Home DNA Damage/DNA Repair DNA-PK inhibitor - mTOR inhibitor CC-115 For research use only.

CC-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.

CC-115 Chemical Structure

CC-115 Chemical Structure

CAS No. 1228013-15-7

Purity & Quality Control

CC-115 Related Products

Signaling Pathway

DNA-PK Signaling Pathways

DNA-PK Signaling Pathway

Biological Activity

Description 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.
Targets
DNA-PK [2]
(Cell-free assay)		 mTOR [2]
(Cell-free assay)		 PI3Kα [2]
(Cell-free assay)
0.013 μM 0.021 μM 0.852 μM
In vitro
In vitro CC-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[1].
Cell Research Cell lines CLL cells
Concentrations 0.35, 1, 3.5 μM
Incubation Time 30 min
Method

Freshly isolated CLL cells are treated with different concentrations of CC-115 for 30 minutes. Subsequently, the cells are exposed to 5-Gy γ-radiation or treated with 10 µg/mL bleomycin (EMD Millipore, Billerica, MA) and incubated for 30 minutes, and cell lysates are made.
Experimental Result Images Methods Biomarkers Images PMID
Growth inhibition assay GI50 29088817
Western blot p-DNA-PK / DNA-PK / p-ATM / ATM / p-NBS1 / p-AKT / AKT / p-4EBP1 / 4EBP1 29088817
In Vivo
In vivo CC-115 decreases lymphadenopathy in CLL patients[1]. 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[2].
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01353625 Completed
Glioblastoma Multiforme|Squamous Cell Carcinoma of Head and Neck|Prostate Cancer|Ewing''s Osteosarcoma|Chronic Lymphocytic Leukemia|Neoplasm Metastasis
Celgene
 April 25 2011 Phase 1

Chemical Information & Solubility

Molecular Weight 336.35 Formula

C16H16N8O
CAS No. 1228013-15-7 SDF Download CC-115 SDF
Smiles CCN1C(=O)CNC2=NC=C(N=C21)C3=C(N=C(C=C3)C4=NC=NN4)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 34 mg/mL ( (101.08 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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