生物活性 | |||
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描述 | AZD0156, a potent and selective ATM inhibitor, exhibits oral activity with an IC50 of 0.58 nM. It blocks ATM-dependent signaling pathways, inhibits DNA damage checkpoint activation, impairs DNA damage repair, and triggers apoptosis in tumor cells. Furthermore, AZD0156 suppresses ATM kinase activity, leading to the prevention of DNA damage checkpoint activation, disruption of DNA repair mechanisms, induction of apoptosis, and ultimately causing death in tumor cells with high ATM expression. Calcipotriol monohydrate, a synthetic analogue of Vitamin D3, binds strongly to the vitamin D receptor. In NHEK cells, without IL-17A or IL-22 stimulation, Calcipotriol marginally increases IL-8 mRNA levels at 0.2 nM or has no effect from 2 to 20 nM. However, IL-17A and IL-22 significantly boost IL-8 mRNA expression, aligning with previous findings. Calcipotriol at 2, 20, and 40 nM dose-dependently diminishes this upregulation[1]. Drug treatments alter NK cell expression of cytotoxicity receptors or KIR. Human NK cells pretreated with 1,25(OH)2D3, Calcipotriol, or FTY720 at 100, 10, or 1 ng/mL for 4 hours show a notable increase in NKp30 surface expression[2]. |
临床研究 | |||||
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NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT02518048 | Skin and Connective Tissue Dis... 展开 >>eases 收起 << | Phase 2 | Completed | - | France ... 展开 >> Centre de Pharmacologie Clinique Appliquée à la Dermatologie (CPCAD) Nice, France, 06000 收起 << |
NCT02416258 | Skin and Connective Tissue Dis... 展开 >>eases 收起 << | Phase 2 | Completed | - | France ... 展开 >> Centre de Pharmacologie Clinique Appliquée à la Dermatologie (CPCAD) Nice, France, 06000 收起 << |
NCT02518048 | - | Completed | - | - |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.32mL 0.46mL 0.23mL |
11.61mL 2.32mL 1.16mL |
23.22mL 4.64mL 2.32mL |
参考文献 |
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