molecules of the month


oral, slow-off, selective CDC7 kinase inhibitor

Ph. I candidate for solid tumors

from HTS and PK optimization

Journal of Medicinal Chemistry

Carna Biosciences, Kobe, JP

Chemical structure of molecule AS-0141 Carna Biosciences CDC7 kinase inhibitor
1 min read

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.

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