| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
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| Targets |
VEGFR-2-IN-29 targets Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2), a receptor tyrosine kinase that plays a critical role in angiogenesis. VEGFR-2 is the primary mediator of VEGF-induced endothelial cell proliferation, migration, and survival, and it is a key regulator of blood vessel formation. By inhibiting VEGFR-2 with an IC50 of 16.5 nM, VEGFR-2-IN-29 blocks the signaling pathways that promote angiogenesis. This inhibition can reduce tumor growth and metastasis by cutting off the blood supply to tumors.
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| ln Vitro |
VEGFR-2-IN-29 (compound 5) (72 hours) suppresses the growth of HUVECs [1].
In vitro, VEGFR-2-IN-29 has been shown to inhibit VEGF-induced proliferation in HUVEC (human umbilical vein endothelial) cells. It is a potent VEGFR-2 inhibitor with an IC50 of 16.5 nM. The compound's activity has been demonstrated in cell-based assays where it suppresses the growth of HUVECs. These in vitro findings support its role as an effective anti-angiogenic agent. The compound is used to study the role of VEGFR-2 in angiogenesis and tumor biology. |
| ln Vivo |
Specific in vivo activity data for VEGFR-2-IN-29 are not detailed in the available literature. However, as a VEGFR-2 inhibitor, it is expected to have anti-angiogenic and anti-tumor effects in vivo. It is used in research related to tumor vasculature and cancer biology. Further studies in animal models are needed to confirm its in vivo efficacy, pharmacokinetics, and safety. The compound is currently in the research phase.
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| Enzyme Assay |
In vitro enzyme assays for VEGFR-2-IN-29 involve measuring the inhibition of VEGFR-2 kinase activity. The kinase is incubated with a peptide substrate and ATP in the presence of varying concentrations of the compound. The incorporation of phosphate into the substrate is measured using a luminescent or radiometric detection system. The IC50 value, representing the concentration required to inhibit 50% of the kinase activity, is calculated from the dose-response curve. The compound is typically dissolved in DMSO for stock solutions and diluted in the assay buffer.
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| Cell Assay |
Cell proliferation assay [1]
Cell Types: HUVEC Tested Concentrations: Incubation Duration: 72 hrs (hours) Experimental Results: demonstrated inhibitory effect on HUVEC proliferation induced by VEGF and bFGF, with IC50 of 15.8 nM and 210 nM respectively. In vitro cell-based assays for VEGFR-2-IN-29 are performed in HUVEC cells to study its anti-angiogenic effects. Cells are seeded in multi-well plates and treated with varying concentrations of the compound for 72 hours. VEGF is added to stimulate cell proliferation, and cell viability is assessed using a standard assay such as MTT. The compound's ability to inhibit VEGF-induced proliferation is determined by measuring the reduction in cell number. The compound is typically dissolved in DMSO and diluted in cell culture medium for treatment. |
| Animal Protocol |
Specific in vivo animal experiment protocols for VEGFR-2-IN-29 are not detailed in the available literature. However, as a potential anti-angiogenic agent, it would likely be tested in tumor xenograft models in mice. In such studies, tumor-bearing mice would be administered the compound orally or intraperitoneally. Tumor growth would be monitored, and angiogenesis would be assessed by measuring microvessel density or by using imaging techniques. The compound's efficacy would be evaluated by comparing tumor growth in treated versus control groups.
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| ADME/Pharmacokinetics |
VEGFR-2-IN-29 has a molecular weight of 293.28 g/mol and the formula C16H11N3O3. It is also known as 3-nitro-N-(quinolin-8-yl)benzamide. The compound is soluble in DMSO at 20 mg/mL. For long-term storage, the compound is kept as a powder at -20°C. Its pharmacokinetic properties, such as absorption, distribution, metabolism, and excretion, have not been extensively characterized in the available literature. However, its solubility in DMSO suggests it could be formulated for in vivo administration.
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| Toxicity/Toxicokinetics |
Specific toxicological data for VEGFR-2-IN-29 are not provided in the available sources. As a research chemical, its safety profile in humans has not been established. The compound is classified as a research reagent and is not for therapeutic or veterinary use. Standard laboratory safety precautions should be followed when handling this compound, including the use of appropriate personal protective equipment.
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| References | |
| Additional Infomation |
VEGFR-2-IN-29 is a small molecule inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2). It has the molecular formula C16H11N3O3 and a molecular weight of 293.28 g/mol. The compound is also known as 3-nitro-N-(quinolin-8-yl)benzamide. It effectively modulates angiogenesis and vascular permeability by inhibiting VEGFR-2 signaling. The compound has demonstrated an IC50 of 16.5 nM against VEGFR-2. In vitro, it inhibits VEGF-induced proliferation in HUVEC cells. It is used in research related to tumor vasculature, cancer biology, and potential therapeutic interventions for diseases characterized by aberrant angiogenesis. The compound is intended for research use only and is not for human consumption.
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| Molecular Formula |
C16H11N3O3
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|---|---|
| Molecular Weight |
293.27684
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| Exact Mass |
293.08
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| CAS # |
62802-77-1
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| PubChem CID |
657169
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| Appearance |
Light brown to brown solid powder
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| LogP |
4.302
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
22
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| Complexity |
423
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
IGPIXGIGDVQTEE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H11N3O3/c20-16(12-5-1-7-13(10-12)19(21)22)18-14-8-2-4-11-6-3-9-17-15(11)14/h1-10H,(H,18,20)
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| Chemical Name |
3-nitro-N-quinolin-8-ylbenzamide
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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 : ~20 mg/mL (~68.19 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 | 3.4097 mL | 17.0486 mL | 34.0971 mL | |
| 5 mM | 0.6819 mL | 3.4097 mL | 6.8194 mL | |
| 10 mM | 0.3410 mL | 1.7049 mL | 3.4097 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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