Tyrphostin AG1433

Tyrphostin AG1433 (SU1433) is a tyrosine kinases inhibitor. AG1433 is also a selective PDGFRβ and VEGFR-2 (Flk-1/KDR) inhibitor with IC50s of 5.0 μM and 9.3 μM, respectively. Tyrphostin AG1433 prevents blood vessel formation[1][2][3][4].

Research Areas >> Cancer

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> PDGFR

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> VEGFR

Flk-1:9.3 μM (IC50)

PDGFRβ:5 μM (IC50)

Tyrphostin AG1433 (0.1-100 μM; 72 hours; GB8B cells) treatment induces moderate cytotoxicity in glioblastoma cells[1]. Cell Viability Assay[1] Cell Line: GB8B cells Concentration: 0.1 μM, 1 μM, 5 μM, 10 μM, 20 μM, 30 μM, 50 μM, 60 μM, 100 μM Incubation Time: 72 hours Result: Induced significant cell death in GB8B cells in a concentration-dependent manner.

Chorion allantoic membrane (CAM) assays are used to determine the effects of the Flk-i inhibitors on angiogenesis. Tyrphostin AG1433 (SU1433) is prepared in methylcellulose pellets and applies to the CAMs of 4-6-day-old chicken embryos. Tyrphostin AG1433 prevents the formation of new yessels under the pellets[2].

[1]. Serban F, et al. Silencing of epidermal growth factor, latrophilin and seven transmembrane domain-containing protein 1 (ELTD1) via siRNA-induced cell death in glioblastoma. J Immunoassay Immunochem. 2017;38(1):21-33.

[2]. Strawn LM, et al. Flk-1 as a target for tumor growth inhibition. Cancer Res. 1996 Aug 1;56(15):3540-5.

[3]. Kim TS, et al. The ZFHX3 (ATBF1) transcription factor induces PDGFRB, which activates ATM in the cytoplasm to protect cerebellar neurons from oxidative stress. Dis Model Mech. 2010 Nov-Dec;3(11-12):752-62.

[4]. Kroll J, et al. The vascular endothelial growth factor receptor KDR activates multiple signal transduction pathways in porcine aortic endothelial cells. J Biol Chem. 1997 Dec 19;272(51):32521-7.