| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
hVEGF-IN-3 targets the VEGF signaling pathway. VEGF is a growth factor that stimulates the formation of new blood vessels (angiogenesis) by binding to its receptors (VEGFRs) on endothelial cells. This compound inhibits the proliferation of cancer cells. By inhibiting hVEGF activity, it reduces tumor growth, and is used to study cell cycle and signal transduction processes.
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| ln Vitro |
In vitro, hVEGF-IN-3 exhibits significant anti-proliferative effects across several human cell lines. It inhibits the proliferation of HT-29 colorectal adenocarcinoma cells with an IC50 of 61 microM. It also inhibits the proliferation of MCF-7 breast cancer cells (IC50 = 142 microM) and HEK-293 human embryonic kidney cells (IC50 = 114 microM). The high IC50 values indicate it is a moderate inhibitor, and it is used primarily as a research tool.
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| ln Vivo |
There are no direct reports of the in vivo activity of hVEGF-IN-3. As a small molecule inhibitor of hVEGF, it could theoretically be used in mouse xenograft models to evaluate anti-tumor efficacy. A typical study would involve daily oral administration of the compound to tumor-bearing mice and measuring tumor growth inhibition. However, due to its high IC50 in the low millimolar range, it would likely require high doses, making it a poor drug candidate.
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| Enzyme Assay |
A non-cellular assay for this compound is not standard, as VEGF is a growth factor, not an enzyme. A direct binding assay could be set up using Surface Plasmon Resonance (SPR). Recombinant hVEGF protein is immobilized on a sensor chip. Varying concentrations of hVEGF-IN-3 (0.1-1000 uM) are flowed over the chip, and the binding affinity (KD) is measured. This would confirm direct physical interaction with the VEGF protein.
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| Cell Assay |
A cell proliferation assay (MTT) is used. HT-29, MCF-7, or HEK-293 cells are seeded in 96-well plates at 5×103 cells/well. After 24 hours, the cells are treated with varying concentrations of hVEGF-IN-3 (0.5-1000 uM) for 48-72 hours. The medium is then replaced with MTT solution and incubated for 4 hours. The formazan crystals are solubilized, and the absorbance is read at 570 nm. The IC50 is calculated from the dose-response curve.
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| Animal Protocol |
There are no direct in vivo experiments reported for hVEGF-IN-3. If an experiment were to be designed, it would be a mouse xenograft model. Nude mice would be injected with HT-29 cells to establish a subcutaneous tumor. Mice would be treated with intraperitoneal or oral hVEGF-IN-3 (e.g., 50-200 mg/kg). Tumor volume and body weight would be measured. The endpoint would be a reduction in tumor growth compared to a vehicle control.
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| ADME/Pharmacokinetics |
hVEGF-IN-3 has a molecular weight of 211.26 g/mol and a predicted logP of approximately 3.5, indicating moderate lipophilicity. It is soluble in DMSO and ethanol. It is not a drug, so PK data is unknown. If administered, it would likely be metabolized by hepatic CYP450 enzymes and have a short half-life. For research use, store at -20degC, protected from light. Soluble in DMSO at 100 mM.
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| Toxicity/Toxicokinetics |
This is a research chemical and not a drug. Its toxicological profile has not been fully characterized. It may cause skin and eye irritation (H315, H319). Standard laboratory safety precautions (gloves, lab coat, goggles) should be used. It is for research use only. Do not consume. Keep away from strong oxidizing agents.
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| References | |
| Additional Infomation |
hVEGF-IN-3 is a small molecule "tool compound" used in cancer biology to inhibit the VEGF pathway. While its potency is modest (IC50 in the 100 uM range), it serves as a probe to study the structure-activity relationship (SAR) for VEGF inhibition. It is distinct from therapeutic VEGF pathway inhibitors like bevacizumab (monoclonal antibody) or small molecule receptor tyrosine kinase inhibitors (e.g., sunitinib). For research use only.
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| Molecular Formula |
C14H13NO
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| Molecular Weight |
211.26
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| CAS # |
46739-60-0
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
3.261
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| SMILES |
COC1C=CC(/C=C/C2C=CN=CC=2)=CC=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) |
DMSO : ~100 mg/mL (~473.35 mM; with ultrasonication)
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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 | 4.7335 mL | 23.6675 mL | 47.3350 mL | |
| 5 mM | 0.9467 mL | 4.7335 mL | 9.4670 mL | |
| 10 mM | 0.4734 mL | 2.3668 mL | 4.7335 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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