Toggle Nav

CC-115

In stock
Catalog No.
B6114
mTOR/DNA-PK inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$110.00
In stock
5mg
$100.00
In stock
10mg
$180.00
In stock
25mg
$395.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

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 [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].

References:
[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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt336.35
Cas No.1228013-15-7
FormulaC16H16N8O
Solubility≥50mg/mL in DMSO
Chemical Name1-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
SDFDownload SDF
Canonical SMILESCCN1C(CN=C2C1=NC(C(C=CC(C3=NNC=N3)=N4)=C4C)=CN2)=O
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor 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.

Quality Control