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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
VEGFR2[1]
The primary target of VEGFR-2-IN-5 hydrochloride 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 ocular diseases such as age-related macular degeneration. |
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| ln Vitro |
In vitro studies have demonstrated that VEGFR-2-IN-5 hydrochloride is 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-5 hydrochloride 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, such as laser-induced choroidal neovascularization in mice. 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-5 hydrochloride 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-5 hydrochloride. 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-5 hydrochloride 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-5 hydrochloride are typical of a small molecule kinase inhibitor. The hydrochloride salt form enhances its solubility and oral bioavailability. Its molecular weight is 400.91, and its chemical formula is C19H25ClN8. 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-5 hydrochloride 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. Toxicological studies involve acute and chronic dosing in animal models to assess safety margins.
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| References | |
| Additional Infomation |
VEGFR-2-IN-5 hydrochloride is a research compound extracted from a patent and is not approved for therapeutic use. It is used in cancer and ophthalmology research to study anti-angiogenic mechanisms and develop targeted 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 |
C19H25CLN8
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| Molecular Weight |
400.91
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| Exact Mass |
400.189
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| CAS # |
2700435-52-3
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| Related CAS # |
VEGFR-2-IN-5;1430089-64-7
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| PubChem CID |
154925632
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| Appearance |
Off-white to light yellow solid powder
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
28
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| Complexity |
437
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CC1C2=CC(=NN2)NC3=NC(=NC=C3)NC4=CC=C(C=C4)NCCCN.Cl
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| InChi Key |
CQMVZDBUFYZLTC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H24N8.ClH/c20-9-1-10-21-14-4-6-15(7-5-14)23-19-22-11-8-17(25-19)24-18-12-16(26-27-18)13-2-3-13;/h4-8,11-13,21H,1-3,9-10,20H2,(H3,22,23,24,25,26,27);1H
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| Chemical Name |
2-N-[4-(3-aminopropylamino)phenyl]-4-N-(5-cyclopropyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine;hydrochloride
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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: 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: 230 mg/mL (573.69 mM)
H2O: 100 mg/mL (249.43 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 | 2.4943 mL | 12.4716 mL | 24.9433 mL | |
| 5 mM | 0.4989 mL | 2.4943 mL | 4.9887 mL | |
| 10 mM | 0.2494 mL | 1.2472 mL | 2.4943 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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