CC-115

Catalog No.S7891

For research use only.

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

CAS No. 1228013-15-7

Selleck's CC-115 has been cited by 7 Publications

Purity & Quality Control

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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

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].

Assay
Methods Test Index 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 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].

Protocol (from reference)

Cell Research:

[1]

  • 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.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 336.35
Formula

C16H16N8O

CAS No. 1228013-15-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCN1C(=O)CNC2=NC=C(N=C21)C3=C(N=C(C=C3)C4=NC=NN4)C

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01353625 Completed Drug: CC-115 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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

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.

Handling Instructions

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