Guadecitabine (SGI-110)

Catalog No.S7013 Batch:S701301

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Technical Data

Formula

C18 H23 N9 O10 P . Na
Molecular Weight 579.39 CAS No. 929904-85-8
Solubility (25°C)* In vitro DMSO 100 mg/mL (172.59 mM)
Water 50 mg/mL (86.29 mM)
Ethanol Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

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

Cell Assay:

[5]
  • Cell lines

    UMUC-3 cells

  • Concentrations

    2 μM

  • Incubation Time

    24 h

  • Method

    Cells were treated with indicated concentrations of drug.
Animal Study:

[3]
  • Animal Models

    Human bladder cancers xenografts EJ6

  • Dosages

    10 mg/kg

  • Administration

    i.p. or s.c.

Selleck's Guadecitabine (SGI-110) has been cited by 7 publications

DNA methyltransferase inhibition promotes recruitment of myeloid-derived suppressor cells to the tumor microenvironment through induction of tumor cell-intrinsic interleukin-1 [ Cancer Lett, 2023, 552:215982] PubMed: 36309209
DNA Methyltransferase 1 Targeting Using Guadecitabine Inhibits Prostate Cancer Growth by an Apoptosis-Independent Pathway [ Cancers (Basel), 2023, 15(10)2763] PubMed: 37345101
DNA methylation subtypes guiding prognostic assessment and linking to responses the DNA methyltransferase inhibitor SGI-110 in urothelial carcinoma [ BMC Med, 2022, 20(1):222] PubMed: 35843958
Growth Inhibition and Induction of Innate Immune Signaling of Chondrosarcomas with Epigenetic Inhibitors [ Mol Cancer Ther, 2021, 20(12):2362-2371] PubMed: 34552007
Growth Inhibition and Induction of Innate Immune Signaling of Chondrosarcomas with Epigenetic Inhibitors [ Mol Cancer Ther, 2021, molcanther.MCT-21-0066-A.2021] PubMed: 34552007
Smac mimetics and TRAIL cooperate to induce MLKL-dependent necroptosis in Burkitt's lymphoma cell lines [ Neoplasia, 2021, 23(5):539-550] PubMed: 33971465
Epigenetic repression of miR-375 is the dominant mechanism for constitutive activation of the PDPK1/RPS6KA3 signalling axis in multiple myeloma [ Br J Haematol, 2017, 178(4):534-546] PubMed: 28439875

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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