Molecular Formula | C16H16N8O
|
Molar Mass | 336.35 |
Density | 1.56±0.1 g/cm3(Predicted) |
Boling Point | 587.3±60.0 °C(Predicted) |
Solubility | DMSO: ≥ 32 mg/mL |
pKa | 5.94±0.20(Predicted) |
Storage Condition | -20℃ |
In vitro study | CC-115 inhibits the DNA damage repair pathway and TORK in CLL cells and causes caspase-induced cell death in dormant CLL cells. It induced cell death with an IC50 of 0.51 μm. CC-115 was able to restore cd40-induced chemoresistance, reducing the expression of Mcl-1, Bfl-1 and Bcl-XL induced by cd40-stimulation in CLL cells. It also inhibits the proliferation of CLL cells. In healthy B cells, CC-115 induced cell death with an IC50 of 0.93 μm. CC-115 and NU7441 can completely block the proliferation of CD4 and CD8 T cells. Overall, CC-115 can induce direct toxicity, inhibiting signaling pathways important for CLL survival, chemoresistance, and proliferation. |
In vivo study | In patients with chronic lymphocytic leukemia (CLL patients), CC-115 reduce their lymphadenopathy. In a variety of species, CC-115 has a good in vivo pharmacokinetic distribution, the oral bioavailability in mice, rats, dogs were 53%, 76%, ~ 100%. CC-115 has favorable physicochemical and pharmacokinetic properties, inhibits the mTOR signaling pathway and inhibits tumor growth in vivo. In vitro and in vivo experiments have drug safety, suitable for clinical drug development. |