| Size | Price | Stock | Qty |
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| 25mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
Flk-1 (IC50 = 700 nM)
SU-1498 is a selective inhibitor of the receptor tyrosine kinase VEGF receptor 2 (VEGFR2), also known as Flk-1. It is a potent, reversible inhibitor with an IC50 of 700 nM. By inhibiting VEGFR2, SU-1498 blocks the signaling pathways that promote angiogenesis, endothelial cell proliferation, and migration. The compound has negligible activity at several other serine/threonine and tyrosine kinases, indicating selectivity for VEGFR2. Its mechanism of action involves the inhibition of VEGFR2 tyrosine kinase activity. |
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| ln Vitro |
SU1498 encourages the build-up of phosphorylated extracellular kinases (ERKs) in human aortic and umbilical vein endothelial cells. This process is contingent upon the activity of B-Raf, MEK kinases, and the upstream elements of the MAPK pathway. SU1498 is ineffective on its own; the increased accumulation of phospho-ERKs is only seen in cells that have been stimulated with sphingosine 1-phosphate or protein growth factors[2]. In MS1 VEGF cells, SU1498 inhibits VEGFR2 signal transduction.Ets-1 expression levels are reduced in the presence of SU1498, indicating that VEGF-VEGFR-2 interactions supported baseline levels of Ets-1 expression and that disruption of this autocrine interaction with SU1498 resulted in decreased expression of Ets-1[3]. U87 cell apoptosis and proliferation are markedly impacted by SU1498 treatment. Glycerophosphocholine decreases and lipids increase significantly when exposed to SU1498. Consequently, the cytoplasm of U87 cells treated with SU1498 exhibits an accumulation of lipid droplets[4].
In vitro, SU-1498 inhibits VEGFR2 (Flk-1) with an IC50 of 700 nM. It is a potent, reversible, and selective inhibitor of VEGFR-2. Inhibition of VEGFR-2 blocks angiogenesis in in vitro models. The compound is cell-permeable. Its in vitro activity is characterized by potent and selective inhibition of VEGFR2 signaling and angiogenesis. |
| ln Vivo |
In vivo, SU-1498 inhibits VEGFR2 and blocks angiogenesis in in vivo models. It is used to study the role of VEGFR2 signaling in diverse processes, including angiogenesis, tumor growth, neural progenitor cell survival, and neuroregeneration. However, detailed in vivo efficacy data for specific disease models are limited in the available literature. SU-1498 is primarily used as a research tool for studying VEGFR2 biology.
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| Enzyme Assay |
Pipetted into tubes (1 μL each), the ERK1 or ERK2 solution is combined with 0–10 μL of 50 μM SU1498 (in kinase buffer without ATP). Buffered tube only receives buffer. The mixtures are incubated for 10 minutes at 25°C after the volume is adjusted to 11 μL using the same buffer. After that, 40 μL of the Elk1-ATP-buffer solution is added, and the incubations are kept going for 30 minutes at 30°C. After heating the mixture of 4× sample buffer mix for 10 minutes at 95°C, 20 μL is added to stop the reactions. SDS-PAGE is used to fractionate the samples (15 μL), and anti-phospho-Elk1 antibody is used for immunoblotting to identify phosphorylated Elk1[2].
In vitro enzyme assays for SU-1498 typically involve measuring the inhibition of VEGFR2 (Flk-1) tyrosine kinase activity. The compound inhibits VEGFR2 with an IC50 of 700 nM. 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 order to perform the cell proliferation assay, 30,000 U87 cells are seeded in each well of a 24-well plate and left to attach overnight. Next, the cells are treated in triplicate wells for 24 or 72 hours at varying concentrations of either SU1498 (1 µM to 30 µM) or bevacizumab (10 ng/mL to 250 µg/mL). After that, the MTT test is used to evaluate the cell viability[4].
