化合物 CC-115 hydrochloride T61505

Product Introduction
Bioactivity


英文名: CC-115 hydrochloride

描述: CC-115 hydrochloride is a potent dual inhibitor of DNA-PK and mTOR kinase, exhibiting IC50 values of 13 nM and 21 nM, respectively. It effectively blocks both mTORC1 and mTORC2 signaling pathways.

体外活性: CC-115 inhibits PC-3 cells proliferation with an IC 50 of 138 nM. In a kinase selectivity assessment against a panel of 250 protein kinases at 3 μM, only one kinase other than mTOR kinase is identified with more than 50% inhibition (cFMS 57%, IC 50 =2.0 μM). Of the PI3K related kinases (PIKKs) tested, CC-115 proves to be equipotent against DNA PK (IC 50 =15 nM) and demonstrates 40 to >1000 fold selectivity against the remaining PIKKs tested; PI3K-alpha (IC 50 =0.85 μM), ATR (50% inhibition at 30 μM) and ATM (IC 50 >30 μM). The IC 50 values for CC-115 are >10 μM against a panel of CYP enzymes and >33 μM for the hERG (human ether-a-go-go-related gene) ion channel. When screened in a single point assay at 10 μM against a Cerep receptor and enzyme panel only one target is inhibited >50% (PDE3, IC 50 =0.63 μM) [1].

体内活性: CC-115 hydrochloride shows good in vivo PK profiles across multiple species with 53%, 76% and ~100% oral bioavailability in mouse, rat and dog, respectively. CC-115 is tested at lower doses of 0.25, 0.5 and 1 mg/kg bid or 1 mg/kg qd, with observed corresponding tumor volume reductions of 46%, 57%, 66% and 57% respectively. CC-115 sustains inhibition though 24 hours. At the 1 mg/kg dose CC-115 shows significant inhibition at 1 and 3 hours, CC-115 demonstrating inhibition through 10 hours. CC-115 is evaluated using both once (qd) and twice (bid) daily dosing schedules [1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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