572888-M

SU1498

A potent, reversible, ATP-competitive and selective inhibitor of Flk-1 kinase (IC₅₀ = 700 nM), a vascular endothelial growth factor (VEGF) receptor kinase.

• Synonym(s): SU1498, (E)-3-(3,5-Diisopropyl-4-hydroxyphenyl)-2-[(3-phenyl-n-propyl)amino-carbonyl]acrylonitrile, VEGFR Tyrosine Kinase Inhibitor VIII, VEGFR2 Kinase Inhibitor X
• Empirical Formula (Hill Notation): C₂₅H₃₀N₂O₂
• Molecular Weight: 390.52
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• assay: ≥95% (HPLC)
• form: solid
• potency: 700 nM IC₅₀
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: pale yellow
• solubility: DMSO: 5 mg/mL
• storage temp.: −20°C

Description

General description

A potent, reversible, ATP-competitive and selective inhibitor of Flk-1 kinase (IC₅₀ = 700 nM), a vascular endothelial growth factor (VEGF) receptor kinase. Also reduces the expression of ets-1, a transcription factor stimulated by VEGF. Has only a weak inhibitory effect on PDGF-receptor (IC₅₀ >50 µM), EGF-receptor (IC₅₀ >100 µM), and HER2 (IC₅₀ >100 µM) kinases. Acts as an angiogenesis inhibitor as shown by its activity in the chorioallantoic membrane (CAM) assay and in an in vivo VEGF-induced permeability assay.

A potent, reversible, ATP-competitive and selective inhibitor of Flk-1 kinase (IC₅₀ = 700 nM), a vascular endothelial growth factor (VEGF) receptor kinase. Has only a weak inhibitory effect on PDGF receptor (IC₅₀ >50 µM), EGF-receptor (IC₅₀ >100 µM), and HER-2 (IC₅₀ >100 µM) kinases. Acts as an angiogenesis inhibitor as shown by its activity in the chorioallantoic membrane (CAM) assay and in an in vivo VEGF-induced permeability assay.

Biochem/physiol Actions

Primary Target
Flk-1 kinase

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Arbiser, J.L., et al. 2000. Am. J. Pathol. 156, 1469.
Strawn, L.M., et al. 1996. Cancer Res. 56, 3540.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 1
• flash_point_f: Not applicable
• flash_point_c: Not applicable