1. Epigenetics
  2. DNA Methyltransferase
  3. Guadecitabine sodium

Guadecitabine sodium (Synonyms: SGI-110 sodium; S-110 sodium)

Cat. No.: HY-15229 Purity: 96.68%
Handling Instructions

Guadecitabine sodium (SGI-110 sodium) 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 sodium Chemical Structure

Guadecitabine sodium Chemical Structure

CAS No. : 929904-85-8

Size Price Stock Quantity
5 mg USD 850 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1200 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of Guadecitabine sodium:

Top Publications Citing Use of Products

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

    IC50 & Target[1]

    DNMT1

     

    In Vitro

    After HCT116 colorectal carcinoma cells are treated for 6 days, a dose-dependent increase in p16expression is observed with Guadecitabine sodium (SGI-110 sodium). In addition, T24 and HCT116 cells treated with Guadecitabine sodium or 5-aza-CdR for 3 days show a dose-dependent increase in the level of p16 protein, showing the competence of Guadecitabine sodium to inhibit DNA methylation and induce p16 at both mRNA and protein levels as well as 5-aza-CdR. Thus, Guadecitabine sodium is able to inhibit DNA methylation at 5′-region and induce the expression of the p16 gene in T24 and HCT116 cells at concentrations comparable to 5-aza-CdR, and the induction of p16 expression by both agents correlates with the demethylation at the 5′-end region of the gene in both cell lines. Guadecitabine sodium is slightly less toxic than 5-aza-CdR at the doses tested up to 1 μM concentration but displaying similar toxicity at 10 μM concentration[1].

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

    In Vivo

    Guadecitabine sodium (SGI-110 sodium) at 10mg/kg is an effective dose at reducing DNA methylation and retarding tumor growth, and caused roughly the same level of toxicity as 5-Aza-CdR. Guadecitabine sodium is effective in vivo at reactivating the expression of the p16 gene, which is heavily methylated in the parent EJ6 cells. Guadecitabine sodium is effective in reducing the level of DNA methylation in vivo at the p16 promoter region. Guadecitabine sodium is better tolerated than 5-Aza-CdR in vivo, suggesting that it can be an attractive alternative for potential clinical use[2].

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

    Clinical Trial
    Molecular Weight

    579.39

    Formula

    C₁₈H₂₃N₉NaO₁₀P

    CAS No.
    SMILES

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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    H2O : 50 mg/mL (86.30 mM; Need ultrasonic and warming)

    DMSO : 50 mg/mL (86.30 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.7260 mL 8.6298 mL 17.2595 mL
    5 mM 0.3452 mL 1.7260 mL 3.4519 mL
    10 mM 0.1726 mL 0.8630 mL 1.7260 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  1% DMSO    99% saline

      Solubility: ≥ 0.5 mg/mL (0.86 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (4.31 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (4.31 mM); Clear solution

    • 4.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (4.31 mM); Clear solution

    • 5.

      Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% saline

      Solubility: ≥ 2.5 mg/mL (4.31 mM); Clear solution

    • 6.

      Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (4.31 mM); Clear solution

    • 7.

      Add each solvent one by one:  PBS

      Solubility: 33.33 mg/mL (57.53 mM); Clear solution; Need ultrasonic

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [1]

    T24 cells are plated at a low density (100 per 60-mm dish) and treated with varying concentrations of 5-aza-CdR and S-110 (0.1, 0.2, 10 μM. Colonies are allowed to form for 10 to 14 days, fixed with methanol, and stained with 10% Giemsa. The number of colonies from an untreated control plate is used to calculate the plating efficiency in percent at each concentration. Triplicate dishes are used, and error bars are represented by 1 SD of the mean[1].

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

    Animal Administration
    [2]

    Mouse: Athymic nu/nu mice are inoculated subcutaneously 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 received molar equivalents of either S-110 or 5-Aza-CdR. The agents are administered SQ once weekly at a dose of 12.2 mg/kg for S-110 and 5.0 mg/kg for 5-Aza-CdR 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[2].

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

    References

    Purity: 98.05%

    • 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-110S-110SGI110SGI 110S110S 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 sodium
    Cat. No.:
    HY-15229
    Quantity:
    MCE Japan Authorized Agent: