| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
VEGFR2 (vascular endothelial growth factor receptor 2, also known as KDR). VEGFR2-IN-7 is an inhibitor of VEGFR2, a receptor tyrosine kinase that mediates VEGF-induced angiogenesis. VEGFR2 is expressed on endothelial cells and is the primary receptor responsible for VEGF-induced endothelial cell proliferation, migration, and tube formation. Activation of VEGFR2 by VEGF leads to autophosphorylation and activation of downstream signaling pathways including MAPK/ERK, PI3K/AKT, and PLCγ, which promote endothelial cell survival, proliferation, and angiogenesis.
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| ln Vitro |
VEGFR2-IN-7 (compound E) is an inhibitor of VEGFR2, used in cancer research. It shows promise in preclinical models of cancer, particularly in solid tumors. The compound inhibits VEGFR2 kinase activity, thereby blocking VEGF-induced signaling and angiogenesis. By inhibiting angiogenesis, VEGFR2-IN-7 can reduce tumor blood supply, leading to tumor growth inhibition and potentially tumor regression. Detailed IC50 values for VEGFR2 inhibition are not provided in the available literature.
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| ln Vivo |
VEGFR2-IN-7 has shown promise in preclinical models of cancer, particularly in solid tumors, and could provide a valuable therapeutic strategy for tumors resistant to conventional therapies. By inhibiting VEGFR2-mediated angiogenesis, the compound can reduce tumor growth and metastasis. The compound may be effective against tumors that are dependent on VEGF-driven angiogenesis for growth and survival.
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| Enzyme Assay |
In vitro kinase assays are performed using recombinant VEGFR2 enzyme incubated with ATP substrate and varying concentrations of VEGFR2-IN-7. Phosphorylation is measured via radiometric, fluorescence-based, or ELISA-based methods to determine IC50 for kinase inhibition. The assays are typically carried out in optimized buffer conditions (e.g., HEPES pH 7.5, MgCl2, DTT) at room temperature or 30°C. Dose-response curves are fitted to determine IC50 values.
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| Cell Assay |
Endothelial cells (e.g., HUVECs, human umbilical vein endothelial cells) or cancer cell lines are treated with VEGFR2-IN-7 at graded concentrations. VEGF-induced cell proliferation is assessed using standard viability assays (MTT, CCK-8). Cell migration is assessed using wound healing or transwell migration assays. Tube formation assays are performed by plating endothelial cells on Matrigel and measuring the formation of capillary-like structures. The ability of VEGFR2-IN-7 to inhibit these VEGF-induced responses confirms its anti-angiogenic activity.
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| Animal Protocol |
Mouse xenograft models bearing solid tumors are administered VEGFR2-IN-7 via oral or intraperitoneal routes. Tumor volume is measured regularly using calipers, and body weight is monitored to assess tolerability. At study endpoint, tumors are collected for histopathological analysis. Tumor angiogenesis is assessed by immunohistochemistry for CD31 (an endothelial cell marker) to measure microvessel density. Tumor growth inhibition is calculated by comparing tumor volumes in treated and control groups.
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| ADME/Pharmacokinetics |
Predicted to have moderate oral bioavailability typical of small-molecule VEGFR2 inhibitors. Metabolic clearance is mediated by hepatic CYP450 enzymes. Standard pharmacokinetic parameters (Cmax, Tmax, AUC, t1/2, clearance, volume of distribution) are evaluated in rodents following both intravenous and oral administration. Formulation in suitable vehicles (e.g., DMSO/PEG400/saline) is required for in vivo administration. Detailed PK data specific to VEGFR2-IN-7 are not extensively reported in the available literature.
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| Toxicity/Toxicokinetics |
Expected to have a manageable safety profile at therapeutic doses based on the established safety of VEGFR2 inhibitors. VEGFR2 inhibitors (e.g., sunitinib, sorafenib, pazopanib) are clinically approved and have well-characterized safety profiles. Potential toxicities may include hypertension (due to effects on vascular tone), fatigue, gastrointestinal effects (diarrhea, nausea), and hand-foot skin reaction. Standard toxicology studies are required for therapeutic development. As a research compound, detailed toxicology data are not publicly available.
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| References | |
| Additional Infomation |
VEGFR2-IN-7 is a research-grade small-molecule VEGFR2 inhibitor for oncology research. Molecular formula: C18H17NO3, molecular weight: 295.33. CAS: 174258-31-2. Synonyms: compound E, {3-[(5-methyl-2-phenyl-1,3-oxazol-4-yl)methoxy]phenyl}methanol. It is used in studies of angiogenesis and cancer therapy. For research use only, not for human therapeutic use.
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| CAS # |
174258-31-2
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| Appearance |
White to off-white solid powder
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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 :~200 mg/mL (~677.21 mM; with sonication)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 5 mg/mL (16.93 mM) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one),clear solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared,you can add 100 μL of 50.0 mg/mL clear DMSO stock solution and add it to 400 μL PEG300 and mix well. Then add 50 μL Tween-80 to the above system and mix well. Then continue to add 450 μL of physiological saline to make up to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 5 mg/mL (16.93 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one),clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared,you can add 100 μL of 50.0 mg/mL clear DMSO stock solution and add it to 900 μL corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
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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