1. Epigenetics
  2. DNA Methyltransferase
  3. Guadecitabine

Guadecitabine (Synonyms: SGI-110)

Cat. No.: HY-13542 Purity: 98.00%
Handling Instructions

Guadecitabine (SGI-110) is a second-generation DNA methyltransferases (DNMT) inhibitor for research of acute myeloid leukemia (AML) and myelodysplastic syndromes (MDS).

For research use only. We do not sell to patients.

Guadecitabine Chemical Structure

Guadecitabine Chemical Structure

CAS No. : 929901-49-5

Size Stock
100 mg   Get quote  
250 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Other In-stock Forms of Guadecitabine:

Other Forms of Guadecitabine:

Top Publications Citing Use of Products

    Guadecitabine purchased from MCE. Usage Cited in: Neoplasia. 2020 May 25;22(7):274-282.

    Immunoblot of the total RH30 and RH41 cell extracts treated with the indicated concentrations of SGI-110 or DMSO (control) for 5 days, probed with antibodies against FGFR4, FOXO1, IGF-1R and MYOD1.

    Guadecitabine purchased from MCE. Usage Cited in: Neoplasia. 2020 May 25;22(7):274-282.

    Immunofluorescent analysis of RH30 and RH41 cells treated with DMSO or indicated concentrations of SGI-110 for 5 days.

    View All DNA Methyltransferase Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Guadecitabine (SGI-110) is a second-generation DNA methyltransferases (DNMT) inhibitor for research of acute myeloid leukemia (AML) and myelodysplastic syndromes (MDS)[1].

    IC50 & Target[1]

    DNA Methyltransferase

     

    In Vitro

    Exposure to Guadecitabine induces the expression of investigated cancer/testis antigens (CTA) in CTA-negative cancer cells. Results show that Guadecitabine induces and/or strongly up-regulates the constitutive levels of MAGE-A3- and NY-ESO-1-specific mRNA expression in neoplastic cells of all histotypes investigated. Exposure to Guadecitabine significantly (p<0.05) up-regulates the constitutive levels of expression of HLA class I antigens, HLA-A2 allospecificity, and of the co-stimulatory molecule ICAM-1, on Mel 275 melanoma cells. Results show that treatment with Guadecitabine induces a significant (p<0.01) reduction in the constitutive methylation levels of CTA promoters in investigated cancer cells. Mean values of the percentage of demethylation induced by Guadecitabine in MAGE-A1 and NY-ESO-1 promoters are 57 and 30 %, in Mel 195, and 22 and 33 % in MZ-1257 RCC cells, respectively[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    In Vivo

    Guadecitabine (S110) is effective at retarding tumor growth. While the tumors do not shrink in size with Guadecitabine treatment, they experience very minimal growth while the tumors treated with PBS only show substantial growth. In addition, Guadecitabine induces much less toxicity as determined by mouse weight changes when given subcutaneously (SQ) compare to that with IP injections[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    Molecular Weight

    557.41

    Formula

    C₁₈H₂₄N₉O₁₀P

    CAS No.

    929901-49-5

    SMILES

    O=C1C2=C(N([[email protected]]3C[[email protected]](O)[[email protected]@H](COP(O)(O[[email protected]@H]4[[email protected]@H](CO)O[[email protected]@H](N5C=NC(N)=NC5=O)C4)=O)O3)C=N2)NC(N)=N1

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years

    *The compound is unstable in solutions, freshly prepared is recommended.

    Solvent & Solubility
    In Vitro: 

    H2O

    References
    Cell Assay
    [2]

    Cells (3 to 4×105) are seeded in a T75 tissue culture flask and treated 24 h later with Guadecitabine , by replacing the medium with fresh one containing 1 μM or 10 μM of Guadecitabine, every 12 h for 2 days (4 pulses) and then with fresh medium without drugs for additional 2 days. Control cultures are treated under similar experimental conditions in the absence of drug[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [3]

    Athymic nu/nu mice are inoculated subcutaneously (SQ) in the right hind flank with 107 EJ6 bladder cancer cells. After tumors reach 0.5 cm in diameter, animals are stratified into three groups with eight animals per group to begin treatments. Doses and dosing schedules are designed so that each group receives molar equivalents of Guadecitabine (S110). The agent is administered SQ once weekly at a dose of 12.2 mg/kg for Guadecitabine for three weeks. The study includes an appropriate PBS control group. Tumor sizes by caliper and body weight measurements are taken twice weekly to monitor tumor growth inhibition and tolerability[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.
    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Keywords:

    GuadecitabineSGI-110SGI110SGI 110DNA MethyltransferaseDNMTsDNA MTasesInhibitorinhibitorinhibit

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

     

    Salutation

    Applicant Name *

     

    Email address *

    Phone number *

     

    Organization name *

    Department *

     

    Requested quantity *

    Country or Region *

         

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    Guadecitabine
    Cat. No.:
    HY-13542
    Quantity:
    MCE Japan Authorized Agent: