2. Epigenetics
  3. DNA Methyltransferase
  4. Guadecitabine

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

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Guadecitabine 構造式

Guadecitabine 構造式

CAS 番号 : 929901-49-5

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Guadecitabine 関連抗体

Top Publications Citing Use of Products

    Guadecitabine purchased from MedChemExpress. 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 purchased from MedChemExpress. 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 purchased from MedChemExpress. 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.

    DNA Methyltransferase アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    DNA Methyltransferase DNMT1 DNMT3 MGMT

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    製品説明

    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

     

    体外実験

    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].

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

    Guadecitabine 関連抗体
    体内実験

    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    臨床実験
    分子量

    557.41

    分子式

    C18H24N9O10P
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years

    *The compound is unstable in solutions, freshly prepared is recommended.
    溶剤 & 溶解度
    体外: 

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    純度とドキュメンテーション
    参考文献
    細胞実験
    [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].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    動物実験
    [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].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献
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    Guadecitabine Related Classifications

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    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

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    • 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.

    Keywords:

    Guadecitabine929901-49-5SGI-110SGI110SGI 110DNA MethyltransferaseDNMTsDNA MTasesInhibitorinhibitorinhibit

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    製品名:
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    製品番号:
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