Sulindac (Synonyms: 舒林酸; MK-231)

目录号: HY-B0008 纯度: 99.81%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Sulindac (MK-231) 是一种口服活性非甾体类抗炎药。Sulindac 也是一种免疫调节剂。Sulindac 可用于脊柱关节炎、痛风性关节炎及多种癌症如结直肠癌、肺癌的研究。

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Sulindac Chemical Structure

CAS No. : 38194-50-2

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥605	In-stock
100 mg	￥550	In-stock
500 mg	￥950	In-stock
1 g		询价
5 g		询价

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

生物活性
纯度 & 产品资料
参考文献

生物活性

Sulindac (MK-231) is an orally active nonsteroidal anti-inflammatory agent. Sulindac also is an immunomodulatory agent. Sulindac can be used for the research of arthritis of the spine, gouty arthritis and kinds of cancer including colorectal cancer (CRC) and lung cancer^[1]^[2].

IC₅₀ & Target^[1]

COX-2

Autophagy

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A549	IC₅₀	> 50 μM Compound: Sulindac	Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay	[PMID: 32987314]
A549	IC₅₀	> 50 μM Compound: Sulindac	Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay	[PMID: 32987314]
A549	IC₅₀	> 50 μM Compound: Sulindac	Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 32987314]
BXPC-3	IC₅₀	980 μM Compound: SUL	Cytotoxicity against human BxPC3 cells assessed as growth inhibition after 24 hrs by MTT assay Cytotoxicity against human BxPC3 cells assessed as growth inhibition after 24 hrs by MTT assay	[PMID: 24273639]
COLO 320	IC₅₀	> 200 μM Compound: a	Cytotoxicity against human COLO320 cells after 72 hrs by WST-1 assay Cytotoxicity against human COLO320 cells after 72 hrs by WST-1 assay	[PMID: 20801552]
HeLa	IC₅₀	> 50 μM Compound: Sulindac	Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 24 hrs by MTT assay Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 24 hrs by MTT assay	[PMID: 32987314]
HeLa	IC₅₀	> 50 μM Compound: Sulindac	Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 48 hrs by MTT assay Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 48 hrs by MTT assay	[PMID: 32987314]
HeLa	IC₅₀	> 50 μM Compound: Sulindac	Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 32987314]
HT-29	IC₅₀	1729 μM Compound: Sulindac	Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 22940705]
HT-29	IC₅₀	800 μM Compound: SUL	Cytotoxicity against human HT-29 cells assessed as growth inhibition after 24 hrs by MTT assay Cytotoxicity against human HT-29 cells assessed as growth inhibition after 24 hrs by MTT assay	[PMID: 24273639]
Jurkat	IC₅₀	699 μM Compound: SUL	Cytotoxicity against human Jurkat cells assessed as growth inhibition after 24 hrs by MTT assay Cytotoxicity against human Jurkat cells assessed as growth inhibition after 24 hrs by MTT assay	[PMID: 24273639]
MCF7	IC₅₀	> 50 μM Compound: Sulindac	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay	[PMID: 32987314]
MCF7	IC₅₀	> 50 μM Compound: Sulindac	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay	[PMID: 32987314]
MCF7	IC₅₀	> 50 μM Compound: Sulindac	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 32987314]
MCF7	IC₅₀	965 μM Compound: SUL	Cytotoxicity against human MCF7 cells assessed as growth inhibition after 24 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as growth inhibition after 24 hrs by MTT assay	[PMID: 24273639]
MDCK	IC₅₀	300 μM Compound: Sulindac	Anti-proliferative activity was evaluated by its ability to inhibit proliferation of MDCK cells Anti-proliferative activity was evaluated by its ability to inhibit proliferation of MDCK cells	[PMID: 11844707]
MDCK	IC₅₀	320 μM Compound: Sulindac	Anti-proliferative activity was evaluated by its ability to inhibit proliferation of MDCK-f3 (Madin-Darby canine kidney f3) cell line Anti-proliferative activity was evaluated by its ability to inhibit proliferation of MDCK-f3 (Madin-Darby canine kidney f3) cell line	[PMID: 11844707]
MIA PaCa-2	IC₅₀	> 200 μM Compound: a	Cytotoxicity against human MIAPaCa2 cells after 72 hrs by WST-1 assay Cytotoxicity against human MIAPaCa2 cells after 72 hrs by WST-1 assay	[PMID: 20801552]
MIA PaCa-2	IC₅₀	300 μM Compound: Sulindac	Cytotoxicity against human MIA PaCa-2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Cytotoxicity against human MIA PaCa-2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35439009]
NIH3T3	IC₅₀	200 μM Compound: Sulindac	Anti-proliferative activity was evaluated by its ability to inhibit proliferation of murine NIH3T3 fibroblasts Anti-proliferative activity was evaluated by its ability to inhibit proliferation of murine NIH3T3 fibroblasts	[PMID: 11844707]
REF	IC₅₀	100 μM Compound: Sulindac	Anti-proliferative activity was evaluated by its ability to inhibit proliferation of rat embryonic fibroblasts (REF) Anti-proliferative activity was evaluated by its ability to inhibit proliferation of rat embryonic fibroblasts (REF)	[PMID: 11844707]
SW480	IC₅₀	> 50 μM Compound: Sulindac	Cytotoxicity against human SW480 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay Cytotoxicity against human SW480 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay	[PMID: 32987314]
SW480	IC₅₀	> 50 μM Compound: Sulindac	Cytotoxicity against human SW480 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay Cytotoxicity against human SW480 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay	[PMID: 32987314]
SW480	IC₅₀	> 50 μM Compound: Sulindac	Cytotoxicity against human SW480 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Cytotoxicity against human SW480 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 32987314]
SW480	IC₅₀	800 μM Compound: Sulindac	Anti-proliferative activity was evaluated by its ability to inhibit proliferation of SW480 cells Anti-proliferative activity was evaluated by its ability to inhibit proliferation of SW480 cells	[PMID: 11844707]

