[CAS NO. 38194-50-2] Sulindac

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PRODUCTS SPECIFICATIONS [38194-50-2]

Catalog

HY-B0008

Brand

MCE

CAS

38194-50-2

DESCRIPTION [38194-50-2]

Overview

MDL	MFCD00599589
Molecular Weight	356.41
Molecular Formula	C20H17FO3S
SMILES	O=C(CC(C1=C2C=CC(F)=C1)=C(/C2=C/C3=CC=C(C=C3)S(C)=O)C)O

For research use only. We do not sell to patients.

Summary

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

COX-2

Autophagy

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] .

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.

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] .

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

NCT Number	Sponsor	Condition	Start Date	Phase
NCT00841204	National Cancer Institute (NCI)	Precancerous Condition	February 2009	Phase 2
NCT01856322	National Cancer Institute (NCI)\|Charite University, Berlin, Germany\|National Institutes of Health Clinical Center (CC)	Colorectal Cancer\|Liver Metastasis\|Colorectal Adenocarcinoma	April 2013	Phase 2
NCT01636128	Cancer Prevention Pharmaceuticals, Inc.\|University of Arizona	Focus of Study: Drug Response Biomarkers, Chemoprevention, Neoplasms	March 2014	Phase 2
NCT01843179	Massachusetts General Hospital	Acute Myeloid Leukemia	January 2014	Phase 2
NCT04542135	Stony Brook University\|Medical University of South Carolina\|Cedars-Sinai Medical Center	Breast Cancer	November 20, 2020	Phase 2
NCT00343629	Mayo Clinic\|National Cancer Institute (NCI)	Unspecified Adult Solid Tumor, Protocol Specific	April 2006	Not Applicable
NCT01187901	University of Utah\|National Cancer Institute (NCI)	Adenomatous Polyposis Coli	April 2010	Phase 2
NCT01349881	Southwest Oncology Group\|National Cancer Institute (NCI)\|Cancer Prevention Pharmaceuticals, Inc.	Colorectal Neoplasms	March 1, 2013	Phase 3
NCT00039520	Fox Chase Cancer Center\|National Cancer Institute (NCI)	Breast Cancer	January 2002	Phase 2
NCT04823052	Healx Limited	Fragile X Syndrome	May 25, 2022	Phase 2
NCT00299195	Memorial Sloan Kettering Cancer Center\|Amrita Institute of Sciences, AIMS, Cochin, India\|Weill Medical College of Cornell University\|Regional Cancer Center(RCC), Trivandrum, India\|Narayana Hrudayalaya Hospitals	Leukoplakia, Oral\|Benign Neoplasms	February 23, 2006	Not Applicable
NCT00368927	National Cancer Institute (NCI)	Precancerous Condition\|Stage I Non-small Cell Lung Cancer\|Tobacco Use Disorder	August 2006	Phase 2
NCT00755976	Cancer Trials Ireland	Melanoma (Skin)	August 2007	Phase 2
NCT00068419	Children´s Oncology Group\|National Cancer Institute (NCI)	Desmoid Tumor	February 2004	Phase 2
NCT00003365	University of Medicine and Dentistry of New Jersey\|National Cancer Institute (NCI)\|Rutgers, The State University of New Jersey	Colorectal Cancer	August 1996	Not Applicable
NCT00335504	National Cancer Institute (NCI)	Colon Cancer\|Precancerous Condition\|Rectal Cancer	March 2006	Phase 2
NCT00392665	Massachusetts General Hospital\|Dana-Farber Cancer Institute\|Emory University\|University of North Carolina, Chapel Hill\|Genentech, Inc.\|OSI Pharmaceuticals	Squamous Cell Carcinoma of the Head and Neck (SCCHN)	October 2006	Phase 2
NCT00118365	National Cancer Institute (NCI)	Precancerous Condition	July 1998	Phase 3
NCT00062023	M.D. Anderson Cancer Center\|National Cancer Institute (NCI)	Colorectal Cancer	June 2003	Phase 2
NCT00319007	Radboud University Medical Center\|Dutch Cancer Society	Adenomatous Polyposis Coli	April 2006	Phase 2
NCT01515137	University of Pittsburgh\|OSI Pharmaceuticals	Head and Neck Squamous Cell Carcinoma	November 2005	Phase 1
NCT01483144	Cancer Prevention Pharmaceuticals, Inc.	Familial Adenomatous Polyposis	October 2013	Phase 3
NCT00245024	National Cancer Institute (NCI)\|University of Arizona	Breast Cancer	November 2005	Phase 1
NCT01761877	Stony Brook University	Inflammation\|Cancer\|Pain\|Hypertension	December 2012	Phase 2
NCT01245816	Cancer Prevention Pharmaceuticals, Inc.	Familial Adenomatous Polyposis	March 2011	Phase 3
NCT00176618	University of Medicine and Dentistry of New Jersey\|Rutgers, The State University of New Jersey	Aberrant Crypt Foci	April 2004	Not Applicable
NCT04207944	Duke University\|Johns Hopkins University\|Massachusetts General Hospital\|Memorial Sloan Kettering Cancer Center\|National Cancer Institute (NCI)	IPMN\|IPMN, Pancreatic	July 10, 2020	Phase 2

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL ( 140.29 mM ; Need ultrasonic)

H ₂ O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (7.01 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (7.01 mM); Clear solution

* All of the co-solvents are available by MCE.

References

Synonyms

1H-Indene-3-acetic acid, 5-fluoro-2-methyl-1-[[4-(methylsulfinyl)phenyl]methylene]-, (1Z)-

1H-Indene-3-acetic acid, 5-fluoro-2-methyl-1-[[4-(methylsulfinyl)phenyl]methylene]-, (Z)-

(1Z)-5-Fluoro-2-methyl-1-[[4-(methylsulfinyl)phenyl]methylene]-1H-indene-3-acetic acid

cis-5-Fluoro-2-methyl-1-[(p-methylsulfinyl)benzylidenyl]indene-3-acetic acid

Sulindac

Clinoril

MK 231

Arthrocine

Mobilin

cis-Sulindac

Sulindac sulfoxide

Clisundac

Artribid

Reumofil

Sulreuma

Algocetil

Citireuma

Sudac

Aflodac

Reumyl

Sulinol

Imbaral

(Z)-5-Fluoro-2-methyl-1-[p-(methylsulfinyl)benzylidene]indene-3-acetic acid