Su1498

SKU: orb1223244

Description

SU 1498 is a selective inhibitor of the receptor tyrosine kinase VEGF receptor 2 (VEGFR2, aka FLK1; IC50 = 700 nM), having negligible activity at several other serine/threonine and tyrosine kinases.1, 2 It effectively blocks signaling through VEGFR2 both in vitro and in vivo.1, 3 SU 1498 is used to study the role of VEGFR2 signaling in diverse processes, including angiogenesis, tumor growth, neural progenitor cell survival, and neuroregeneration.

Key Properties

• CAS Number: 168835-82-3
• MW: 390.53
• Purity: >98% (HPLC)
• Formula: C₂₅H₃₀N₂O₂
• SMILES: O=C(/C(=C/c1cc(C(C)C)c(O)c(C(C)C)c1)/C#N)NCCCc1ccccc1
• Target: VEGFR2
• Solubility: DMSO : ≥ 150 mg/mL. 384.10 mM

Bioactivity

• In Vitro:
  SU1498 stimulates accumulation of phosphorylated ERKs in human umbilical vein endothelial cells and in human aortic endothelial cells in a manner that is dependent on the functioning of the upstream components of the MAPK pathway, B-Raf, and MEK kinases. The enhanced accumulation of phospho-ERKs is observed only in cells that have been stimulated with sphingosine 1-phosphate or protein growth factors; SU1498 by itself is ineffective. SU1498 blocks signal transduction from VEGFR2 in MS1 VEGF cells. In the presence of SU1498, levels of Ets-1 are decreased, suggesting that VEGF-VEGFR-2 interactions contributed to baseline levels of Ets-1 expression, and interruption of this autocrine interaction with SU1498 led to decreased expression of Ets-1. SU1498 treatment significantly impacts U87 cell proliferation and apoptosis. SU1498 induces a marked increase in lipids and a decrease in glycerophosphocholine. Accordingly, accumulation of lipid droplets is seen in the cytoplasm of SU1498-treated U87 cells.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SU-1498 | SU 1498 | SU1498 | Tyrphostin SU 1498

Quick Database Links

Gene Symbol

VEGFR2