| 产品描述： | DNA-PK 抑制剂;DNA-PK Inhibitors;;InformationCC-115 CC-115 is a dual inhibitor of DNA-dependent protein kinase (DNA-PK) and mammalian target of rapamycin (mTOR) with IC50 values of 0.013 μM and 0.021 μM, respectively. It has potential antineoplastic activity.TargetsDNA-PK (Cell-free assay); mTOR (Cell-free assay); PI3Kα (Cell-free assay) 0.013 μM; 0.021 μM; 0.852 μMIn vitroCC-115 inhibits the DNA damage repair pathway and TORK in CLL cells and induces caspase-dependent cell death in resting CLL cells. It induces cell death with an IC50 of 0.51 µM. CC-115 reverts CD40-induced chemoresistance. CC-115 treatment significantly reduces induction of expression Mcl-1, Bfl-1, and Bcl-XL on CD40 stimulation in CLL cells. It also blocks proliferation of CLL cells. In healthy B cells, CC-115 induces cell death with an IC50 of 0.93 µM. CC-115 and NU7441 completely block the proliferation of CD4+ and CD8+ T cells. Taken together, CC-115 induces direct cytotoxicity and can block signaling pathways that are important for CLL survival, chemo-resistance and proliferation in the in the LN microenvironment.In vivoCC-115 decreases lymphadenopathy in CLL patients. 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 has favorable physicochemical and pharmacokinetic properties, demonstrates in vivo mTOR pathway inhibition and tumor growth inhibition, as well as a good in vitro and in vivo safety profile, suitable for clinical development.Cell Research(from reference)Cell lines：CLL cells Concentrations：0.35, 1, 3.5 μM Incubation Time：30 min |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京