CAY10404|cas:340267-36-9|西域试剂

CAY10404,99.79%

产品编号：Bellancom-121537| CAS NO：340267-36-9| 分子式：C₁₇H₁₂F₃NO₃S| 分子量：367.34

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-121537	￥1000.00	杭州北京（现货）
Bellancom-121537	￥1800.00	杭州北京（现货）
Bellancom-121537	￥3800.00	杭州北京（现货）
Bellancom-121537	￥6500.00	杭州北京（现货）
Bellancom-121537	￥10500.00	杭州北京（现货）

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CAY10404

产品介绍

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 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. 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.

体外研究

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-X_L) 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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

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

Cell Line:	H460 cells
Concentration:	20, 50, 100 µM
Incubation Time:	For 3 days
Result:	Induced apoptosis.

Western Blot Analysis

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-X_L) and pAkt and pGSK-3β, without changing the level of the pro-apoptotic protein (Bax) and total Akt and GSK-3β protein levels.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Adult male C57Bl/6J mice weighing 24-30 g
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.

体内研究

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

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Adult male C57Bl/6J mice weighing 24-30 g
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.

体内研究

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

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Adult male C57Bl/6J mice weighing 24-30 g
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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (272.23 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
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。