SU5416 (Semaxinib) is a reversible, ATP-competitive, oxindole-based inhibitor of Flk-1/KDR receptor tyrosine kinase. SU5416 inhibits VEGF-dependent phosphorylation of the Flk-1 receptor in Flk-1-overexpressing NIH 3T3 cells with a IC50 of 1.04 uM. In an ELISA-based assay, SU5416 inhibits autophosphorylation of the Flk-1 receptor at an IC50 of 1.23 uM. [1]
In a mitogenic/proliferation assay in HUVECs, the IC50 of SU5416 is extremely time-dependent, ranging from 1 uM to 40 nM at 48h incubation. These data in conjunction with dose-ranging studies support regimens of less than once-daily dosing of SU5416. [2]
More recent studies have shown that SU5416 is also an agonist of the aryl hydrocarbon receptor (AHR), leading to the generation of regulatory T-cells in vitro. SU5416 also upregulates CYP1A1 and CYP1B1. [3]
Technical information:
| Chemical Formula: | C15H14N2O | |
| CAS #: | 204005-46-9 | |
| Molecular Weight: | 238.28 | |
| Purity: > 98% | ||
| Appearance: | White | |
| Chemical Name: | 2H-Indol-2-one, 3-[(3,5-dimethyl-1H-pyrrol-2-yl)methylene]-1,3-dihydro-, (3Z) | |
| Solubility: | Up to 20 mM in DMSO | |
| Synonyms: | SU5416, SU 5416, su-5416, Semaxinib |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Fong et al., SU5416 Is a Potent and Selective Inhibitor of the Vascular Endothelial Growth Factor Receptor (Flk-1/KDR) That Inhibits Tyrosine Kinase Catalysis, Tumor Vascularization, and Growth of Multiple Tumor Types. Cancer Res. 1999, 59, 99-106. Pubmed ID: 9892193 |
| 2. | Mendel et al., The Angiogenesis Inhibitor SU5416 Has Long-lasting Effects on Vascular Endothelial Growth Factor Receptor Phosphorylation and Function. Clin. Cancer Res. 2000, 6, 4848-4858. Pubmed ID: 11156244 |
| 3. | Mezrich et al., SU5416, a VEGF Receptor Inhibitor and Ligand of the AHR, Represents a New Alternative for Immunomodulation. PLOS One, 2012, 7(9), e44547. |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.
