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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C16H16N8O |
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分子量 | 336.35 | CAS No. | 1228013-15-7 | |
Solubility (25°C)* | 体外 | DMSO | 34 mg/mL (101.08 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <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. |
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. |
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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]. |
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]. |
細胞アッセイ | 細胞株 | CLL cells |
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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. |
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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 |
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 |
Kinase Inhibitors of DNA-PK, ATM and ATR in Combination with Ionizing Radiation Can Increase Tumor Cell Death in HNSCC Cells While Sparing Normal Tissue Cells [ Genes (Basel), 2021, 12(6)925] | PubMed: 34204447 |
Senescence Induction by Combined Ionizing Radiation and DNA Damage Response Inhibitors in Head and Neck Squamous Cell Carcinoma Cells [ Cells, 2020, 9(9)E2012] | PubMed: 32883016 |
Maintenance Therapy for ATM-Deficient Pancreatic Cancer by Multiple DNA Damage Response Interferences after Platinum-Based Chemotherapy [ Cells, 2020, 9(9)E2110] | PubMed: 32948057 |
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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