Home Methylation Others Guadecitabine (SGI-110) For research use only.

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

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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 lnformation & 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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