GlpBio

SGI-110

目录号: GC17428纯度: >98%同义词: SGI-110
COASDSData Sheet
SGI-110 (SGI-110) 是第二代 DNA 甲基转移酶 (DNMT) 抑制剂，用于研究急性髓性白血病 (AML) 和骨髓增生异常综合征 (MDS)。
SGI-110
Cas No.: 929901-49-5
规格价格库存数量操作
2mg¥4,253.00现货
1
5mg¥8,033.00现货
1
10mg¥11,340.00现货
1
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文献被引

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    31, 1291–1307 (2021)

产品描述 Description

SGI-110 is a second generation DNA methyltransferase (DNMT) inhibitor that is synthesized as a dinucleotide consisting of a deoxyguanosine (5’-DACpG-3’) and 5-AZA-CdR bonds with a natural phosphodiester linkage. Unlike other DNMT inhibitors that are susceptible to rapid inactivation by cytidine deaminase (CDA), SGI-110 is highly resistant to deamination by CDA. In previous studies, SGI-110 has been demonstrated to effectively retard tumor growth in human bladder cancer xenografts through both intraperitoneal (i.p.) and subcutaneous (s.c.) administration and to exhibit epigenetic remodeling activity, in which the expression of p16 in cancer cells is restored through demethylation of the 5’-end region of the gene.

References:
[1]Tellez CS1, Grimes MJ, Picchi MA, Liu Y, March TH, Reed MD, Oganesian A, Taverna P, Belinsky SA. SGI-110 and entinostat therapy reduces lung tumor burden and reprograms the epigenome. Int J Cancer. 2014 Mar 26. doi: 10.1002/ijc.28865. [Epub ahead of print]
[2]Coral S1, Parisi G, Nicolay HJ, Colizzi F, Danielli R, Fratta E, Covre A, Taverna P, Sigalotti L, Maio M. Immunomodulatory activity of SGI-110, a 5-aza-2'-deoxycytidine-containing demethylating dinucleotide. Cancer Immunol Immunother. 2013 Mar;62(3):605-14. doi: 10.1007/s00262-012-1365-7. Epub 2012 Nov 9.
[3]Foulks JM1, Parnell KM, Nix RN, Chau S, Swierczek K, Saunders M, Wright K, Hendrickson TF, Ho KK, McCullar MV, Kanner SB. Epigenetic drug discovery: targeting DNA methyltransferases. J Biomol Screen. 2012 Jan;17(1):2-17. doi: 10.1177/1087057111421212. Epub 2011 Sep 30.

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

Parental A2780 cells and A2780-CDDP resistant cells

Preparation method

This compound is soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

0.1, 0.3, 1 or 5 μM; 48 hrs

Applications

At the moderate dose of 5 μM, SGI-110 increased the sensitivity of OC cells to CDDP, resulting in a > 2-fold reduction in the IC50 for CDDP: 28 μM CDDP IC50 for A2780-CDDP resistant cells and 42 μM CDDP IC50 for parental A2780 cells. SGI-110 increased the sensitivity of both the parental and the resistant A2780 cells to CDDP. It was demonstrated that SGI-110 chemosensitized the A2780 cells by demethylation and reexpression of MLH1, RASSF1A and HOXA11.
Animal experiment [2]:

Animal models

Nude rats bearing Calu6 cells

Dosage form

20 mg/kg; s.c.; twice per week, for 4 weeks

Applications

In nude rats bearing Calu6 cells, SGI-110 alone reduced tumor burden by 35%, and the combination treatment with SGI-110 ﹢ Entinostat significantly reduced tumor burden by 56%. Besides, SGI-110 alone or in combination with Entinostat decreased the pleomorphic cell population similarly, to approximately 25%. However, compared with the control group, these 2 treatment groups showed some cumulative toxicity. After 4 weeks of treatment, body weights of rats reduced by 13 ~ 18%.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Fang F, Munck J, Tang J, Taverna P, Wang Y, Miller DF, Pilrose J, Choy G, Azab M, Pawelczak KS, VanderVere-Carozza P, Wagner M, Lyons J, Matei D, Turchi JJ, Nephew KP. The novel, small-molecule DNA methylation inhibitor SGI-110 as an ovarian cancer chemosensitizer. Clin Cancer Res. 2014 Dec 15;20(24):6504-16.

[2]. Tellez CS1, Grimes MJ, Picchi MA, Liu Y, March TH, Reed MD, Oganesian A, Taverna P, Belinsky SA. SGI-110 and entinostat therapy reduces lung tumor burden and reprograms the epigenome. Int J Cancer. 2014 Mar 26.

产品文档 Product Documents

Purity:>98%
COASDSData Sheet

化学性质Chemical Properties

CAS 号
929901-49-5
同义词
SGI-110
化学名
[(2S,3R,5R)-5-(2-amino-6-oxo-3H-purin-9-yl)-3-hydroxyoxolan-2-yl]methyl [5-(4-amino-2-oxo-1,3,5-triazin-1-yl)-2-(hydroxymethyl)oxolan-3-yl] hydrogen phosphate
SMILES
C1C(C(OC1N2C=NC3=C2NC(=NC3=O)N)COP(=O)(O)OC4CC(OC4CO)N5C=NC(=NC5=O)N)O
分子式
C18H24N9O10P
分子量
557.41 g/mol
溶解性
DMSO : 50 mg/mL (86.30 mM); Water
保存条件
Store at -20°C,unstable in solution, ready to use.
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol