Guadecitabine (Synonyms: SGI-110)

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Data Sheet SDS COA Handling Instructions

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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.

Guadecitabine Chemical Structure

CAS No. : 929901-49-5

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8 Publications Citing Use of MCE Guadecitabine

Cell Viability Assay

: 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.

: 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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Biological Activity
Protocol
Purity & Documentation
References
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Description

Guadecitabine (SGI-110) is a second-generation DNA methyltransferases (DNMT) inhibitor for research of acute myeloid leukemia (AML) and myelodysplastic syndromes (MDS)^[1].

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

Guadecitabine (S110) is effective at retarding tumor growth. While the tumors do not shrink in size with Guadecitabine treatment, they experience very minimal growth while the tumors treated with PBS only show substantial growth. In addition, Guadecitabine induces much less toxicity as determined by mouse weight changes when given subcutaneously (SQ) compare to that with IP injections^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

557.41

Formula

C₁₈H₂₄N₉O₁₀P

CAS No.

929901-49-5

Appearance

Solid

Color

White to off-white

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years

*The compound is unstable in solutions, freshly prepared is recommended.

Solvent & Solubility

In Vitro:

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 98.0%

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Data Sheet (274 KB) SDS (252 KB)

COA (247 KB) HNMR (243 KB) RP-HPLC (379 KB)

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]

Cell Assay ^[2]	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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[3]	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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Guadecitabine929901-49-5SGI-110SGI110SGI 110DNA MethyltransferaseDNMTsDNA MTasesInhibitorinhibitorinhibit

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