AZD0156

目录号：S8375 批次号：S837502

化学数据

	别名	N/A	储存条件 (自收到货起)	3年 / -20°C / 粉状 1年 / -80°C / 溶于溶剂
	化学式	C₂₆H₃₁N₅O₃
	分子量	461.56	CAS号	1821428-35-6
Solubility (25°C)*	体外	DMSO	2 mg/mL (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.

制备储备液

生物活性

产品描述

AZD0156 是有效的、选择性的ATM激酶抑制剂，具有潜在的化疗/辐射增敏和抗肿瘤活性。AZD0156 可防止DNA损伤检查点激活，破坏DNA损伤修复，诱导肿瘤细胞凋亡，并导致过表达ATM的肿瘤细胞死亡。

靶点

ATM ^[1]

体外研究

AZD0156在细胞实验中对ATM具有亚纳摩尔级别的抑制作用，对ATM的选择性比对PIKK家族的其他酶高1000倍以上^[1]。

体内研究

AZD0156是一种具有细胞透性、高度可溶的化合物，具有良好的临床前药代动力学特性（如口服生物利用度）。在小鼠异种移植瘤模型中，AZD0156与DSB诱导剂通过口服途径给药具有强大的功效。AZD0156目前正处于早期临床检测^[1]。

参考文献

[1] Kurt G. Pike. Cancer Res. 2016, 76(14 Suppl):Abstract nr 4859.

AZD0156在文献中得到引用

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
Synergistic Activity of DNA Damage Response Inhibitors in Combination with Radium-223 in Prostate Cancer [ Cancers (Basel), 2024, 16(8)1510]	PubMed: 38672592
Inhibition of ATM or ATR in combination with hypo-fractionated radiotherapy leads to a different immunophenotype on transcript and protein level in HNSCC [ Front Oncol, 2024, 14:1460150]	PubMed: 39411143
Afatinib or Bevacizumab in combination with Osimertinib efficiently control tumor development in orthotopic murine models of non-small lung cancer [ PLoS One, 2024, 19(6):e0304914]	PubMed: 38935790
Methylation of NRIP3 Is a Synthetic Lethal Marker for Combined PI3K and ATR/ATM Inhibitors in Colorectal Cancer [ Clin Transl Gastroen, 2024, 15(3):e00682]	PubMed: 38235705
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

特定的存储和包装每个产品的信息在产品说明书上都有注明。大多数Selleck产品，在推荐的条件下存储可稳定保存两年。产品有时建议的储存温度不同，大多数建议储存在-20°C，抑制剂属于化学试剂，可在常温下运输储存两周左右。即使如此，我们保证产品的出货量将保持产品质量的条件下，一般都会放入冰袋。望阁下收到产品后，请按照产品数据表建议适当存储。

如果需要长期保存，请于零下二十度低温保存。禁止用于人体及治疗！

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