CC-115

製品コードS7891 バッチS789102

化学情報

	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	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.

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. 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].

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

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：

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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