating antitumor efficacy would involve administration of the compound in rodent xenograft models bearing tumor cells (e.g., B16 melanoma or other VEGFR2-dependent tumors). Doses would be determined from in vitro potency data and preliminary toxicity assessments. Route of administration would depend on the compound's solubility and bioavailability. Treatment duration and frequency would be optimized based on pharmacokinetic and pharmacodynamic data. Endpoints would include tumor growth inhibition, angiogenesis assessment (CD31 staining), survival, and histopathological analysis. Researchers should consult primary literature for updated protocols and conduct appropriate dose-finding and efficacy studies.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of (Z)-FeCP-oxindole have not been extensively characterized in published literature. The compound has molecular weight 329.17 and molecular formula C19H15FeNO. The ferrocenyl group enhances lipophilicity, which may facilitate cellular uptake and membrane permeability. The compound is soluble in DMSO at ~50 mg/mL (~151.90 mM). For in vivo formulations, DMSO-based formulations can be prepared. Storage: powder at -20°C for 3 years, 4°C for 2 years; in solvent at -80°C for 6 months, -20°C for 1 month. Specific pharmacokinetic parameters such as half-life, Cmax, AUC, bioavailability, and tissue distribution have not been reported. Researchers planning in vivo studies should conduct appropriate pharmacokinetic studies to determine these parameters. The compound's ferrocenyl group may affect its metabolic stability and elimination.
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| Toxicity/Toxicokinetics |
Toxicology data for (Z)-FeCP-oxindole are limited in publicly available sources. The compound's ferrocenyl group may have implications for redox activity and potential toxicity, as ferrocene derivatives can generate reactive oxygen species. However, comprehensive toxicology studies (acute and chronic toxicity, genotoxicity, reproductive toxicity, cardiotoxicity) have not been reported. The compound has demonstrated anticancer activity at IC50 <1 µM in B16 cells, indicating potent biological activity. The compound is for research use only and is not approved for human therapeutic use. Standard laboratory safety precautions should be followed when handling (Z)-FeCP-oxindole. The compound should be stored properly and disposed of in accordance with applicable regulations. Researchers should consult the material safety data sheet (MSDS) for detailed safety information.
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| References | |
| Additional Infomation |
(Z)-FeCP-oxindole has CAS number 1137967-28-2, molecular formula C19H15FeNO, and molecular weight 329.17. It is a selective inhibitor of human VEGFR2 with IC50 = 200 nM (or 220 nM). At 10 µM, the compound significantly inhibits VEGFR1 and PDGFRα or β. The compound exhibits anticancer activity against B16 murine melanoma cells with IC50 <1 µM. The ferrocenyl group enhances lipophilicity and cellular uptake, while the oxindole core contributes to bioactivity through interactions with key signaling proteins. The compound has shown potential in anticancer research due to its ability to interfere with cellular redox balance and induce apoptosis. Purity: ≥98%. The compound is a brown to reddish brown solid powder. Solubility: DMSO ~50 mg/mL (~151.90 mM). Storage: powder at -20°C for 3 years, 4°C for 2 years; in solvent at -80°C for 6 months, -20°C for 1 month. Not approved for clinical use; for research purposes only. The compound is a valuable tool for studying VEGFR2 signaling and angiogenesis.
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| Molecular Formula |
C19H15FENO
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| Molecular Weight |
329.1735060215
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| Exact Mass |
329.05
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| CAS # |
1137967-28-2
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| PubChem CID |
90488891
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| Appearance |
Brown to reddish brown solid powder
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
22
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| Complexity |
353
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| Defined Atom Stereocenter Count |
0
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| SMILES |
[CH-]1C=CC=C1.C1=CC=C2C(=C1)C(=C(N2)[O-])C=C3C=CC=C3.[Fe+2]
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| InChi Key |
MTGBTDOTYGXLBK-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C14H11NO.C5H5.Fe/c16-14-12(9-10-5-1-2-6-10)11-7-3-4-8-13(11)15-14;1-2-4-5-3-1;/h1-9,15-16H;1-5H;/q;-1;+2/p-1
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| Chemical Name |
cyclopenta-1,3-diene;3-(cyclopenta-2,4-dien-1-ylidenemethyl)-1H-indol-2-olate;iron(2+)
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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 : ~50 mg/mL (~151.90 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 | 3.0379 mL | 15.1897 mL | 30.3794 mL | |
| 5 mM | 0.6076 mL | 3.0379 mL | 6.0759 mL | |
| 10 mM | 0.3038 mL | 1.5190 mL | 3.0379 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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