LY-3177833 is a orally available, potent and selective inhibitor of CDC7 (Cell Division Cycle 7-related Protein Kinase), inhibiting CDC7/DBF4 I and pMCM2 (S53) with IC50 values of 3.3 nM and 290 nM, respectively. The inhibition profoundly impacts chromosome dynamics. Broad antitumor activity was associated with robust dose/exposure-dependent in vivo target inhibition in mouse xenograft models. In addition, the preclinical profile of the compound was different from nonselective CDC7 inhibitors and cytotoxic agents, which supports its clinical development with a continuous dosing regimen.

KEYWORDS: LY-3177833 | Supplier | CDC7 inhibitor | LY3177833 | LY 3177833 | CT-LY3177 | CAS [1627696-51-8] | DNA-RNA | CDC7 | Inhibitor | Enzymes