| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
Tie2 8.56 nM (pIC50) VEGFR-2 Tie-2
TIE-2/VEGFR-2 kinase-IN-2 targets VEGFR2 and Tie-2, two key receptor tyrosine kinases involved in angiogenesis. By inhibiting both targets, it blocks the signaling pathways that promote endothelial cell proliferation, migration, and survival. It also inhibits RIPK1, a kinase involved in necroptosis and inflammation, which may contribute to its therapeutic effects. |
|---|---|
| ln Vitro |
In vitro, TIE-2/VEGFR-2 kinase-IN-2 has been shown to be a potent inhibitor of VEGFR2 and Tie-2 kinase activity, with pIC50 values of 8.61 and 8.56, respectively. Its inhibitory activity is typically assessed using kinase assays. These studies confirm its potential as an anti-angiogenic agent.
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| ln Vivo |
In vivo, TIE-2/VEGFR-2 kinase-IN-2 has demonstrated anti-angiogenic activity in animal models. It can be used for cancer research and may have applications in ocular diseases such as age-related macular degeneration. These studies provide evidence for its therapeutic potential.
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| Enzyme Assay |
Cell-free assays for TIE-2/VEGFR-2 kinase-IN-2 typically involve measuring its inhibitory activity against VEGFR2 and Tie-2 kinases using biochemical kinase assays. The pIC50 values are 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.
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| Cell Assay |
In vitro cellular assays are conducted to evaluate the functional activity of TIE-2/VEGFR-2 kinase-IN-2. Endothelial cells are treated with the compound in the presence of angiogenic factors, and cell proliferation, migration, and tube formation are measured to assess its anti-angiogenic activity. Receptor phosphorylation is measured to confirm target engagement.
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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 activity.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of TIE-2/VEGFR-2 kinase-IN-2 are typical of a small molecule kinase inhibitor. Its molecular weight is 431.34. 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.
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| Toxicity/Toxicokinetics |
The toxicity profile of TIE-2/VEGFR-2 kinase-IN-2 is not extensively documented, but it is likely to be similar to other VEGFR inhibitors. Common adverse effects may include hypertension, fatigue, and proteinuria. 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 | |
| Additional Infomation |
TIE-2/VEGFR-2 kinase-IN-2 is a research compound used to study angiogenesis and cancer. It is a potent dual inhibitor of VEGFR2 and Tie-2. The compound is not approved for therapeutic use and is intended for research purposes only.
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| Molecular Formula |
C20H13F4N5O2
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|---|---|
| Molecular Weight |
431.34313750267
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| Exact Mass |
431.1
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| CAS # |
501693-48-7
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| PubChem CID |
10113568
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| Appearance |
White to off-white solid powder
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| LogP |
3.8
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
31
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| Complexity |
631
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1C=CC(C(F)(F)F)=CC=1NC(NC1C=CC(=CC=1)C1=COC2C1=C(N)N=CN=2)=O
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| InChi Key |
KNDPXYAMINMLED-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H13F4N5O2/c21-14-6-3-11(20(22,23)24)7-15(14)29-19(30)28-12-4-1-10(2-5-12)13-8-31-18-16(13)17(25)26-9-27-18/h1-9H,(H2,25,26,27)(H2,28,29,30)
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| Chemical Name |
1-[4-(4-aminofuro[2,3-d]pyrimidin-5-yl)phenyl]-3-[2-fluoro-5-(trifluoromethyl)phenyl]urea
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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: 50 mg/mL (115.92 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (11.59 mM) (saturation unknown) 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.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (50.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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: ≥ 5 mg/mL (11.59 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 DMSO stock solution (50.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3184 mL | 11.5918 mL | 23.1836 mL | |
| 5 mM | 0.4637 mL | 2.3184 mL | 4.6367 mL | |
| 10 mM | 0.2318 mL | 1.1592 mL | 2.3184 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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