1. Epigenetics
  2. DNA Methyltransferase
  3. Guadecitabine

Guadecitabine (Synonyms: SGI-110)

Cat. No.: HY-13542 Purity: 98.00%
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Guadecitabine (SGI-110) is a DNA methyltransferases (DNMT) inhibitor.

For research use only. We do not sell to patients.

Guadecitabine Chemical Structure

Guadecitabine Chemical Structure

CAS No. : 929901-49-5

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Description

Guadecitabine (SGI-110) is a DNA methyltransferases (DNMT) inhibitor.

IC50 & Target

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].

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].

Clinical Trial
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

H2O

References
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
Molecular Weight

557.41

Formula

C₁₈H₂₄N₉O₁₀P

CAS No.

929901-49-5

SMILES

O=C1C2=C(N([[email protected]]3C[[email protected]](O)[[email protected]@H](COP(O)(O[[email protected]@H]4[[email protected]@H](CO)O[[email protected]@H](N5C=NC(N)=NC5=O)C4)=O)O3)C=N2)NC(N)=N1

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Guadecitabine
Cat. No.:
HY-13542
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Guadecitabine

Cat. No.: HY-13542