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Guadecitabine sodium

Catalog No. T12790   CAS 929904-85-8
Synonyms: SGI-110 sodium, S-110 sodium

Guadecitabine sodium is a inhibitor of second-generation DNA methyltransferases (DNMT) .

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Guadecitabine sodium Chemical Structure
Guadecitabine sodium, CAS 929904-85-8
Pack Size Availability Price/USD Quantity
25 mg 6-8 weeks $ 1,670.00
50 mg 6-8 weeks $ 2,180.00
100 mg 6-8 weeks $ 2,800.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Guadecitabine sodium is a inhibitor of second-generation DNA methyltransferases (DNMT) .
In vitro HCT116 colorectal carcinoma cells are treated After 6 days, in p16expression is observed with Guadecitabine sodium (SGI-110 sodium) show a dose-dependent increase . In addition, a dose-dependent increase in the level of p16 protein in T24 and HCT116 cells treated with Guadecitabine sodium or 5-aza-CdR for 3 days, showing the competence of Guadecitabine sodium to inhibit DNA methylation and induce p16 at both mRNA and protein levels as well as 5-aza-CdR. Thus, Guadecitabine sodium is able to inhibit DNA methylation at 5′-region and induce the expression of the p16 gene in T24 and HCT116 cells at concentrations comparable to 5-aza-CdR, and the induction of p16 expression by both agents correlates with the demethylation at the 5′-end region of the gene in both cell lines. Guadecitabine sodium is slightly less toxic than 5-aza-CdR at the doses tested up to 1 μM concentration but displaying similar toxicity at 10 μM concentration[1].
In vivo Guadecitabine sodium(10mg/kg )is an effective dose at reducing DNA methylation and retarding tumor growth, and caused roughly the same level of toxicity as 5-Aza-CdR. Guadecitabine sodium is effective in vivo at reactivating the expression of the p16 gene, which is heavily methylated in the parent EJ6 cells. Guadecitabine sodium is effective in reducing the level of DNA methylation in vivo at the p16 promoter region. Guadecitabine sodium is better tolerated than 5-Aza-CdR in vivo[2].
Synonyms SGI-110 sodium, S-110 sodium
Molecular Weight 580.407
Formula C18H24N9NaO10P
CAS No. 929904-85-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (86.30 mM), sonification is recommended.

H2O: Soluble

TargetMolReferences and Literature

1. Yoo CB, et al. Delivery of 5-aza-2'-deoxycytidine to cells using oligodeoxynucleotides. Cancer Res. 2007 Jul 1;67(13):6400-8. 2. Chuang JC, et al. S-110, 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.

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Keywords

Guadecitabine sodium 929904-85-8 Chromatin/Epigenetic DNA Methyltransferase SGI-110 sodium S-110 sodium inhibitor inhibit

 

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