|CC-115 mTOR/DNA-PK inhibitor|
Sample solution is provided at 25 µL, 10mM.
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Quality Control & MSDS
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Purity = 97.34%
- COA (Certificate Of Analysis)
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
|Cas No.||1228013-15-7||SDF||Download SDF|
|Solubility||≥50mg/mL in DMSO||Storage||Store at -20°C|
|Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|
IC50: 21/ 13 nM for mTOR/DNA-PK
CC-115 is a inhibitor of mTOR/DNA-PK.
The mammalian target of rapamycin (mTOR) kinase is a key mediator of the phosphoinositide 3-kinase /protein kinase B (AKT pathway). The DNA-dependent protein kinase (DNA-PK) is a critical component of the DNA repair machinery governings the response to DNA damage, which serves to maintain genome integrity.
In vitro: Previous study found that the proliferation induced by CD40(+) interleukin-21 stimulation could be completely blocked by CC-115, and CD40-mediated resistance to fludarabine and venetoclax could also be reverted by CC-115. Moreover, BCR-mediated signaling was blocked by CC-115 and in CLL samples from patients with acquired resistance to idelalisib treatment .
In vivo: Preclinical studies showed that CC-115 had good in vivo PK profiles across multiple species with 53%, 76%, and around100% oral bioavailability in mouse, rat, and dog, respectively .
Clinical trial: Clinical efficacy of CC-115 was studied in 8 patients with relapsed/refractory CLL/small lymphocytic lymphoma harboring ATM deletions/mutations. Results showed that all but one patient had a decrease in lymphadenopathy, leading to 1 IWCLL partial response (PR) and 3 PRs with lymphocytosis. These early promising clinical activity suggested that CC-115 might be developed further for treatment of CLL .
 Thijssen R,et al. Dual TORK/DNA-PK inhibition blocks critical signaling pathways in chronic lymphocytic leukemia. Blood.2016 Jul 28;128(4):574-83.
 Mortensen DS, et al. Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. J Med Chem. 2015 Jul 23;58(14):5599-5608.