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CC-115
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CC-115
CAS No. : 1228013-15-7
MCE 站:CC-115
产品活性:CC-115 是一种有效的双重 DNA-PK 和 mTOR 抑制剂,IC50 分别为 13 nM 和 21 nM。CC-115 阻断 mTORC1 和 mTORC2 信号通路。
研究领域:Cell Cycle/DNA Damage | PI3K/Akt/mTOR
In Vitro: CC-115 inhibits PC-3 cells proliferation with an IC50 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%, IC50=2.0 μM). Of the PI3K related kinases (PIKKs) tested, CC-115 proves to be equipotent against DNA PK (IC50=15 nM) and demonstrates 40 to >1000 fold selectivity against the remaining PIKKs tested; PI3K-alpha (IC50=0.85 μM), ATR (50% inhibition at 30 μM) and ATM (IC50>30 μM). The IC50 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, IC50=0.63 μM).
In Vivo: CC-115 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.
相关产品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Cell Cycle/DNA Damage Compound Library | Kinase Inhibitor Library | PI3K/Akt/mTOR Compound Library | Stem Cell Signaling Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Autophagy Compound Library | Anti-Aging Compound Library | Drug Repurposing Compound Library | Antioxidants Compound Library | Differentiation Inducing Compound Library | Reprogramming Compound Library | Oxygen Sensing Compound Library | Anti-COVID-19 Compound Library | Glycolysis Compound Library | Cytoskeleton Compound Library | Glutamine Metabolism Compound Library | Anti-Breast Cancer Compound Library | Anti-Lung Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Blood Cancer Compound Library | Rapamycin | LY294002 | Everolimus | MHY1485 | 3BDO | Temsirolimus | Salidroside | Torkinib | PI-103 | D-α-Hydroxyglutaric acid disodium | L-Leucine | Dihydromyricetin | PKI-402 | LTURM34 | Polyphyllin I | Rheb inhibitor NR1 | GSK1059615 | GNE-317 | PP121 | WYE-354 | Cyclovirobuxine D | HDACs/mTOR Inhibitor 1 | XL388 | ETP-46464 | Palomid 529 | WAY-600 | Arnicolide D | (+)-Usnic acid | hSMG-1 inhibitor 11j | mTOR inhibitor-1
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