Home Methylation DNMT inhibitor Guadecitabine sodium

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Guadecitabine sodium DNMT inhibitor

Cat.No.S7013

Guadecitabine sodium(SGI-110 sodium; S-110 sodium) is a next-generation hypomethylating agent.
Guadecitabine sodium DNMT inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 579.39

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Quality Control

Batch: S701301 DMSO]100 mg/mL]false]Water]50 mg/mL]false]Ethanol]Insoluble]false Purity: 99.93%
99.93

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (172.59 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 50 mg/mL

Ethanol : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 579.39 Formula

C18 H23 N9 O10 P . Na

 Storage (From the date of receipt)
CAS No. 929904-85-8 -- Storage of Stock Solutions

Synonyms SGI-110 sodium; S-110 sodium SMILES C1C(C(OC1N2C=NC3=C2N=C(NC3=O)N)COP(=O)([O-])OC4CC(OC4CO)N5C=NC(=NC5=O)N)O.[Na+]

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Mechanism of Action

Targets/IC50/Ki
DNA methyltransferase
In vitro

Guadecitabine (SGI-110) is a 5-aza-2′-deoxycytidine-containing demethylating dinucleotide that works via a mechanism similar to that of 5-aza-CdR after incorporation of its aza-moiety into DNA. However, it is well protected from deamination by cytidine deaminase. This compound (1 μM) induces a significant decrease in the level of methylation in both T24 and HCT116 cells and is able to induce robust p16 expression. It also causes depletion of extractable DNMT1 in cells at 1 μM concentration. Furthermore, it decreases the plating efficiency of T24 bladder carcinoma cells in a dose-dependent manner, with no colonies forming at 10 μM concentration, which is quite similar to 5-aza-CdR in T24 cells.

It shows immunomodulatory activity in vitro. At 1 μM, it induces/up-regulates the expression of several cancer/testis antigens (CTA) (i.e., MAGE-A1, MAGE-A2, MAGE-A3, MAGE-A4, MAGE-A10, GAGE1-2, GAGE 1-6, NY-ESO-1, and SSX 1-5) in cancer cell lines (cutaneous melanoma, mesothelioma, renal cell carcinoma, and sarcoma cells), both at mRNA and at protein levels. This compound also up-regulates the expression of HLA class I antigens and of ICAM-1, resulting in improved recognition of cancer cells by gp100-specific CTL.

In vivo

Guadecitabine (SGI-110) is as effective as 5-Aza-CdR, but is better tolerated in mice. This compound (10 mg/kg) displays potent activity on inducing p16 expression, reducing DNA methylation at the p16 promoter region, and retarding tumor growth in human xenograft. It is effective by both i.p. and s.c. deliveries.

References
  • [4] https://pubmed.ncbi.nlm.nih.gov/31060979/
  • [5] https://pubmed.ncbi.nlm.nih.gov/35843958/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-08-05)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03220477 ACTIVE_NOT_RECRUITING
Lung Cancer
Memorial Sloan Kettering Cancer Center
 2017-08-04 PHASE1
NCT02935361 ACTIVE_NOT_RECRUITING
Chronic Myelomonocytic Leukemia; Myelodysplastic Syndrome; Recurrent Acute Myeloid Leukemia With Myelodysplasia-Related Changes
University of Southern California
 2016-11-02 PHASE1; PHASE2
NCT02998567 ACTIVE_NOT_RECRUITING
Non Small Cell Lung Cancer
Royal Marsden NHS Foundation Trust
 2017-01-26 PHASE1
NCT02684162 COMPLETED
Acute Myeloid Leukemia; Chronic Myelomonocytic Leukemia; Myelodysplastic Syndrome; Recurrent Acute Myeloid Leukemia; Recurrent Myelodysplastic Syndrome
M.D. Anderson Cancer Center
 2016-06-22 PHASE2
NCT02131597 COMPLETED
High Risk Myelodysplastic Syndrome
M.D. Anderson Cancer Center
 2014-11-10 PHASE2
NCT04340843 ACTIVE_NOT_RECRUITING
Locally Advanced Unresectable Primary Central Chondrosarcoma; Metastatic Primary Central Chondrosarcoma; Unresectable Primary Central Chondrosarcoma
National Cancer Institute (NCI)
 2020-09-08 PHASE2

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