| Size | Price | Stock | Qty |
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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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| 250mg |
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| 500mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
VEGFR2 (IC50 = 14.8 μM); EGFR (IC50 = 36.7 μM)
SU 5214 is a potent VEGFR2 inhibitor that also inhibits EGFR. It is a modulator of tyrosine kinase signal transduction. The compound has IC50s of 14.8 μM for FLK-1 (VEGFR2) and 36.7 μM for EGFR. By inhibiting these receptor tyrosine kinases, SU 5214 modulates signaling pathways involved in angiogenesis and cell proliferation. Its mechanism of action involves the inhibition of VEGFR2 and EGFR tyrosine kinase activities. |
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| ln Vitro |
In vitro, SU 5214 induces NQO1 activity with a ratio of 4.03 and CYP1A1 activity with a ratio of 2.48 in mouse Hepa-1c1c7 cells at a concentration of 1 μM after 48 hours. It has IC50s of 14.8 μM for FLK-1 (VEGFR2) and 36.7 μM for EGFR. Its in vitro activity is characterized by inhibition of VEGFR2 and EGFR signaling and modulation of NQO1 and CYP1A1 activities.
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| ln Vivo |
In vivo, SU 5214 has been studied for its potential anti-angiogenic and anti-tumor effects in preclinical models. As a VEGFR2 inhibitor, it blocks angiogenesis, thereby limiting the supply of nutrients and oxygen to tumors. However, detailed in vivo efficacy data for specific disease models are limited in the available literature. SU 5214 is primarily used as a research tool for studying VEGFR2 and EGFR biology.
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| Enzyme Assay |
In vitro enzyme assays for SU 5214 typically involve measuring the inhibition of VEGFR2 (FLK-1) and EGFR tyrosine kinase activities. The compound inhibits VEGFR2 with an IC50 of 14.8 μM and EGFR with an IC50 of 36.7 μM. These assays confirm the compound's mechanism of action as a VEGFR2 and EGFR inhibitor.
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| Cell Assay |
In vitro cellular assays for SU 5214 typically involve treating cells such as mouse Hepa-1c1c7 cells with the compound and measuring NQO1 and CYP1A1 activities. The compound induces NQO1 activity with a ratio of 4.03 and CYP1A1 activity with a ratio of 2.48 at 1 μM after 48 hours. These cell-based studies demonstrate the compound's effects on drug-metabolizing enzymes.
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| Animal Protocol |
In vivo animal models for SU 5214 may include xenograft tumor models to evaluate its anti-angiogenic and anti-tumor effects. The compound is administered by appropriate routes, and tumor growth inhibition is measured. However, detailed animal protocol information for SU 5214 is limited in the available literature. The compound is primarily used as a research tool for studying VEGFR2 and EGFR biology.
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| ADME/Pharmacokinetics |
SU 5214 has a molecular formula of C21H21NO2 and a molecular weight of 319.4 g/mol. The compound is typically stored under appropriate conditions to maintain stability. Its physicochemical properties support its use in both in vitro and in vivo studies. SU 5214's solubility and formulation for administration should be optimized based on specific experimental requirements. The compound is a modulator of tyrosine kinase signal transduction.
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| Toxicity/Toxicokinetics |
SU 5214 is a VEGFR2 and EGFR inhibitor with a well-characterized mechanism of action. As with any kinase inhibitor, potential toxicity may include off-target effects on other kinases and disruption of normal cellular signaling. The compound's safety profile should be evaluated in preclinical toxicology studies. SU 5214 is for research use only and is not approved for human therapeutic use. It represents a valuable tool for studying VEGFR2 and EGFR biology.
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| References | |
| Additional Infomation |
SU 5214 (CAS# 186611-04-1) is a potent VEGFR2 inhibitor with IC50s of 14.8 μM for FLK-1 (VEGFR2) and 36.7 μM for EGFR. It is a modulator of tyrosine kinase signal transduction. SU 5214 induces NQO1 activity with a ratio of 4.03 and CYP1A1 activity with a ratio of 2.48 in mouse Hepa-1c1c7 cells at 1 μM after 48 hours. The compound is for research use only and is not approved for human therapeutic use.
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| Molecular Formula |
C16H13NO2
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|---|---|
| Molecular Weight |
251.279924154282
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| Exact Mass |
251.094
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| Elemental Analysis |
C, 76.48; H, 5.21; N, 5.57; O, 12.73
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| CAS # |
186611-04-1
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| Related CAS # |
186611-04-1
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| PubChem CID |
672251
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| Appearance |
White to yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
469.4±45.0 °C at 760 mmHg
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| Flash Point |
237.7±28.7 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.657
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| LogP |
3.42
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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 |
2
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| Heavy Atom Count |
19
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| Complexity |
377
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C1C(=CC2C=CC=CC=2OC)C2C=CC=CC=2N1
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| InChi Key |
NEQZEVOPIKSAJP-RAXLEYEMSA-N
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| InChi Code |
InChI=1S/C16H13NO2/c1-19-15-9-5-2-6-11(15)10-13-12-7-3-4-8-14(12)17-16(13)18/h2-10H,1H3,(H,17,18)/b13-10-
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| Chemical Name |
(3Z)-3-[(2-methoxyphenyl)methylidene]-1H-indol-2-one
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| Synonyms |
SU 5214
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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: 50~100 mg/mL (199~398 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 | 3.9796 mL | 19.8981 mL | 39.7962 mL | |
| 5 mM | 0.7959 mL | 3.9796 mL | 7.9592 mL | |
| 10 mM | 0.3980 mL | 1.9898 mL | 3.9796 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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