Biological Activity
10074-G5 is an inhibitor of c-Myc-Max dimerization with an IC50 of 146 μM.
In Vitro
10074-G5 inhibits the growth of Daudi Burkitt's lymphoma cells and disruptes c-Myc/Max dimerization. The IC50 values against Daudi and HL-60 cells are 15.6 and 13.5 μM, respectively[1]. 10074-G5 binds the Myc peptide Myc353-437 with a Kd value of 2.8 μM in the region Arg363-Ile381. 10074-G5 binds in a cavity that is created by a kink (Asp379-Ile381) in the N-terminus of an induced helical domain (Leu370–Arg378)[3].
In Vivo
The plasma half-life of 10074-G5 in mice treated with 20 mg/kg i.v. is 37 min, and peak plasma concentration was 58 μM, which is 10-fold higher than peak tumor concentration[1].
References & source
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.
