2. Epigenetics
  3. DNA Methyltransferase
  4. Guadecitabine sodium

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

Cat. No.: HY-15229 Purity: 98.04%
COA 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

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5 mg USD 850 In-stock
10 mg USD 1200 In-stock
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Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of Guadecitabine sodium:

Guadecitabine sodium Related Antibodies

Top Publications Citing Use of Products

    Guadecitabine sodium purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2023 Mar 18;42(1):67.  [Abstract]

    Guadecitabine (1mg/kg; s.c.; single daily for 13 consecutive days) significantly decreases mean tumor volume of mice.

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

    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.  [Abstract]

    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:

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    DNA Methyltransferase DNMT1 DNMT3 MGMT

    • 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.

    Guadecitabine sodium Related Antibodies
    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

    Appearance

    Solid

    Formula

    C18H23N9NaO10P
    CAS No.
    SMILES

    O=C1C2=C(N([C@H]3C[C@H](O)[C@@H](COP(O[C@@H]4[C@@H](CO)O[C@@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

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    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:  PBS

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

    • 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

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 98.05%

    COA (247 KB) HNMR (221 KB) RP-HPLC (423 KB)

    Handling Instructions (2659 KB)
    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
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    Guadecitabine sodium Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Keywords:

    Guadecitabine929904-85-8SGI-110S-110SGI110SGI 110S110S 110DNA MethyltransferaseDNMTsDNA MTasesInhibitorinhibitorinhibit

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