同义名 :	-
	CAS号 :	340267-36-9
	货号 :	A358706
	分子式 :	C17H12F3NO3S
	纯度 :	99%+
	分子量 :	367.34
	MDL号 :	MFCD05863975
	存储条件：	Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

生物活性

描述

COX-2, a key enzyme that catalyzed the rate-limiting steps in the conversion of arachidonic acid to prostaglandins, played a pivotal role in the inflammatory process[4]. CAY10404 is a potent and selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 1 nM and a selectivity index (SI; COX-1 IC50/COX-2 IC50) of >500000.[1]. CAY10404 (10-100 µM; for 3 days) inhibits the growth of NSCLC cell lines in a concentration-dependent manner and has an average 50% inhibitory concentration (IC50) of 60-100 µM. CAY10404 (20-100 µM; for 3 days) induces apoptosis in NSCLC cells. CAY10404 (80 µM; for 3 days) induces a concentration-dependent decrease in the level of the anti-apoptotic proteins (Bcl-2 and Bcl-XL) and pAkt and pGSK-3β. CAY10404 (20, 50, 80, 100 µM; for 14 days) compromises the ability of H460 cells to form colonies in anchorage-independent growth in a concentration-dependent manner[3]. CAY10404 (10 mg/kg) had no significant antinociceptive activities to thermal nociception in naïve mice, however, coadministration of minocycline, with CAY10404 produced significant antinociceptive effects[5]. When radioresistant SH-EP cells were treated with CAY10404, a 49% decrease in cell viability was observed; pretreatment with CAY10404 followed by ortho-voltage irradiation further enhanced cell death (58%) suggesting radiosensitization is triggered by CAY10404[6].

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	2.72mL 0.54mL 0.27mL	13.61mL 2.72mL 1.36mL	27.22mL 5.44mL 2.72mL

参考文献

[1]A G Habeeb, et al. Design and synthesis of 4,5-diphenyl-4-isoxazolines: novel inhibitors of cyclooxygenase-2 with analgesic and antiinflammatory activity. J Med Chem. 2001. 44(18), 2921-7. [2]Joshua A Robertson, et al. The role of cyclooxygenase-2 in mechanical ventilation-induced lung injury. Am J Respir Cell Mol Biol. 2012 Sep;47(3):387-94. [3]Yongseon Cho, et al. Effects of CAY10404 on the PKB/Akt and MAPK pathway and apoptosis in non-small cell lung cancer cells. Respirology. 2009. 14(6), 850-8. [4]Jiahua Cui,Jinping Jia. Natural COX-2 Inhibitors as Promising Anti-inflammatory Agents: An Update. Curr Med Chem. 2021. 28(18), 3622-3646. [5]Ala'a Ahmed Abu-Ghefreh, Willias Masocha. Enhancement of antinociception by coadministration of minocycline and a non-steroidal anti-inflammatory drug indomethacin in naïve mice and murine models of LPS-induced thermal hyperalgesia and monoarthritis. BMC Musculoskelet Disord. 2010. 11:276. [6]Bhupesh Parashar,et al. Inhibition of human neuroblastoma cell growth by CAY10404, a highly selective Cox-2 inhibitor. J Neurooncol. 2005. 71(2), 141-8.