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。
生物活性 | Sulindac (MK-231) is an orally active nonsteroidalanti-inflammatoryagent. Sulindac also is an immunomodulatory agent. Sulindac can be used for the research of arthritis of the spine, gouty arthritis and kinds ofcancerincluding colorectalcancer(CRC) and lungcancer[1][2]. |
IC50& Target[1] | |
体外研究 (In Vitro) | Sulindac (MK-231) (500 μM, 48 h) is effective in preventing TGF-β1-induced EMT, as indicated by upregulation of the epithelial marker, E-cadherin, and downregulation of mesenchymal markers and transcription factors[1]. Sulindac (500 μM, 48 h) can inhibit TGF-β1-enhanced migration and invasion of A549 cells[1]. Sulindac (500 μM, 48 h) enhances the reversal of TGF-β1-induced EMT by sulindac and SIRT1 upregulation promoted TGF-β1-induced EMT[1].
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. |
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体内研究 (In Vivo) | Sulindac (MK-231) (15 mg/kg, p.o., bid (sulindac alone); 7.5 mg/kg p.o., bid (sulindac combination with PD-L1)) shows a significant reduction in tumor volume and increases infiltration of CD8+ T lymphocytes in the tumor tissues when treated with combination therapy[2]. Sulindac (15 mg/kg, p.o., bid (sulindac alone); 7.5 mg/kg p.o., bid (sulindac combination with PD-L1)) can downregulate PD-L1 by blocking NF-κB signaling, which in turn led to a decrease in exosomal P[2]. Sulindac (15 mg/kg, p.o., bid (sulindac alone); 7.5 mg/kg p.o., bid (sulindac combination with PD-L1)) leads to increased availability of PD-L1 Ab by downregulating PD-L1 in combination therapy[2]. Sulindac (15 mg/kg, p.o., bid (sulindac alone); 7.5 mg/kg p.o., bid (sulindac combination with PD-L1)) has not a systemic inhibitory effect on prostaglandin E2 (PGE2) in low-dose does[2].
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. |
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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 | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 50 mg/mL(140.29 mM;Need ultrasonic) H2O :< 0.1 mg/mL(insoluble) 配制储备液 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 |
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此方案可获得 ≥ 2.5 mg/mL (7.01 mM,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;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 (7.01 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.01 mM,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 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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