CC-115 是一种双重 mTOR/DNA-PK 的抑制剂,IC50分别为 21 nM 和 13 nM,可阻断mTORC1和mTORC2信号通路。
产品描述
CC-115 is a inhibitor of mTOR/DNA-PK (IC50= 21/ 13 nM).
体外活性
The IC50 values for CC-115 are >10 μM against a panel of CYP enzymes and >33 μM for the hERG ion channel. When screened in a single point assay at 10 μM against a Cerep receptor and enzyme panel only one target was inhibited >50% (PDE3, IC50 = 0.63 μM).
体内活性
CC-115 shows good PK profiles across multiple species with 53%, 76%, and 100% oral bioavailability in mouse, rat, and dog, respectively. CC-115, with favorable physicochemical and pharmacokinetic properties, demonstrates mTOR pathway inhibition and tumor growth inhibition, as well as a good safety profile, suitable for Clinicalal development.
细胞实验
Freshly isolated CLL cells are treated with different concentrations of CC-115 for 30 minutes. Subsequently, the cells are exposed to 5-Gy γ-radiation or treated with 10 µg/mL bleomycin (EMD Millipore, Billerica, MA) and incubated for 30 minutes, and cell lysates are made. (Only for Reference)
Cas No.
1228013-15-7
分子式
C16H16N8O
分子量
336.359
别名
CC 115
储存和溶解度
DMSO:62 mg/mL (184.3 mM)
H2O:<1 mgml
Ethanol:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years