CC-115

- Overview
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    Background
    
    IC50: 21/ 13 nM for mTOR/DNA-PKCC-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 [1]. 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 [2]. 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 [1].
    
    [1] 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.
    [2] 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.
- Properties
  - Alternative Name
    
    1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,5-dihydropyrazino[2,3-b]pyrazin-2(1H)-one
    
    CAS Number
    
    1228013-15-7
    
    Molecular Formula
    
    C16H16N8O
    
    Molecular Weight
    
    336.35
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥50 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

CC-115

Background

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