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。
生物活性 | CAY10404 is a potent and selectivecyclooxygenase-2 (COX-2)inhibitor with anIC50of 1 nM and a selectivity index (SI;COX-1IC50/COX-2 IC50) of >500000. CAY10404 is a potentPKB/AktandMAPKsignaling pathways inhibitor and inducesapoptosisin non-small cell lungcancer(NSCLC) cells. CAY10404, a diarylisoxazole, has good analgesic, anti-inflammatory, and anti-cancer activities[1][2][3]. |
IC50& Target | COX-2 1 nM (IC50) | COX-1 >500 μM (IC50) |
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体外研究 (In Vitro) | CAY10404 (compound 7) exhibits no inhibition of COX-1 (IC50>500 μM)[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[3]. CAY10404 (20-100 μM; for 3 days) induces apoptosis in NSCLC cells[3]. 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[3]. 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].
Cell Viability Assay[3] Cell Line: | Non-small cell lung cancer (NSCLC) cells (H1703, H358, H460) | Concentration: | 10-100 μM | Incubation Time: | For 3 days | Result: | Inhibited the growth of NSCLC cell lines in a concentration-dependent manner. |
Apoptosis Analysis[3] Cell Line: | H460 cells | Concentration: | 20, 50, 100 μM | Incubation Time: | For 3 days | Result: | Induced apoptosis. |
Western Blot Analysis[3] Cell Line: | NSCLC cells (H358, H460) | Concentration: | 80 μM | Incubation Time: | For 3 days | Result: | Induced a concentration-dependent decrease in the level of the anti-apoptotic proteins (Bcl-2 and Bcl-XL) and pAkt and pGSK-3β, without changing the level of the pro-apoptotic protein (Bax) and total Akt and GSK-3β protein levels. |
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体内研究 (In Vivo) | CAY10404 (50 mg/kg/day; ip; for 4 days) decreases lung inflammation in HTV mice and attenuates ventilator-induced lung injury[2].
Animal Model: | Adult male C57Bl/6J mice weighing 24-30 g[2] | Dosage: | 50 mg/kg | Administration: | IP; daily; for 4 days | Result: | Attenuated cyclooxygenase activity, significantly decreasing BAL PGE2 and 6-keto PGF1α. Decreased lung inflammation in HTV mice (high tidal volume; 20 ml/kg; for 4 hours) and attenuates ventilator-induced lung injury. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | -20°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
溶解性数据 | In Vitro: DMSO : 100 mg/mL(272.23 mM;Need ultrasonic) 配制储备液 1 mM | 2.7223 mL | 13.6114 mL | 27.2227 mL | 5 mM | 0.5445 mL | 2.7223 mL | 5.4445 mL | 10 mM | 0.2722 mL | 1.3611 mL | 2.7223 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (stored under nitrogen)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: 2.5 mg/mL (6.81 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (6.81 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: 2.5 mg/mL (6.81 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (6.81 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (6.81 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.81 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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