AZD0156

製品コードS8375 バッチS837503

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

C26H31N5O3
分子量 461.56 CAS No. 1821428-35-6
Solubility (25°C)* 体外 Ethanol 2 mg/mL (4.33 mM)
DMSO Insoluble
Water 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.

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生物活性

製品説明 AZD0156 is a potent and selective inhibitors of ATM kinase, with potential chemo-/radio-sensitizing and antineoplastic activities. AZD0156 prevents DNA damage checkpoint activation, disrupts DNA damage repair, induces tumor cell apoptosis, and leads to cell death of ATM-overexpressing tumor cells.
in vitro AZD0156 shows sub-nanomolar potency in cell based assays of ATM inhibition with selectivities of greater than 1000 fold over other members of the PIKK family of enzymes[1].
in vivo AZD0156 is a permeable, highly soluble compound with excellent preclinical pharmacokinetic properties including oral bioavailability. This compound shows robust efficacy in mouse xenograft models after oral administration when combined with DSB inducing agents. It is currently undergoing early clinical assessment[1].

プロトコル(参考用のみ)

参考

  • http://cancerres.aacrjournals.org/content/76/14_Supplement/4859

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：

KEAP1 and STK11/LKB1 alterations enhance vulnerability to ATR inhibition in KRAS mutant non-small cell lung cancer [ Cancer Cell, 2025, 43(8):1530-1548.e9] PubMed: 40645185
ATM-dependent DNA damage response constrains cell growth and drives clonal hematopoiesis in telomere biology disorders [ J Clin Invest, 2025, 135(8)e181659] PubMed: 40179146
USP37 counteracts HLTF to protect damaged replication forks and promote survival of BRCA1-deficient cells and PARP inhibitor resistance [ Nucleic Acids Res, 2025, 53(12)gkaf544] PubMed: 40548939
SETD1A-dependent EME1 transcription drives PARPi sensitivity in HR deficient tumour cells [ Br J Cancer, 2025, 132(8):690-702] PubMed: 39994444
Inhibiting the DNA damage repair of HNSCC cells in combination with normo-fractionated radiotherapy influences clonogenicity, senescence and expression of NK cell activation markers [ Sci Rep, 2025, 15(1):31827] PubMed: 40883442
Oncogenic p53 induces mitotic errors in lung cancer cells by recopying DNA replication forks conferring targetable proliferation advantage [ Res Sq, 2025, rs.3.rs-7303237] PubMed: 40831504
In vivo DNA replication dynamics unveil aging-dependent replication stress [ Cell, 2024, S0092-8674(24)00963-2] PubMed: 39293447
Tumour-intrinsic PDL1 signals regulate the Chk2 DNA damage response in cancer cells and mediate resistance to Chk1 inhibitors [ Mol Cancer, 2024, 23(1):242] PubMed: 39478560
Developmental signals control chromosome segregation fidelity during pluripotency and neurogenesis by modulating replicative stress [ Nat Commun, 2024, 15(1):7404] PubMed: 39191776
Targeting ATM enhances radiation sensitivity of colorectal cancer by potentiating radiation-induced cell death and antitumor immunity [ J Adv Res, 2024, S2090-1232(24)00601-5] PubMed: 39708961

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。