1. Epigenetics
  2. DNA Methyltransferase
  3. Guadecitabine

Guadecitabine (Synonyms: SGI-110)

製品番号: HY-13542 純度: 98.00%
取扱説明書

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

容量 在庫状況
100 mg   お問い合わせ  
250 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

Other 在庫あり 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.

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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].

    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].

    臨床実験
    分子量

    557.41

    分子式

    C₁₈H₂₄N₉O₁₀P

    CAS 番号

    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

    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: 

    H2O

    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].

    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].

    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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    Keywords:

    GuadecitabineSGI-110SGI110SGI 110DNA MethyltransferaseDNMTsDNA MTasesInhibitorinhibitorinhibit

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    製品名:
    Guadecitabine
    製品番号:
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