体外研究
(In Vitro)

Sulindac (MK-231) (500 μM，48 小时) 可有效预防 TGF-β1 诱导的 EMT，表现为上皮标记物 E-钙粘蛋白的上调以及间充质标记物和转录因子的下调^[1]。
Sulindac (500 μM，48 h) 抑制 TGF-β1 增强的 A549 细胞迁移和侵袭^[1]。
Sulindac (500 μM，48 h) 增强 Sulindac 对 TGF-β1 诱导的 EMT 的逆转作用，SIRT1 上调促进 TGF-β1 诱导的 EMT^[1]。

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

Western Blot Analysis^[1]

Cell Line:	A549 cells
Concentration:	500 μM
Incubation Time:	48 h
Result:	Inhibit transforming growth factor (TGF)-β1-induced epithelial-mesenchymal transition in A549 cells.

Immunofluorescence^[1]

Cell Line:	A549 cells
Concentration:	500 μM
Incubation Time:	48 h
Result:	Reversed SIRT-1 expression by TGF-β1 and inhibited the TGF-β1-induced cadherin switch.

Cell Migration Assay ^[1]

Cell Line:	A549 cells
Concentration:	500 μM
Incubation Time:	48 h
Result:	Inhibited migration, decreased resistance co-treatment with TGF-β1.

Cell Invasion Assay^[1]

Cell Line:	A549 cells
Concentration:	500 μM
Incubation Time:	40 h; 48 h
Result:	Could effectively inhibit the TGF- β1-induced increase in invasion by lung cancer cells.

