572632-M

SU5614

A potent, cell-permeable, reversible, ATP-competitive, and selective inhibitor of VEGF (Flk-1; IC₅₀ = 1.2 µM) and PDGF (IC₅₀ = 2.9 µM) receptor tyrosine kinases.

• Synonym(s): SU5614, 5-Chloro-3-[(3,5-dimethylpyrrol-2-yl)methylene]-2-indolinone, VEGFR Tyrosine Kinase Inhibitor VII, VEGFR2 Kinase Inhibitor IX
• Empirical Formula (Hill Notation): C₁₅H₁₃ClN₂O
• CAS Number: 186611-56-3
• Molecular Weight: 272.73
• UNSPSC Code: 12352200

Properties

• Assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: orange-red
• solubility: DMSO: 10 mg/mL
• storage temp.: 2-8°C
• InChI: 1S/C15H13ClN2O/c1-8-5-9(2)17-14(8)7-12-11-6-10(16)3-4-13(11)18-15(12)19/h3-7,17H,1-2H3,(H,18,19)
• InChI key: XLBQNZICMYZIQT-UHFFFAOYSA-N

Description

General description

A potent, cell-permeable, reversible, ATP-competitive, and selective inhibitor of VEGF (Flk-1; IC₅₀ = 1.2 µM) and PDGF (IC50 = 2.9 µM) receptor tyrosine kinases. Does not have any effect on the EGF and IGF receptor tyrosine kinases. Also inhibits the VEGF-driven mitogenesis of human umbilical vein endothelial cells (HUVECs; IC₅₀ ≤680 nM). Inhibits Flt3 phosphorylation in Flt3/Itd-BaF3 cells.

A potent, cell-permeable, reversible, ATP-competitive, and selective inhibitor of VEGF (Flk-1; IC₅₀ = 1.2 µM) and PDGF (IC₅₀ = 2.9 µM) receptor tyrosine kinases. Does not have any effect on the EGF and IGF receptor tyrosine kinases. Also inhibits the VEGF-driven mitogenesis of human umbilical vein endothelial cells (HUVECs; IC₅₀ ≤ 680 nM). Inhibits Flt3 phosphorylation in Flt3/Itd-BaF3 cells.

Biochem/physiol Actions

Primary Target
VEGF Flk-1

Target IC₅₀: 1.2 µM, 2.9 µM against VEGF (Flk-1) and PDGF receptor tyrosine kinases, respectively; ≤680 nM against the VEGF-driven mitogenesis of human umbilical vein endothelial cells (HUVECs)

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 2 months at -20°C.

Other Notes

Cools, J., et al. 2004. Cancer Res.64, 6385.
Sun, L., et al. 1998. J. Med. Chem. 41, 2588.

Legal Information

Not available for sale in the United States.

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable