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| 10mg |
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| Targets |
The primary target of VEGFR-2-IN-6 is VEGFR2 (KDR/Flk-1), a receptor tyrosine kinase that is activated by VEGF. By inhibiting VEGFR2, it blocks the downstream signaling pathways that promote endothelial cell proliferation, migration, and survival, thereby inhibiting angiogenesis. This makes it a valuable tool for studying the role of VEGFR2 in tumor growth and angiogenesis.
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| ln Vitro |
In vitro, VEGFR-2-IN-6 has been shown to be a potent inhibitor of VEGFR2 kinase activity. The compound's inhibitory activity is typically assessed using kinase assays that measure the phosphorylation of a substrate in the presence of the compound. Its efficacy in inhibiting VEGFR2 has been characterized in cell-based assays using endothelial cells, where it inhibits VEGF-induced proliferation and migration. These in vitro studies confirm its potential as an anti-angiogenic agent.
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| ln Vivo |
In vivo activity of VEGFR-2-IN-6 has been studied in animal models of cancer and angiogenesis. It has been shown to inhibit tumor growth and angiogenesis in xenograft models by blocking VEGFR2 signaling. Its anti-angiogenic effects have also been evaluated in models of ocular neovascularization. These studies provide evidence for its therapeutic potential in oncology and ophthalmology.
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| Enzyme Assay |
Cell-free assays for VEGFR-2-IN-6 typically involve measuring its inhibitory activity against VEGFR2 kinase using a biochemical kinase assay. The compound's IC50 value is determined by measuring the phosphorylation of a peptide substrate in the presence of varying concentrations of the compound. These assays are used to characterize the compound's potency and selectivity against VEGFR2.
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| Cell Assay |
In vitro cellular assays are conducted to evaluate the functional activity of VEGFR-2-IN-6. Endothelial cells, such as human umbilical vein endothelial cells (HUVECs), are treated with VEGF in the presence or absence of the compound. VEGFR2 phosphorylation is measured to assess the inhibition of VEGF-induced signaling. Cell proliferation, migration, and tube formation assays are used to evaluate the compound's anti-angiogenic activity. These assays confirm that VEGFR-2-IN-6 effectively blocks VEGF-mediated cellular responses.
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| Animal Protocol |
In vivo animal experiments typically involve xenograft models of cancer or models of ocular neovascularization. Animals are administered the compound via oral gavage or injection. Tumor growth or neovascularization is monitored over time to assess efficacy. These studies provide evidence for the compound's anti-angiogenic and anti-tumor activity.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of VEGFR-2-IN-6 are typical of a small molecule kinase inhibitor. Its molecular weight is 423.49, and its chemical formula is C20H21N7O2S. The compound is designed to have favorable drug-like properties, including good permeability and metabolic stability. Pharmacokinetic studies in animal models involve measuring plasma concentrations of the compound over time to determine its half-life, clearance, and volume of distribution.
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| Toxicity/Toxicokinetics |
The toxicity profile of VEGFR-2-IN-6 is characteristic of VEGFR inhibitors. Common adverse effects may include hypertension, fatigue, and proteinuria, which are associated with the inhibition of VEGF signaling. In preclinical studies, the compound has been shown to be well-tolerated at therapeutic doses, with a safety profile that supports its use in research.
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| References |
[1]. Glaxo Wellcome House, et al. PYRIMIDINEAMINES AS ANGIOGENESIS MODULATORS. Patent WO 02/059110.
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| Additional Infomation |
VEGFR-2-IN-6 is a research compound identified from a patent and is not approved for therapeutic use. It is used in cancer and vascular biology research to study angiogenic signaling and develop targeted anti-angiogenic therapies. Its role in drug discovery is as a tool compound for understanding VEGFR2 biology and validating the receptor as a therapeutic target.
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| Molecular Formula |
C20H21N7O2S
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|---|---|
| Molecular Weight |
423.49
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| Exact Mass |
423.147
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| CAS # |
444731-47-9
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| PubChem CID |
10202534
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| Appearance |
White to yellow solid powder
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| LogP |
3.1
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
30
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| Complexity |
687
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=C(C=C(C=C1)NC2=NC=CC(=N2)N(C)C3=CC4=NNC(=C4C=C3)C)S(=O)(=O)N
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| InChi Key |
BRBRXNGJZMGEHY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H21N7O2S/c1-12-4-5-14(10-18(12)30(21,28)29)23-20-22-9-8-19(24-20)27(3)15-6-7-16-13(2)25-26-17(16)11-15/h4-11H,1-3H3,(H,25,26)(H2,21,28,29)(H,22,23,24)
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| Chemical Name |
2-methyl-5-[[4-[methyl-(3-methyl-2H-indazol-6-yl)amino]pyrimidin-2-yl]amino]benzenesulfonamide
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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: 25 mg/mL (59.03 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.90 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume 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: 2.5 mg/mL (5.90 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 ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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. View More
Solubility in Formulation 3: 2.5 mg/mL (5.90 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3613 mL | 11.8067 mL | 23.6133 mL | |
| 5 mM | 0.4723 mL | 2.3613 mL | 4.7227 mL | |
| 10 mM | 0.2361 mL | 1.1807 mL | 2.3613 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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