Tyrphostin AG1433

  Cat. No.:  DC28402   Featured
Chemical Structure
168835-90-3
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Field of application
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.
Cas No.: 168835-90-3
Synonyms: AG1433;AG-1433;AG 1433
SMILES: OC1C(O)=CC(C2C=NC3C(=CC(=C(C=3)C)C)N=2)=CC=1
Formula: C16H14N2O2
M.Wt: 266.29
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: [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.
Description: 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].
Target: Flk-1:9.3 μM (IC50) PDGFRβ:5 μM (IC50)
In Vivo: 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].
In Vitro: 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.
References: [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.
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