SGI-110
(Synonyms: SGI-110) 目录号 : GC17428
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)。
Cas No.:929901-49-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
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Cell lines |
Parental A2780 cells and A2780-CDDP resistant cells |
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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. |
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Reacting condition |
0.1, 0.3, 1 or 5 μM; 48 hrs |
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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]: | |
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Animal models |
Nude rats bearing Calu6 cells |
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Dosage form |
20 mg/kg; s.c.; twice per week, for 4 weeks |
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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%. |
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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. |
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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. | |
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.
| Cas No. | 929901-49-5 | SDF | |
| 别名 | 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 | ||
| Canonical 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 |
| 溶解度 | DMSO : 50 mg/mL (86.30 mM); Water | 储存条件 | 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℃，然后在超声波浴中震荡一段时间。 |
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| 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。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.794 mL | 8.9701 mL | 17.9401 mL |
| 5 mM | 0.3588 mL | 1.794 mL | 3.588 mL |
| 10 mM | 0.1794 mL | 0.897 mL | 1.794 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。