Tyrphostin AG1433 Chemical Properties

Melting point:

280-282 °C

Boiling point:

490.9±45.0 °C(Predicted)

Density 

1.300±0.06 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMSO: 62.5 mg/mL (234.71 mM)

pka

8.32±0.20(Predicted)

form 

Solid

color 

Light yellow to khaki

Tyrphostin AG1433 Usage And Synthesis

Uses

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].

Biological Activity

Tyrphostin AG1433 (SU1433) is a tyrosine kinase inhibitor. It is also a selective PDGFRβ and VEGFR-2 (Flk-1/KDR) inhibitor with IC50 of 5.0 μM and 9.3 μM, respectively. It prevents blood vessel formation.

in vivo

target

IC 50

Flk-1: 9.3 μM (IC₅₀); PDGFRβ: 5 μM (IC₅₀)

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. DOI:10.1080/15321819.2016.1209217
[2] Strawn LM, et al. Flk-1 as a target for tumor growth inhibition. Cancer Res. 1996 Aug 1;56(15):3540-5. PMID:8758924
[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. DOI:10.1242/dmm.004689
[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. DOI:10.1074/jbc.272.51.32521

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