| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| Other Sizes |
| Targets |
KDR 0.02 μM (IC50) Flt-1 0.18 μM (IC50) EGFR 0.24 μM (IC50)
VEGFR-IN-1 targets VEGFR2 (KDR), a key receptor tyrosine kinase involved in angiogenesis. By inhibiting VEGFR2 with an IC50 of 3 nM, it blocks the signaling pathways that promote endothelial cell proliferation, migration, and survival. It also inhibits other kinases, including Flt-1 (VEGFR1), c-Kit, EGF-R, and c-Src, making it a multi-targeted inhibitor. |
|---|---|
| ln Vitro |
In vitro, VEGFR-IN-1 is a potent inhibitor of VEGFR2 (KDR) with an IC50 of 3 nM. It also inhibits Flt-1 (IC50 = 0.02 µM), c-Kit (IC50 = 0.24 µM), EGF-R (IC50 = 7.3 µM), and c-Src (IC50 = 7 µM). Its activity is assessed using biochemical kinase assays that measure the phosphorylation of a substrate in the presence of the compound. It blocks VEGF-induced signaling to suppress endothelial cell proliferation and angiogenesis.
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| ln Vivo |
In vivo, VEGFR-IN-1 is a potent angiogenesis inhibitor that is widely used in anti-tumor angiogenesis research. By blocking VEGF-induced signaling, it suppresses endothelial cell proliferation and angiogenesis. Its efficacy would be evaluated in animal models of cancer, where tumor growth and angiogenesis are monitored to assess the compound's anti-tumor activity.
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| Enzyme Assay |
Cell-free assays for VEGFR-IN-1 typically involve measuring its inhibitory activity against VEGFR2 (KDR) and other kinases using biochemical kinase assays. The IC50 values are determined by measuring the phosphorylation of a peptide substrate in the presence of varying concentrations of the inhibitor. These assays are used to characterize the compound's potency and selectivity profile against a panel of kinases.
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| Cell Assay |
In vitro cellular assays are conducted to evaluate the functional activity of VEGFR-IN-1. Endothelial cells are treated with VEGF in the presence or absence of the compound. VEGFR2 phosphorylation is measured to assess the inhibition of VEGF-induced signaling. Endothelial cell proliferation, migration, and tube formation assays are used to evaluate the compound's anti-angiogenic activity. These assays confirm that VEGFR-IN-1 effectively blocks VEGF-mediated angiogenesis.
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| Animal Protocol |
In vivo animal experiments typically involve xenograft models of cancer. Mice bearing tumors are administered VEGFR-IN-1. Tumor growth and angiogenesis are monitored over time to assess the compound's efficacy. These studies are essential for demonstrating the in vivo anti-angiogenic and anti-tumor activity of the compound.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of VEGFR-IN-1 are typical of a small molecule inhibitor. Its molecular weight is 337.8. While detailed PK parameters are not widely published, its properties suggest it is designed to have favorable drug-like characteristics to support efficacy in vivo. It is soluble in DMSO.
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| Toxicity/Toxicokinetics |
The toxicity profile of VEGFR-IN-1 is not extensively documented. As a research compound, standard safety precautions should be taken when handling it. Its use is restricted to research purposes and it is not intended for human consumption. Preclinical studies would be required to fully assess its safety profile.
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| References | |
| Additional Infomation |
VEGFR-IN-1 is a research compound that is widely used as a potent angiogenesis inhibitor in cancer research. Its ability to potently inhibit VEGFR2 (IC50 = 3 nM) and block VEGF-induced signaling makes it a valuable tool for studying angiogenesis and developing anti-cancer therapies. The compound is not approved for therapeutic use.
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| Molecular Formula |
C19H16CLN3O
|
|---|---|
| Molecular Weight |
337.80
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| Exact Mass |
337.098
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| CAS # |
269390-69-4
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| PubChem CID |
9797919
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| Appearance |
White to off-white solid powder
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| LogP |
4.745
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
24
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| Complexity |
392
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C(C(=C1)C(=O)NC2=CC=C(C=C2)Cl)NCC3=CC=NC=C3
|
| InChi Key |
GGPZCOONYBPZEW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H16ClN3O/c20-15-5-7-16(8-6-15)23-19(24)17-3-1-2-4-18(17)22-13-14-9-11-21-12-10-14/h1-12,22H,13H2,(H,23,24)
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| Chemical Name |
N-(4-chlorophenyl)-2-(pyridin-4-ylmethylamino)benzamide
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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 Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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: 125 mg/mL (370.04 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (6.16 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (6.16 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9603 mL | 14.8017 mL | 29.6033 mL | |
| 5 mM | 0.5921 mL | 2.9603 mL | 5.9207 mL | |
| 10 mM | 0.2960 mL | 1.4802 mL | 2.9603 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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