SU 4312

SU 4312 is a selective, cell-permeable inhibitor of VEGFR2 and PDGFR tyrosine kinases (IC₅₀s = 0.8 and 19.4 μM, respectively).¹ It demonstrates IC₅₀ values >100 μM at EGFR, HER2, and IGF-1R.¹ SU 4312 has been shown to inhibit VEGF-dependent angiogenesis in a zebrafish assay (IC₅₀ = 1.8 µM) without affecting normal cells.² SU 4312 has also been shown to prevent MPP⁺-induced neuronal apoptosis in vitro, as well as to decrease MPTP-induced loss of dopaminergic neurons, reduce expression of mRNA for tyrosine hydroxylase, and impair swimming behavior in zebrafish.³

WARNING This product is not for human or veterinary use.

1. Sun, L., Tran, N., Tang, F., et al. Synthesis and biological evaluations of 3-substituted indolin-2-ones: A novel class of tyrosine kinase inhibitors that exhibit selectivity toward particular receptor tyrosine kinases. J. Med. Chem. 41(14), 2588-2603 (1998).

2. Tran, T.C., Sneed, B., Haider, J., et al. Automated, quantitative screening assay for antiangiogenic compounds using transgenic zebrafish. Cancer Res. 67(23), 11386-11392 (2007).

3. Cui, W., Zhang, Z., Li, W., et al. The anti-cancer agent SU4312 unexpectedly protects against MPP+ -induced neurotoxicity via selective and direct inhibition of neuronal NOS. Br. J. Pharmacol. 168(5), 1201-1214 (2013).