| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| 1g | |||
| Other Sizes |
Purity: ≥98%
| Targets |
Flk-1 (IC50 = 9.6 μM)
SU 5205 is a VEGFR2 inhibitor that specifically targets and inhibits the activity of vascular endothelial growth factor receptor 2 (VEGFR2), a receptor involved in angiogenesis and the formation of new blood vessels. VEGFR2 is the primary receptor for VEGF-mediated angiogenesis. By inhibiting VEGFR2, SU 5205 blocks the signaling pathways that promote endothelial cell proliferation, migration, and tube formation. The compound inhibits ligand-induced VEGF endothelial mitogenesis. Its mechanism of action involves the inhibition of VEGFR2 tyrosine kinase activity. |
|---|---|
| ln Vitro |
SU5205 suppresses VEGF-induced endothelial mitogenesis with an IC50 of 5.1 μM[1].
In vitro, SU 5205 inhibits human umbilical vein endothelial cell (HUVEC) mitogenesis induced by VEGF or acidic FGF with IC50 values of 0.9 and 0.6 μM, respectively. It inhibits ligand-induced VEGF endothelial mitogenesis with an IC50 of 5.1 μM. The compound shows an IC50 of 9.6 μM for VEGFR2 (FLK-1) inhibition. Its in vitro activity is characterized by potent inhibition of VEGFR2 signaling and endothelial cell proliferation. |
| ln Vivo |
In vivo, SU 5205 has been studied for its 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 5205 is primarily used as a research tool for studying VEGFR2 biology and angiogenesis.
|
| Enzyme Assay |
In vitro enzyme assays for SU 5205 typically involve measuring the inhibition of VEGFR2 (FLK-1) tyrosine kinase activity. The compound inhibits VEGFR2 with an IC50 of 9.6 μM. These assays confirm the compound's mechanism of action as a VEGFR2 inhibitor. The compound's selectivity for VEGFR2 over other kinases can also be assessed.
|
| Cell Assay |
In vitro cellular assays for SU 5205 typically involve treating human umbilical vein endothelial cells (HUVECs) with the compound and measuring mitogenesis induced by VEGF or acidic FGF. The compound inhibits VEGF- and FGF-induced mitogenesis with IC50 values of 0.9 and 0.6 μM, respectively. These cell-based studies demonstrate the compound's functional inhibition of VEGFR2 signaling and endothelial cell proliferation.
|
| Animal Protocol |
In vivo animal models for SU 5205 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 5205 is limited in the available literature. The compound is primarily used as a research tool for studying VEGFR2 biology and angiogenesis.
|
| ADME/Pharmacokinetics |
SU 5205 has a molecular formula of C15H10FNO and a molecular weight of 239.25 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 5205's solubility and formulation for administration should be optimized based on specific experimental requirements. The compound is a VEGFR2 inhibitor used in angiogenesis research.
|
| Toxicity/Toxicokinetics |
SU 5205 is a VEGFR2 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 angiogenesis. The compound's safety profile should be evaluated in preclinical toxicology studies. SU 5205 is for research use only and is not approved for human therapeutic use. It represents a valuable tool for studying VEGFR2 biology and angiogenesis.
|
| References |
|
| Additional Infomation |
SU 5205 (CAS# 3476-86-6) is an inhibitor of VEGFR2 (FLK-1), a receptor tyrosine kinase involved in angiogenesis, with an IC50 of 9.6 μM. It inhibits ligand-induced VEGF endothelial mitogenesis with an IC50 of 5.1 μM. SU 5205 inhibits human umbilical vein endothelial cell (HUVEC) mitogenesis induced by VEGF or acidic FGF with IC50 values of 0.9 and 0.6 μM, respectively. The compound is for research use only and is not approved for human therapeutic use.
|
| Molecular Formula |
C15H10FNO
|
|---|---|
| Molecular Weight |
239.2494
|
| Exact Mass |
239.075
|
| Elemental Analysis |
C, 75.30; H, 4.21; F, 7.94; N, 5.85; O, 6.69
|
| CAS # |
3476-86-6
|
| Related CAS # |
3476-86-6
|
| PubChem CID |
5398217
|
| Appearance |
Yellow solid powder
|
| LogP |
3.456
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
1
|
| Heavy Atom Count |
18
|
| Complexity |
358
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
FC1C([H])=C([H])C(=C([H])C=1[H])C([H])=C1C(N([H])C2=C([H])C([H])=C([H])C([H])=C12)=O
|
| InChi Key |
QIERHADIMMFZNE-LCYFTJDESA-N
|
| InChi Code |
InChI=1S/C15H10FNO/c16-11-7-5-10(6-8-11)9-13-12-3-1-2-4-14(12)17-15(13)18/h1-9H,(H,17,18)/b13-9-
|
| Chemical Name |
(3Z)-3-[(4-fluorophenyl)methylidene]-1H-indol-2-one
|
| Synonyms |
SU 5205; SU5205; SU-5205
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO: 48~250 mg/mL (200.6~1045.0 mM)
Ethanol: ~3 mg/mL (12.5 mM) |
|---|---|
| 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 | 4.1797 mL | 20.8986 mL | 41.7973 mL | |
| 5 mM | 0.8359 mL | 4.1797 mL | 8.3595 mL | |
| 10 mM | 0.4180 mL | 2.0899 mL | 4.1797 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA