| Size | Price | Stock | Qty |
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| 2mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
VEGFR2
SU5208 primarily targets VEGFR2 (also known as KDR), a receptor tyrosine kinase that plays a central role in angiogenesis. It also inhibits other kinases such as PDGFR and c-Kit, making it a multi-targeted inhibitor. Its IC50 for VEGFR2 is 0.02 µM (20 nM). By blocking VEGFR2 signaling, SU5208 effectively impedes angiogenesis and tumor growth. |
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| ln Vitro |
In vitro, SU5208 potently inhibits VEGFR2 kinase activity with an IC50 of 0.02 µM (20 nM) in cell-free kinase assays. It is used as a reference inhibitor in studies of angiogenesis, tumor vascular biology, and kinase signaling pathways. Its activity is well-documented in the literature.
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| ln Vivo |
In vivo, SU5208 is utilized in research to study angiogenesis and tumor growth. By inhibiting VEGFR2 and other angiogenic receptors, it can potentially suppress tumor vascularization and growth in preclinical models. Its effectiveness in blocking angiogenesis makes it a valuable tool for cancer research.
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| Enzyme Assay |
In vitro kinase assays are performed using purified VEGFR2 enzyme. The compound is incubated with the enzyme and a substrate (e.g., a peptide or ATP). The degree of phosphorylation is measured, and the IC50 is calculated. This assay allows for the direct assessment of the compound's potency against its primary target.
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| Cell Assay |
Cells expressing VEGFR2, such as endothelial cells, are treated with SU5208. The compound's effect on VEGF-stimulated cell proliferation, migration, or tube formation is measured to assess its functional anti-angiogenic activity. These cellular assays confirm the compound's mechanism of action.
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| Animal Protocol |
The anti-angiogenic and antitumor activity of SU5208 is typically evaluated in mouse models. For example, its effect on tumor growth and angiogenesis can be assessed in xenograft models or in models of neovascularization. These in vivo studies are crucial for evaluating the compound's potential as a therapeutic agent.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of SU5208, such as its absorption, distribution, metabolism, and excretion, would be studied in preclinical species to understand its systemic exposure and guide in vivo dosing.
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| Toxicity/Toxicokinetics |
The toxicity profile of SU5208 would be evaluated in standard toxicology studies. Given its mechanism as a kinase inhibitor, potential off-target effects and toxicities would need to be characterized.
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| References | |
| Additional Infomation |
SU5208 is a well-characterized tool compound in the indolinone class of kinase inhibitors. It serves as a reference for understanding structure-activity relationships in this class and for studying angiogenesis and kinase signaling. It is a valuable tool in cancer research.
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| Molecular Formula |
C13H9NOS
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|---|---|
| Molecular Weight |
227.28166
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| Exact Mass |
227.04
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| Elemental Analysis |
C, 68.70; H, 3.99; N, 6.16; O, 7.04; S, 14.11
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| CAS # |
62540-08-3
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| Related CAS # |
62540-08-3
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| PubChem CID |
727529
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| Appearance |
Yellow to orange solid powder
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| LogP |
3.378
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
16
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| Complexity |
326
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C2C(=C1)C(=CC3=CC=CS3)C(=O)N2
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| InChi Key |
QMTIIBUDOBNABZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H9NOS/c15-13-11(8-9-4-3-7-16-9)10-5-1-2-6-12(10)14-13/h1-8H,(H,14,15)
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| Chemical Name |
3-(thiophen-2-ylmethylidene)-1H-indol-2-one
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| Synonyms |
thienylmethylene oxindole; 3-[(Thien-2-yl)methylene]-2-indolinone; 3-[(Thien-2-yl)methylene]-2-indolinone; 3-(thiophen-2-ylmethylidene)-1H-indol-2-one; SU5208; Maybridge3_000930
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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: ~45 mg/mL (~198.0 mM)
Ethanol: ~2 mg/mL (~8.8 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 | 4.3999 mL | 21.9993 mL | 43.9986 mL | |
| 5 mM | 0.8800 mL | 4.3999 mL | 8.7997 mL | |
| 10 mM | 0.4400 mL | 2.1999 mL | 4.3999 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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