Guadecitabine (SGI-110)

Catalog No.S7013 Synonyms: S-110

For research use only.

Guadecitabine (SGI-110, S-110) is a next-generation hypomethylating agent whose active metabolite decitabine has a longer in-vivo exposure time than intravenous decitabine.

Guadecitabine (SGI-110) Chemical Structure

CAS No. 929904-85-8

Selleck's Guadecitabine (SGI-110) has been cited by 3 Publications

Purity & Quality Control

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Biological Activity

Description Guadecitabine (SGI-110, S-110) is a next-generation hypomethylating agent whose active metabolite decitabine has a longer in-vivo exposure time than intravenous decitabine.
Targets
DNA methyltransferase [1]
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]

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]

Protocol (from reference)

Animal Research:

[3]

  • Animal Models: Human bladder cancers xenografts EJ6
  • Dosages: 10 mg/kg
  • Administration: i.p. or s.c.
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(172.59 mM)
Water 50 mg/mL
(86.29 mM)
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 579.39
Formula

C18 H23 N9 O10 P . Na

CAS No. 929904-85-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1C(C(OC1N2C=NC3=C2N=C(NC3=O)N)COP(=O)([O-])OC4CC(OC4CO)N5C=NC(=NC5=O)N)O.[Na+]

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

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Molarity Calculator

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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.

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