CC-115

製品コードS7891 バッチS789104

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C16H16N8O
分子量 336.35 CAS No. 1228013-15-7
Solubility (25°C)* 体外 DMSO 67 mg/mL (199.19 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 CC-115 is a dual inhibitor of DNA-dependent protein kinase (DNA-PK) and mammalian target of rapamycin (mTOR), with potential antineoplastic activity.
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. This compound reverts CD40-induced chemoresistance. Its 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, this chemical induces cell death with an IC50 of 0.93 µM. It and NU7441 completely block the proliferation of CD4+ and CD8+ T cells. Taken together, this compound 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].
in vivo CC-115 decreases lymphadenopathy in CLL patients[1]. This compound shows good in vivo PK profiles across multiple species with 53%, 76%, and ∼100% oral bioavailability in mouse, rat, and dog, respectively. It 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].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 CLL cells
濃度 0.35, 1, 3.5 μM
反応時間 30 min
実験の流れ

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.

参考

  • https://pubmed.ncbi.nlm.nih.gov/27235137/
  • https://pubmed.ncbi.nlm.nih.gov/26102506/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Targeting synthetic lethality between non-homologous end joining and radiation in very-high-risk medulloblastoma [ Cell Rep Med, 2025, 6(7):102202] PubMed: 40562042
Functional screening in human HSPCs identifies optimized protein-based enhancers of Homology Directed Repair [ Nat Commun, 2024, 15(1):2625] PubMed: 38521763
Different Impacts of DNA-PK and mTOR Kinase Inhibitors in Combination with Ionizing Radiation on HNSCC and Normal Tissue Cells [ Cells, 2024, 13(4)304] PubMed: 38391917
MDM2 antagonists promote CRISPR/Cas9-mediated precise genome editing in sheep primary cells [ Mol Ther Nucleic Acids, 2023, 31:309-323] PubMed: 36726409
DNA-PKcs as an upstream mediator of OCT4-induced MYC activation in small cell lung cancer [ Biochim Biophys Acta Gene Regul Mech, 2023, 1866(2):194939] PubMed: 37116859
CC-115 Mediates GSDME-Dependent Pyroptosis in Lung Adenocarcinoma Through the Akt/Bax Pathway [ J Cancer, 2023, 14(8):1350-1361] PubMed: 37283803
Inhibition of mTORC1/2 and DNA-PK via CC-115 Synergizes with Carboplatin and Paclitaxel in Lung Squamous Cell Carcinoma [ Mol Cancer Ther, 2022, molcanther.0053.2022] PubMed: 35732569
Novel Treatments of Uveal Melanoma Identified with a Synthetic Lethal CRISPR/Cas9 Screen [ Cancers (Basel), 2022, 14(13)3186] PubMed: 35804957
Influence of alectinib and crizotinib on ionizing radiation - in vitro analysis of ALK/ROS1-wildtype lung tissue cells [ Neoplasia, 2022, 27:100780] PubMed: 35278911
Viability fingerprint of glioblastoma cell lines: roles of mitotic, proliferative, and epigenetic targets [ Sci Rep, 2021, 11(1):20338] PubMed: 34645858

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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