Guadecitabine
Based on 12 publication(s) in Google Scholar
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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- CAS No.: 929901-49-5
- Formule: C18H24N9O10P
- Masse moléculaire:557.41
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Stockage:Powder -20°C, 3 years
* The compound is unstable in solutions, freshly prepared is recommended.
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Publications Citing Use of MedChemExpress (MCE) Guadecitabine
More- Cancer Res. 2020 Jul 15;80(14):3046-3056. [Abstract]
- Mol Cell. 2022 Oct 20;82(20):3901-3918.e7. [Abstract]
- J Exp Clin Cancer Res. 2023 Mar 18;42(1):67. [Abstract]
- J Transl Med. 2024 Mar 1;22(1):223. [Abstract]
- Neoplasia. 2020 May 25;22(7):274-282. [Abstract]
- Epigenomes. 2021 Dec 14;5(4):27. [Abstract]
- JID Innov. 2024 Oct 16;5(2):100319. [Abstract]
- McGill University. 2025.
- bioRxiv. 2025 February 08.
- bioRxiv. 2024 August 09.
- Research Square Print. January 3rd, 2023.
- University of Siena. 2021 May.
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Cell Proliferation/Viability Assay
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IF
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Activité biologique
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DNA Methyltransferase |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 929901-49-5
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Appearance Solid
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Masse moléculaire 557.41
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Formule C18H24N9O10P
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Color White to off-white
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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
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Synonyms
SGI-110
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years * The compound is unstable in solutions, freshly prepared is recommended.
Publications (12)
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Journal Impact Factor
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Most Recent
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Cancer Res
Targeting Hippo-Dependent and Hippo-Independent YAP1 Signaling for the Treatment of Childhood Rhabdomyosarcoma. [Abstract]2020 Jul 15;80(14):3046-3056. PMID: 32354737 -
Mol Cell
2022 Oct 20;82(20):3901-3918.e7. PMID: 36206767 -
J Exp Clin Cancer Res
Guadecitabine increases response to combined anti-CTLA-4 and anti-PD-1 treatment in mouse melanoma in vivo by controlling T-cells, myeloid derived suppressor and NK cells. [Abstract]2023 Mar 18;42(1):67. PMID: 36934257
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.
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J Transl Med
Epigenetic remodeling to improve the efficacy of immunotherapy in human glioblastoma: pre-clinical evidence for development of new immunotherapy approaches. [Abstract]2024 Mar 1;22(1):223. PMID: 38429759 -
Neoplasia
Molecular mechanisms of Guadecitabine induced FGFR4 down regulation in alveolar rhabdomyosarcomas. [Abstract]2020 May 25;22(7):274-282. PMID: 32464274
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.
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Epigenomes
Epigenetic Immune Remodeling of Mesothelioma Cells: A New Strategy to Improve the Efficacy of Immunotherapy. [Abstract]2021 Dec 14;5(4):27. PMID: 34968251 -
JID Innov
DNA Methyltransferase Inhibition Upregulates the Costimulatory Molecule ICAM-1 and the Immunogenic Phenotype of Melanoma Cells. [Abstract]2024 Oct 16;5(2):100319. PMID: 39867570 -
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Solvant et solubilité
Protocole
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) has not independently confirmed the accuracy of these methods. They are for reference only.
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) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Foulks JM, et al. Epigenetic drug discovery: targeting DNA methyltransferases. J Biomol Screen. 2012 Jan;17(1):2-17. [Content Brief]
[2]. Chuang JC, et al. S110, a 5-Aza-2'-deoxycytidine-containing dinucleotide, is an effective DNA methylation inhibitor in vivo and can reduce tumor growth. Mol Cancer Ther. 2010 May;9(5):1443-50. [Content Brief]
[3]. Coral S, et al. Immunomodulatory activity of SGI-110, a 5-aza-2'-deoxycytidine-containing demethylating dinucleotide. Cancer Immunol Immunother. 2013 Mar;62(3):605-14. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Guadecitabine Related Classifications
HY-13542 Related Classifications
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