AZD7648

製品コードS8843 バッチS884301

印刷

化学情報

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

C18H20N8O2
分子量 380.40 CAS No. 2230820-11-6
Solubility (25°C)* 体外 DMSO 6 mg/mL (15.77 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 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.
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].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 HeLa cells
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.
動物実験 動物モデル SCID mice
投薬量 4-100 mg/kg
投与方法 p.o.

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
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。

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