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).
The free form of the compound is prone to instability, it is advisable to consider the stable salt form (Guadecitabine sodium) that retains the same biological activity.
For research use only. We do not sell to patients.
- CAS No.: 929901-49-5
- Formula: C18H24N9O10P
- Molecular Weight:557.41
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Storage:Powder -20°C, 3 years
* The compound is unstable in solutions, freshly prepared is recommended.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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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 Jul;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.
Customer Validation & Images
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Cell Proliferation/Viability Assay
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WB
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IF
All DNA Methyltransferase Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
DNA Methyltransferase |
In Vitro
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.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 929901-49-5
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Appearance Solid
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Molecular Weight 557.41
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
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 Jul;22(7):274-282. PMID: 32464274
Guadecitabine purchased from MedChemExpress. Usage Cited in: Neoplasia. 2020 Jul;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 Jul;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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Solvent & Solubility
In Vitro:
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
Purity & Documentation
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Data Sheet (275 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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Handling Instructions (2659 KB)
References
[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]
Guadecitabine Related Classifications
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