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CAY10404

CAS No. : 340267-36-9

MCE 站：CAY10404

产品活性：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。

研究领域：Immunology/Inflammation  |  PI3K/Akt/mTOR  |  Apoptosis

作用靶点：COX  |  Akt  |  Apoptosis

In Vitro: CAY10404 (compound 7) exhibits no inhibition of COX-1 (IC₅₀>500 ?M).
CAY10404 (10-100 ?M; 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 ?M.
CAY10404 (20-100 ?M; for 3 days) induces apoptosis in NSCLC cells.
CAY10404 (80 ?M; for 3 days) induces a concentration-dependent decrease in the level of the anti-apoptotic proteins (Bcl-2 and Bcl-X_L) and pAkt and pGSK-3β.
CAY10404 (20, 50, 80, 100 ?M; for 14 days) compromises the ability of H460 cells to form colonies in anchorage-independent growth in a concentration-dependent manner.

In Vivo: CAY10404 (50 mg/kg/day; ip; for 4 days) decreases lung inflammation in HTV mice and attenuates ventilator-induced lung injury.

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