In vitro cellular assays for SU-1498 typically involve treating endothelial cells with the compound and measuring VEGF-induced proliferation, migration, or tube formation. The compound inhibits VEGFR2 signaling and blocks angiogenesis in these assays. These cell-based studies demonstrate the compound's functional inhibition of VEGFR2 signaling and angiogenesis. |
| Animal Protocol |
In vivo animal models for SU-1498 may include xenograft tumor models or models of angiogenesis, neuroregeneration, or other processes where VEGFR2 signaling plays a role. The compound is administered by appropriate routes, and angiogenesis, tumor growth, or other endpoints are assessed. However, detailed animal protocol information for SU-1498 is limited in the available literature. The compound is primarily used as a research tool.
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| ADME/Pharmacokinetics |
SU-1498 has a molecular formula of C25H30N2O2 and a molecular weight of 390.52 g/mol. Its chemical name is (E)-N-(3''-Phenylpropyl)-α-cyano-3',5'-diisopropyl-4'-hydroxycinnamamide. 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-1498's solubility and formulation for administration should be optimized based on specific experimental requirements.
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| Toxicity/Toxicokinetics |
SU-1498 is a selective 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-1498 is for research use only and is not approved for human therapeutic use. It represents a valuable tool for studying VEGFR2 biology and angiogenesis.
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| References | |
| Additional Infomation |
SU1498 is a monocarboxylic acid amide formed by the condensation of the carboxyl group of (2E)-2-cyano-3-[4-hydroxy-3,5-di(prop-2-yl)phenyl]prop-2-enoic acid with the amino group of 3-phenylpropylamine. It is a vascular endothelial growth factor receptor antagonist. SU1498 belongs to the classes of enamides, phenolic compounds, nitrile compounds, monocarboxylic acid amides, and secondary amides.
SU-1498 (CAS# 168835-82-3) is a selective inhibitor of the receptor tyrosine kinase VEGF receptor 2 (VEGFR2), also known as Flk-1, with an IC50 of 700 nM. It is a potent, reversible, and selective inhibitor of VEGFR-2. SU-1498 is used to study the role of VEGFR2 signaling in diverse processes, including angiogenesis, tumor growth, neural progenitor cell survival, and neuroregeneration. The compound is for research use only and is not approved for human therapeutic use. |
| Molecular Formula |
C25H30N2O2
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| Molecular Weight |
390.527
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| Exact Mass |
390.23
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| Elemental Analysis |
C, 76.89; H, 7.74; N, 7.17; O, 8.19
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| CAS # |
168835-82-3
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| Related CAS # |
168835-82-3
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| PubChem CID |
5941539
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| Appearance |
White to off-white solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
590.6±50.0 °C at 760 mmHg
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| Flash Point |
311.0±30.1 °C
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| Vapour Pressure |
0.0±1.7 mmHg at 25°C
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| Index of Refraction |
1.584
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| LogP |
5.87
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
29
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| Complexity |
577
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O([H])C1C(=C([H])C(/C(/[H])=C(\C#N)/C(N([H])C([H])([H])C([H])([H])C([H])([H])C2C([H])=C([H])C([H])=C([H])C=2[H])=O)=C([H])C=1C([H])(C([H])([H])[H])C([H])([H])[H])C([H])(C([H])([H])[H])C([H])([H])[H]
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| InChi Key |
JANPYFTYAGTSIN-FYJGNVAPSA-N
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| InChi Code |
InChI=1S/C25H30N2O2/c1-17(2)22-14-20(15-23(18(3)4)24(22)28)13-21(16-26)25(29)27-12-8-11-19-9-6-5-7-10-19/h5-7,9-10,13-15,17-18,28H,8,11-12H2,1-4H3,(H,27,29)/b21-13+
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| Chemical Name |
(E)-2-cyano-3-[4-hydroxy-3,5-di(propan-2-yl)phenyl]-N-(3-phenylpropyl)prop-2-enamide
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| Synonyms |
Tyrphostin SU 1498; AG-1498; AG 1498; AG1498; SU-1498; SU 1498; SU1498
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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: 78~100 mg/mL (199.7~256.1 mM)
Ethanol: ~78 mg/mL (~199.7 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.40 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (6.40 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5606 mL | 12.8031 mL | 25.6062 mL | |
| 5 mM | 0.5121 mL | 2.5606 mL | 5.1212 mL | |
| 10 mM | 0.2561 mL | 1.2803 mL | 2.5606 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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