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).
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
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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 | 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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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:
Purity & Documentation
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Data Sheet (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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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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Guadecitabine Related Classifications
HY-13542 Related Classifications
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