CAY10404 是一种有效且高度选择性的环氧合酶 2 (COX-2) 抑制剂，IC₅₀ 为 1 nM，选择性指数 (SI；COX-1 IC₅₀/COX-2 IC₅₀) 为 >500000。CAY10404 是有效的 PKB/Akt 和 MAPK 信号通路抑制剂，可诱导非小细胞肺癌 (NSCLC) 细胞凋亡 (apoptosis)。CAY10404 是一种二芳基异恶唑，具有良好的止痛，抗炎和抗癌活性。

CAY10404 is a potent and selective cyclooxygenase-2 (COX-2) inhibitor with an IC 50 of 1 nM and a selectivity index (SI; COX-1 IC 50 /COX-2 IC 50 ) of >500000. CAY10404 is a potent PKB/Akt and MAPK signaling pathways inhibitor and induces apoptosis in non-small cell lung cancer (NSCLC) cells. CAY10404, a diarylisoxazole, has good analgesic, anti-inflammatory, and anti-cancer activities.

Solid

COX-2 1 nM (IC50) COX-1 >500 μM (IC

CAY10404 (compound 7) exhibits no inhibition of COX-1 (IC50>500 μM).
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.
has not independently confirmed the accuracy of these methods. They are for reference only.

CAY10404 (50 mg/kg/day; ip; for 4 days) decreases lung inflammation in HTV mice and attenuates ventilator-induced lung injury.
has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

-20°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

[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 Aug 30;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.

In Vitro: DMSO : 100 mg/mL (272.23 mM; Need ultrasonic)配制储备液