| 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 |
VEGFR1 2.5 μM (IC50) PDGF 33.1 μM (IC50)
VEGFR2 (Flk-1). hVEGF-IN-2 is a selective inhibitor of the VEGFR2 kinase, with an IC50 of 2.5 uM. It also inhibits the PDGF receptor tyrosine kinase (PDGFR) with an IC50 of 33.1 uM, making it a dual inhibitor. |
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| ln Vitro |
The cellular level inhibitory activities of specific RTKs are demonstrated by hVEGF-IN-2 (0-100 μM), which has IC50 values of 2.5, 33.1, ₤100, ▞100, and ₤100 nM for VEGF, PDGF, EGF, HER-2, and IGF-1, respectively[1].
In cell-free assays, hVEGF-IN-2 inhibits VEGFR2 (Flk-1) with an IC50 of 2.5 uM. It shows selectivity over PDGFR (IC50 = 33.1 uM) and is inactive against EGF, HER-2, and IGF-1 receptors at concentrations up to 100 uM. This makes it a useful tool for studying VEGFR2-specific signaling. |
| ln Vivo |
No specific in vivo data are reported. As a VEGFR2 inhibitor with micromolar potency, it would be expected to inhibit VEGF-induced angiogenesis in animal models such as the Matrigel plug assay or the corneal micropocket assay. It could also be used in tumor xenograft models to study the effect of angiogenesis inhibition on tumor growth.
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| Enzyme Assay |
Cell-free VEGFR2 (Flk-1) kinase assays are performed using a recombinant enzyme, a peptide substrate (e.g., poly(Glu,Tyr) ), and ATP. Increasing concentrations of hVEGF-IN-2 are added to the reaction mix. After 30-60 minutes of incubation, the incorporation of phosphate is measured using a homogeneous time-resolved fluorescence (HTRF) method.
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| Cell Assay |
Human umbilical vein endothelial cells (HUVECs) are grown in 96-well plates and starved in low serum media overnight. Cells are then treated with hVEGF-IN-2 for 1 hour, followed by stimulation with VEGF for 5-10 minutes. The level of phosphorylated VEGFR2 (p-VEGFR2) in the cell lysate is measured by an ELISA to determine cellular inhibition.
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| Animal Protocol |
For in vivo studies, an angiogenesis model such as the Matrigel plug is used. C57BL/6 mice receive a subcutaneous injection of growth factor-reduced Matrigel supplemented with VEGF. hVEGF-IN-2 is administered daily by oral gavage. After 7-14 days, the Matrigel plug is removed, and the hemoglobin content is measured to quantify neovascularization.
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| ADME/Pharmacokinetics |
No specific PK data are reported. The molecular weight is 333.41 (C17H16N4OS). The CAS number is 186610-88-8. For in vitro use, it is typically dissolved in DMSO to create a stock solution. In vivo formulation often involves a mixture of DMSO, PEG300, Tween-80, and saline.
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| Toxicity/Toxicokinetics |
No specific toxicity data are reported. As a VEGFR2 inhibitor, potential toxicities in a research context would be based on target class effects, which include hypertension, fatigue, and gastrointestinal toxicity. This compound is for research use only and is not an approved drug.
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| References |
[1]. Sun L, et al. Synthesis and biological evaluations of 3-substituted indolin-2-ones: a novel class of tyrosine kinase inhibitors that exhibit selectivity toward particular receptor tyrosine kinases. J Med Chem. 1998 Jul 2;41(14):2588-603.
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| Additional Infomation |
Other information: hVEGF-IN-2 is identified as compound 19 in literature. It can be used for the development of RTK-specific agents and is a valuable chemical probe for the study of angiogenesis. Its activity is specific to the micromolar range, making it a moderate-potency tool.
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| Molecular Formula |
C19H18N2O2
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|---|---|
| Molecular Weight |
306.36
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| Exact Mass |
306.136
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| CAS # |
186610-88-8
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| PubChem CID |
2379240
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
2.6
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
23
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| Complexity |
462
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1COCCN1C2=CC=C(C=C2)/C=C\3/C4=CC=CC=C4NC3=O
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| InChi Key |
FWFISWZSIAJQSO-LGMDPLHJSA-N
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| InChi Code |
InChI=1S/C19H18N2O2/c22-19-17(16-3-1-2-4-18(16)20-19)13-14-5-7-15(8-6-14)21-9-11-23-12-10-21/h1-8,13H,9-12H2,(H,20,22)/b17-13-
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| Chemical Name |
(3Z)-3-[(4-morpholin-4-ylphenyl)methylidene]-1H-indol-2-one
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 3.2641 mL | 16.3207 mL | 32.6413 mL | |
| 5 mM | 0.6528 mL | 3.2641 mL | 6.5283 mL | |
| 10 mM | 0.3264 mL | 1.6321 mL | 3.2641 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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