Guadecitabine (SGI-110)

Synonyms: S-110

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

Guadecitabine (SGI-110) Chemical Structure

Guadecitabine (SGI-110) Chemical Structure

CAS: 929904-85-8

Selleck's Guadecitabine (SGI-110) has been cited by 6 publications

Purity & Quality Control

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

Guadecitabine (SGI-110) Related Products

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
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 Active not 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

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)

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


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In vivo
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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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