TYRPHOSTIN AG 1024

Description

The binding of insulin-like growth factor 1 (IGF-1) to the IGF-1 receptor (IGF-1R) initiates a cascade of reactions that promote cell growth and transformation by activating the PI3K/Akt signaling pathway, inhibiting apoptotic pathways, and mediating mitogenic actions. Overexpression of IGF-1R confers tumorigenic potential to cells as well as protection from apoptosis. AG-1024 is a selective inhibitor of IGF-1R that inhibits insulin-stimulated cellular proliferation and IGF-1R autophosphorylation with IC₅₀ values of 0.4 and 7 μM, respectively. At 10 nM, AG-1024 can inhibit proliferation and induce apoptosis in human breast cancer MCF-7 cells, and it inhibits autocrine growth of human prostate cancer DU145 cells with an IC₅₀ value of 2.5 μM.

Uses

Tyrphostin AG 1024 is an insulin-like growth factor (IGF)-I receptor antagonist.

Definition

ChEBI: 2-[(3-bromo-5-tert-butyl-4-hydroxyphenyl)methylidene]propanedinitrile is an alkylbenzene.

in vivo

target

IGF-1R

References

[1] párrizas m1, gazit a, levitzki a, wertheimer e, leroith d. specific inhibition of insulin-like growth factor-1 and insulin receptor tyrosine kinase activity and biological function by tyrphostins. endocrinology. 1997 apr;138(4):1427-33.
[2] fan p1, agboke fa1, mcdaniel re1, sweeney ee1, zou x1, creswell k1, jordan vc2.inhibition of c-src blocks oestrogen-induced apoptosis and restores oestrogen-stimulated growth in long-term oestrogen-deprived breast cancer cells. eur j cancer. 2014 jan; 50(2):457-68.