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Guadecitabine (SGI-110)

Name: Guadecitabine (SGI-110)
Brand: Selleck Chemicals
SKU: S7013
Rating: 5 (6 reviews)

Synonyms: S-110

Catalog No.S7013 Purity:99.93%

Guadecitabine (SGI-110, S-110) is a next-generation hypomethylating agent.

Guadecitabine (SGI-110) Chemical Structure

CAS No. 929904-85-8

Purity & Quality Control

Batch: S701301 DMSO]100 mg/mL]false]Water]50 mg/mL]false]Ethanol]Insoluble]false Purity: 99.93%

99.93

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Related Compound Libraries	Kinase Inhibitor Library FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I Bioactive Compound Library-Ⅱ	Click to Expand

Biological Activity

Description

Guadecitabine (SGI-110, S-110) is a next-generation hypomethylating agent.

Targets

DNA methyltransferase ^[1]

In vitro
In vitro	SGI-110 is a 5-aza-2’-deoxycytidine-containing demethylating dinucleotide, which works via a mechanism similar to that of 5-aza-CdR after incorporation of its aza-moiety into DNA. However, SGI-110 is well protected from deamination by cytidine deaminase. SGI-110 (1 μM) induces significantly decrease in the level of methylation in both T24 and HCT116 cells. SGI-110 is able to induce robust p16 expression. SGI-110 (1 μM) causes depletion of extractable DNMT1 in cells. SGI-110 decreases the plating efficiency of T24 bladder carcinoma cells in a dose-dependent manner, with no colonies forming at 10 μM concentration, which is quite similar to 5-aza-CdR in T24 cells. ^[1] SGI-110 shows immunomodulatory activity in vitro. SGI-110 (1 μM) induces/up-regulates the expression of several cancer/testis antigens (CTA) (i.e., MAGE-A1, MAGE-A2, MAGE-A3, MAGE-A4, MAGE-A10, GAGE1-2, GAGE 1-6, NY-ESO-1, and SSX 1-5) in cancer cell lines (cutaneous melanoma, mesothelioma, renal cell carcinoma, and sarcoma cells), both at mRNA and at protein levels. SGI-110 also up-regulates the expression of HLA class I antigens and of ICAM-1, resulting in an improved recognition of cancer cells by gp100-specific CTL. ^[2]
Cell Research	Cell lines	UMUC-3 cells
	Concentrations	2 μM
	Incubation Time	24 h
	Method	Cells were treated with indicated concentrations of drug.

In Vivo
In vivo	SGI-110 is as effective as 5-Aza-CdR, but is better tolerated in mice. SGI-110 (10 mg/kg) displays potent activity on inducing p16 expression, reducing DNA methylation at the p16 promoter region, and retarding tumor growth in human xenograft. SGI-110 is effective by both i.p. and s.c. deliveries. ^[3]
Animal Research	Animal Models	Human bladder cancers xenografts EJ6
	Dosages	10 mg/kg
	Administration	i.p. or s.c.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT03576963	Withdrawn	Colorectal Adenocarcinoma\|CpG Island Methylator Phenotype\|Metastatic Microsatellite Stable Colorectal Carcinoma\|Refractory Colorectal Carcinoma\|Stage IV Colorectal Cancer AJCC v8\|Stage IVA Colorectal Cancer AJCC v8\|Stage IVB Colorectal Cancer AJCC v8\|Stage IVC Colorectal Cancer AJCC v8	University of Southern California\|National Cancer Institute (NCI)\|Bristol-Myers Squibb\|Astex Pharmaceuticals Inc.	January 30 2020	Phase 1\|Phase 2
NCT03085849	Completed	Extensive-stage Small Cell Lung Cancer	Catherine Shu\|Columbia University	December 15 2017	Phase 1
NCT03179943	Active not recruiting	Urothelial Carcinoma	Fox Chase Cancer Center\|Stand Up To Cancer\|Van Andel Research Institute	November 27 2017	Phase 2
NCT02998567	Recruiting	Castration-Resistant Prostatic Cancer\|Non Small Cell Lung Cancer	Royal Marsden NHS Foundation Trust\|Astex Pharmaceuticals Inc.\|Merck Sharp & Dohme LLC\|Institute of Cancer Research United Kingdom	January 26 2017	Phase 1
NCT02892318	Completed	Acute Myeloid Leukemia	Hoffmann-La Roche	October 31 2016	Phase 1

References

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Chemical Information & Solubility

Molecular Weight	579.39	Formula	C₁₈ H₂₃ N₉ O₁₀ P . Na
CAS No.	929904-85-8	SDF	--
Smiles	C1C(C(OC1N2C=NC3=C2N=C(NC3=O)N)COP(=O)([O-])OC4CC(OC4CO)N5C=NC(=NC5=O)N)O.[Na+]
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 100 mg/mL ( (172.59 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 50 mg/mL

Ethanol : Insoluble

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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