Uses
4-(2-Chlorophenoxy)-N-[3-[(methylamino)carbonyl]phenyl]-1-piperidinecarboxamide is a stearoyl-CoA desaturase 1 (SCD1) inhibitor.
Biological Activity
A 939572 is a potent stearoyl-CoA desaturase 1 (SCD1) inhibitor (IC50 = 0.4 nM). Selective for SCD1 over a range of kinases and hERG channels. Inhibits proliferation of squamous cell carcinoma FaDu cells in vitro. Also induces cell death of undifferentiated human embryonic stem cells (ESCs). Orally bioavailable.
in vivo
Athymic nude (nu/nu) mice bearing A498 ccRCC xenografts are treated with A939572 (30mg/kg, p.o.) and Tem individually or in combination over the course of four weeks, and tumor volume (mm3) is recorded. A939572 and Tem monotherapy generate similar growth responses with approximately 20-30% reductions in tumor volume (vs. placebo control) being observed upon study completion, with values reaching statistical significance only within the last week of treatment. The combination group yields over a 60% decrease in tumor volume (vs. placebo control) by study completion with significant reductions recorded after approximately 1 week of treatment[2].
![4-(2-Chlorophenoxy)-N-[3-[(methylamino)carbonyl]phenyl]-1-Piperidinecarboxamide Structure](https://www.chemicalbook.com/CAS2/GIF/1032229-33-6.gif)
