molecules of the month

The Carna Biosciences CDC7 kinase inhibitor, AS-0141, is a clinical candidate for cancer with a structure that contains a hydrazine, furenone, and ester, all rare functional groups for an oral molecule. The molecule has a long residence time on the kinase, and despite a short half-life in mouse, extended target engagement is observed >24 h post-dose. The unusual structure of the molecule was confirmed by single crystal X-ray diffraction. This is also an interesting example of a drug candidate being developed by a drug discovery product supplier – reagents for some of the assays used were supplied by Carna Biosciences’ assay products division.