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Purity: ≥98%
Sulindac (Aflodac; Algocetil; MK231; MK 231; MK-231), belonging to the arylalkanoic acid class of non-steroidal antiinflammatory drugs (NSAIDs), is a non-steroidal COX inhibitor, which potently inhibits prostaglandin synthesis. It has been used in the treatment of acute or chronic inflammatory conditions. Sulindac is a prodrug, derived from sulfinylindene, that is converted in the body to the active NSAID, sulindac sulfide, a cyclooxgenase inhibitor that represses ras signaling, and sulindac sulfone, an antitumor agent, following oral administration in vivo.
| ln Vitro |
TGF-β1-induced epithelial-mesenchymal transition (EMT) is efficiently inhibited by sulindac (MK-231) (500 μM, 48 hours), as evidenced by the overexpression of the epithelial marker E-cadherin and the downregulation of transcription factors and mesenchymal markers [1]. The TGF-β1-enhanced migration and invasion of A549 cells is inhibited by sulindac (500 μM, 48 h) [1]. TGF-β1-induced EMT is more effectively reversed by sulindac (500 μM, 48 h), and SIRT1 overexpression encourages TGF-β1-induced EMT[1].
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| ln Vivo |
Sulindac (MK-231) (15 mg/kg po, bid; sulindac alone); 7.5 mg/kg po, bid; sulindac plus PD-L1)) demonstrated a marked decrease in tumor volume and an increase in CD8+ T cell infiltration. in tumor tissue following combination therapy treatment [2]. By inhibiting the NF-κB signaling pathway, sulindac (15 mg/kg orally twice daily; 7.5 mg/kg orally twice daily; sulindac with PD-L1) can downregulate PD-L1 and reduce exosome P[2]. By downregulating PD-L1 in combination treatment, sulindac (15 mg/kg po, bid; sulindac alone); 7.5 mg/kg po, bid; sulindac in conjunction with PD-L1)) increases the availability of PD-L1 Ab [2]. Prostaglandin E2 (PGE2) is not systemically inhibited by sulindac at low dosages (15 mg/kg po, bid; sulindac alone; 7.5 mg/kg po, bid; sulindac in conjunction with PD-L1)[2].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: A549 cells Tested Concentrations: 500 μM Incubation Duration: 48 h Experimental Results: Inhibit transforming growth factor (TGF)-β1-induced epithelial-mesenchymal transition in A549 cells. Immunofluorescence[1] Cell Types: A549 cells Tested Concentrations: 500 μM Incubation Duration: 48 h Experimental Results: Reversed SIRT-1 expression by TGF-β1 and inhibited the TGF-β1-induced cadherin switch. Cell Migration Assay [1] Cell Types: A549 cells Tested Concentrations: 500 μM Incubation Duration: 48 h Experimental Results: Inhibited migration, diminished resistance co-treatment with TGF-β1. Cell Invasion Assay[1] Cell Types: A549 cells Tested Concentrations: 500 μM Incubation Duration: 40 h; 48 h Experimental Results: Could effectively inhibit the TGF- β1-induced increase in invasion by lung cancer cells. |
| Animal Protocol |
Animal/Disease Models: CT26 syngeneic mouse tumor model[2]
Doses: 15 mg/kg; 7.5 mg/kg Route of Administration: 15 mg/kg, po, bid (sulindac alone); 7.5 mg/kg po, bid (sulindac combination with PD- L1) Experimental Results: 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. |
| References |
[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.
[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. |
| Molecular Formula |
C20H17FO3S
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| Molecular Weight |
356.41
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| CAS # |
38194-50-2
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| Related CAS # |
Sulindac sulfide;49627-27-2;Sulindac sodium;63804-15-9;Sulindac-d3;Sulindac sulfone;59973-80-7
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| SMILES |
O=C(CC(C1=C2C=CC(F)=C1)=C(/C2=C/C3=CC=C(C=C3)S(C)=O)C)O
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| InChi Key |
MLKXDPUZXIRXEP-MFOYZWKCSA-N
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| InChi Code |
InChI=1S/C20H17FO3S/c1-12-17(9-13-3-6-15(7-4-13)25(2)24)16-8-5-14(21)10-19(16)18(12)11-20(22)23/h3-10H,11H2,1-2H3,(H,22,23)/b17-9-
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| Chemical Name |
(Z)-2-(5-fluoro-2-methyl-1-(4-(methylsulfinyl)benzylidene)-1H-inden-3-yl)acetic acid
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.01 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.01 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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