受注:045-509-1970 |
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder | |
化学式 | C18H20N8O2 |
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分子量 | 380.40 | CAS No. | 2230820-11-6 | |
Solubility (25°C)* | 体外 | DMSO | 9 mg/mL (23.65 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 | AZD7648 is a potent inhibitor of DNA-PK with an IC50 of 0.6 nM in biochemical assay and more than 100-fold selective against 396 other kinases. |
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in vitro | AZD7648 inhibits IR-induced DNA-PK S2056 auto phosphoryalation with an IC50 = 92 nM in A549 non-small cell lung cancer (NSCLC) cells. In A549 cells, AZD7648 (≥1 µM) in combination with 2Gy IR for 48 hours leads to a significant accumulation of cells arrested in the G2/M of the cell cycle, a 4-fold increase in micronuclei formation, and 3-fold induction of γH2AX, pATM S1981 and 53BP1 foci formation compared with IR alone[2]. |
in vivo | AZD7648 is a potent and highly selective DNA-PK inhibitor, with good crystalline solubility, permeability and metabolic stability, good bioavailability and predictable pharmacokinetics in preclinical species, and potent knockdown of pRPA and regressions in murine xenograft models when combining with AZD2281 or radiation[1]. |
細胞アッセイ | 細胞株 | HeLa cells |
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濃度 | 10 μM | |
反応時間 | 1 h | |
実験の流れ | Cells were treated with indicated concentration of drug for 1 h. |
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動物実験 | 動物モデル | SCID mice |
投薬量 | 4-100 mg/kg | |
投与方法 | p.o. |
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 |
Negative feedback regulation of MAPK signaling is an important driver of chronic lymphocytic leukemia progression [ Cell Rep, 2023, 42(10):113017] | PubMed: 37792532 |
Phosphatases maintain low catalytic activity of SGK1: DNA damage resets the balance in favor of phosphorylation [ J Biol Chem, 2023, S0021-9258(23)01969-5] | PubMed: 37343701 |
Synergistic cytotoxicity of fludarabine, clofarabine, busulfan, vorinostat and olaparib in AML cells [ Front Oncol, 2023, 13:1287444] | PubMed: 38074694 |
Inhibition of DNA-dependent protein kinase catalytic subunit boosts rAAV transduction of polarized human airway epithelium [ Mol Ther Methods Clin Dev, 2023, 31:101115] | PubMed: 37841417 |
Disparate pathways for extrachromosomal DNA biogenesis and genomic DNA repair [ bioRxiv, 2023, 2023.10.22.563489] | PubMed: 37961138 |
MEK inhibition overcomes chemoimmunotherapy resistance by inducing CXCL10 in cancer cells [ Cancer Cell, 2022, S1535-6108(21)00662-0] | PubMed: 35051357 |
TDP1-independent pathways in the process and repair of TOP1-induced DNA damage [ Nat Commun, 2022, 13(1):4240] | PubMed: 35869071 |
DNA-PKcs promotes fork reversal and chemoresistance [ Mol Cell, 2022, 82-20:3932-3942.e6] | PubMed: 36130596 |
Effective Radiosensitization of Bladder Cancer Cells by Pharmacological Inhibition of DNA-PK and ATR [ Biomedicines, 2022, 10(6)1277] | PubMed: 35740300 |
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。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。