Antibodies
SGI-110
- 貨號 Cat. No.
- S7013
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
SGI-110
Catalog No.S7013
SGI-110 (S-110) is a stable and potent inhibitor for DNA methylation, inhibits DNMT1 when SGI-110 is activated by phosphorylation and incorporated into DNA. Phase 2.
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Biological Activity
| Description | SGI-110 (S-110) is a stable and potent inhibitor for DNA methylation, inhibits DNMT1 when SGI-110 is activated by phosphorylation and incorporated into DNA. Phase 2. | |||||
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| Targets | ||||||
| IC50 | ||||||
| In vitro | SGI-110 is a 5-aza-2’-deoxycytidine-containing demethylating dinucleotide, which works via a mechanism similar to that of 5-aza-CdR after incorporation of its aza-moiety into DNA. However, SGI-110 is well protected from deamination by cytidine deaminase. SGI-110 (1 μM) induces significantly decrease in the level of methylation in both T24 and HCT116 cells. SGI-110 is able to induce robust p16 expression. SGI-110 (1 μM) causes depletion of extractable DNMT1 in cells. SGI-110 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. [1] SGI-110 shows immunomodulatory activity in vitro. SGI-110 (1 μM) induces/up-regulates the expression of several cancer/testis antigens (CTA) (i.e., MAGE-A1, MAGE-A2, MAGE-A3, MAGE-A4, MAGE-A10, GAGE 1-2, 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. SGI-110 also up-regulates the expression of HLA class I antigens and of ICAM-1, resulting in an improved recognition of cancer cells by gp100-specific CTL. [2] | |||||
| In vivo | SGI-110 is as effective as 5-Aza-CdR, but is better tolerated in mice. SGI-110 (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. SGI-110 is effective by both i.p. and s.c. deliveries. [3] | |||||
| Features | ||||||
Protocol(Only for Reference)
Animal Study: [3]
| Animal Models | Human bladder cancers xenografts EJ6 |
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| Dosages | 10 mg/kg |
| Administration | i.p. or s.c. |
References
Clinical Trial Information( data from http://clinicaltrials.gov)
| NCT Number | Recruitment | Conditions | Sponsor /Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT01261312 | Recruiting | MDS|CMML|AML | Astex Pharmaceuticals | 2010-12 | Phase 1|Phase 2 |
| NCT01696032 | Recruiting | Ovarian Cancer | Astex Pharmaceuticals | 2012-09 | Phase 1|Phase 2 |
| NCT01752933 | Recruiting | Hepatocellular Carcinoma | Astex Pharmaceuticals | 2012-12 | Phase 2 |
Chemical Information
| Molecular Weight (MW) | 579.39 |
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| Formula | C18H23N9NaO10P |
| CAS No. | 929901-49-5 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | mg/mL (<1 mM) |
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| Water | mg/mL (<1 mM) | ||
| Ethanol | mg/mL (<1 mM) | ||
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. | |||
| Chemical Name | Guanosine, 2’-deoxy-5-azacytidylyl-(3’→5’)-2’-deoxy- |
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