体内研究
(In Vivo)

Sulindac (MK-231) (15 mg/kg，po，bid (单独 Sulindac)；7.5 mg/kg po，bid (Sulindac 与 PD-L1 组合)) 显示肿瘤体积显著减少并增加 CD8+ T 淋巴细胞的浸润当用联合疗法处理时在肿瘤组织中^[2]。
Sulindac (15 mg/kg，口服，每天两次 (Sulindac 单独使用)；7.5 mg/kg 口服，每天两次 (Sulindac 与PD-L1)) 可通过阻断 NF-κB 信号通路下调 PD-L1，进而导致外泌体 P^[2]减少。
Sulindac (15 mg/kg，po，bid (单独 Sulindac)；7.5 mg/kg po，bid (Sulindac 与 PD-L1 联合)) 通过在联合处理中下调 PD-L1 导致 PD-L1 Ab 的可用性增加^[2]。
Sulindac (15 mg/kg，po，bid (单独 Sulindac)；7.5 mg/kg po，bid (Sulindac 与 PD-L1 组合)) 在低剂量下对前列腺素 E2 (PGE2) 没有系统性抑制作用^[2]。

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

Animal Model:	CT26 syngeneic mouse tumor model^[2]
Dosage:	15 mg/kg; 7.5 mg/kg
Administration:	15 mg/kg, p.o., bid (sulindac alone); 7.5 mg/kg p.o., bid (sulindac combination with PD-L1)
Result:	Downregulated PD-L1 through the blockade of NF-κB signaling and modulate the response of pMMR CRC to anti-PD-L1 immunotherapy. Cound effectively inhibit PD-L1 with no significant systematic toxicity.

Clinical Trial

分子量

356.41

Formula

C₂₀H₁₇FO₃S

CAS 号

38194-50-2

性状

固体

颜色

White to yellow

中文名称

舒林酸

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : 50 mg/mL (140.29 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

H₂O 中的溶解度 : < 0.1 mg/mL (insoluble)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.8058 mL	14.0288 mL	28.0576 mL
5 mM	0.5612 mL	2.8058 mL	5.6115 mL
10 mM	0.2806 mL	1.4029 mL	2.8058 mL

查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

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

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.01 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
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；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.01 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
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。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.81%

选择批次：

Data Sheet (648 KB) SDS (644 KB)

COA (292 KB) LCMS (98 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Byong-Ki Cha, et al. Celecoxib and sulindac inhibit TGF-β1-induced epithelial-mesenchymal transition and suppress lung cancer migration and invasion via downregulation of sirtuin 1. Oncotarget. 2016 Aug 30;7(35):57213-57227. [Content Brief]

[2]. Bin Yi, et al. Sulindac Modulates the Response of Proficient MMR Colorectal Cancer to Anti-PD-L1 Immunotherapy. Mol Cancer Ther. 2021 Jul;20(7):1295-1304. [Content Brief]

Sulindac 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.8058 mL	14.0288 mL	28.0576 mL	70.1439 mL
	5 mM	0.5612 mL	2.8058 mL	5.6115 mL	14.0288 mL
	10 mM	0.2806 mL	1.4029 mL	2.8058 mL	7.0144 mL
	15 mM	0.1871 mL	0.9353 mL	1.8705 mL	4.6763 mL
	20 mM	0.1403 mL	0.7014 mL	1.4029 mL	3.5072 mL
	25 mM	0.1122 mL	0.5612 mL	1.1223 mL	2.8058 mL
	30 mM	0.0935 mL	0.4676 mL	0.9353 mL	2.3381 mL
	40 mM	0.0701 mL	0.3507 mL	0.7014 mL	1.7536 mL
	50 mM	0.0561 mL	0.2806 mL	0.5612 mL	1.4029 mL
	60 mM	0.0468 mL	0.2338 mL	0.4676 mL	1.1691 mL
	80 mM	0.0351 mL	0.1754 mL	0.3507 mL	0.8768 mL
	100 mM	0.0281 mL	0.1403 mL	0.2806 mL	0.7014 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Sulindac (Synonyms: 舒林酸; MK-231)

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生物活性

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参考文献

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完整储备液配制表

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Sulindac (Synonyms: 舒林酸; MK-231)

Customer Review

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Sulindac 相关产品

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参考文献

Sulindac 相关抗体:

摩尔计算器

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完整储备液配制表

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