CC-115 hydrochloride is a potent dual DNA-PK and mTOR kinase inhibitor that blocks both mTORC1 and mTORC2 signaling. It inhibits PC-3 cell proliferation and demonstrates selectivity against other protein kinases and PIKKs, including good selectivity against PI3K-alpha, ATR, and ATM. It shows good in vivo PK profiles across multiple species.
- Potent and dual DNA-PK and mTOR kinase inhibitor (IC50s of 13 nM and 21 nM respectively)
- Blocks both mTORC1 and mTORC2 signaling
- Inhibits PC-3 cells proliferation with an IC50 of 138 nM
- Demonstrates selectivity against other protein kinases and PIKKs
- Shows good in vivo PK profiles across multiple species (53% in mouse, 76% in rat, and ~100% in dog oral bioavailability)
- Leads to significant tumor volume reductions and sustains inhibition in vivo