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は、DNA依存性プロテインキナーゼ(DNA-PK)とラパマイシン標的タンパク質(mTOR)の二重阻害剤であり、抗腫瘍活性を有する可能性があります。
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.
in vivo CC-115 decreases lymphadenopathy in CLL patients. 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.

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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