AZD0156

製品コードS8375 バッチS837502

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	DMSO	2 mg/mL warmed with 50ºC water bath (4.33 mM)
		Ethanol	2 mg/mL (4.33 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 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. AZD0156 shows robust efficacy in mouse xenograft models after oral administration when combined with DSB inducing agents. AZD0156 is currently undergoing early clinical assessment^[1].

プロトコル(参考用のみ)

参考

[1] Kurt G. Pike. Cancer Res. 2016, 76(14 Suppl):Abstract nr 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：

Homology-independent targeted insertion (HITI) enables guided CAR knock-in and efficient clinical scale CAR-T cell manufacturing [ Mol Cancer, 2023, 22(1):100]	PubMed: 37365642
C16orf72/HAPSTR1/TAPR1 functions with BRCA1/Senataxin to modulate replication-associated R-loops and confer resistance to PARP disruption [ Nat Commun, 2023, 14(1):5003]	PubMed: 37591890
Galectin-9 blockade synergizes with ATM inhibition to induce potent anti-tumor immunity [ Int J Biol Sci, 2023, 19(3):981-993]	PubMed: 36778120
Galectin-9 blockade synergizes with ATM inhibition to induce potent anti-tumor immunity [ Int J Biol Sci, 2023, 19(3):981-993]	PubMed: 36778120
Effector memory T cells induce innate inflammation by triggering DNA damage and a non-canonical STING pathway in dendritic cells [ Cell Rep, 2023, S2211-1247(23)01192-0]	PubMed: 37794597
Antioxidants and azd0156 Rescue Inflammatory Response in Autophagy-Impaired Macrophages [ Int J Mol Sci, 2023, 25(1)169]	PubMed: 38203340
Identification of therapeutic sensitivities in a spheroid drug combination screen of Neurofibromatosis Type I associated High Grade Gliomas [ PLoS One, 2023, 18(2):e0277319]	PubMed: 36730269
Mitotic DNA damage promotes chromokinesin-mediated missegregation of polar chromosomes in cancer cells [ Mol Biol Cell, 2023, 34(5):ar47]	PubMed: 36989031
Ku-DNA binding inhibitors modulate the DNA damage response in response to DNA double-strand breaks [ NAR Cancer, 2023, 5(1):zcad003]	PubMed: 36755959
Small-molecule targeted therapies induce dependence on DNA double-strand break repair in residual tumor cells [ Sci Transl Med, 2022, 14(638):eabc7480]	PubMed: 35353542

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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