AZD0156

製品コードS8375 バッチS837501

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	C₂₆H₃₁N₅O₃
	分子量	461.56	CAS No.	1821428-35-6
Solubility (25°C)*	体外	Ethanol	2 mg/mL (4.33 mM)
		DMSO	0.3 mg/mL (0.64 mM)
		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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	AZD0156は、強力で選択的なATMキナーゼ阻害剤であり、化学療法/放射線療法増感作用および抗腫瘍作用の可能性があります。AZD0156は、DNA損傷チェックポイントの活性化を防ぎ、DNA損傷修復を阻害し、腫瘍細胞のアポトーシスを誘導し、ATMを過剰発現する腫瘍細胞の細胞死を誘導します。
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.
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.

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：

Small-molecule targeted therapies induce dependence on DNA double-strand break repair in residual tumor cells [ Science Translational Medicine, March 30, 2022, eabc7480]	PubMed: 35353542
Targeting the DNA Damage Response to Increase Anthracycline-Based Chemotherapy Cytotoxicity in T-Cell Lymphoma [ International Journal of Molecular Sciences, March 30, 2022, 3834]	PubMed: 35409194
USP37 counteracts HLTF to protect damaged replication forks and promote survival of BRCA1-deficient cells and PARP inhibitor resistance [ Nucleic Acids Research, June 20, 2025, gkaf544]	PubMed: 40548939
Incorporation of 53BP1 into phase-separated bodies in cancer cells during aberrant mitosis [ Journal of Cell Science, January 1, 2023, jcs260027]	PubMed: 36606487
Ku–DNA binding inhibitors modulate the DNA damage response in response to DNA double-strand breaks [ NAR Cancer, February 6, 2023, zcad003]	PubMed: 36755959
RPA-independent activation of the ATR/CHK1 pathway [ Proceedings of the National Academy of Sciences, February 10, 2026, e2524246123]	PubMed: 41628322
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

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。