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Guadecitabine sodium (Synonyms: SGI-110 sodium; S-110 sodium) 纯度: 97.10%
Guadecitabine sodium (SGI-110 sodium) 是第二代 DNA 甲基转移酶 (DNMT) 抑制剂,可用于急性髓细胞性白血病 (AML) 和骨髓增生异常综合症 (MDS) 的研究。
Guadecitabine sodium Chemical Structure
CAS No. : 929904-85-8
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2 mg | ¥4500 | In-stock | |
5 mg | ¥8500 | In-stock | |
10 mg | ¥12000 | In-stock | |
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100 mg | 询价 |
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Guadecitabine sodium 相关产品
•相关化合物库:
- Drug Repurposing Compound Library Plus
- Clinical Compound Library Plus
- Bioactive Compound Library Plus
生物活性 |
Guadecitabine sodium (SGI-110 sodium) is a second-generation DNA methyltransferases (DNMT) inhibitor for research of acute myeloid leukemia (AML) and myelodysplastic syndromes (MDS)[1]. |
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IC50 & Target[1] |
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体外研究 (In Vitro) |
After HCT116 colorectal carcinoma cells are treated for 6 days, a dose-dependent increase in p16expression is observed with Guadecitabine sodium (SGI-110 sodium). In addition, T24 and HCT116 cells treated with Guadecitabine sodium or 5-aza-CdR for 3 days show a dose-dependent increase in the level of p16 protein, showing the competence of Guadecitabine sodium to inhibit DNA methylation and induce p16 at both mRNA and protein levels as well as 5-aza-CdR. Thus, Guadecitabine sodium is able to inhibit DNA methylation at 5′-region and induce the expression of the p16 gene in T24 and HCT116 cells at concentrations comparable to 5-aza-CdR, and the induction of p16 expression by both agents correlates with the demethylation at the 5′-end region of the gene in both cell lines. Guadecitabine sodium is slightly less toxic than 5-aza-CdR at the doses tested up to 1 μM concentration but displaying similar toxicity at 10 μM concentration[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 (In Vivo) |
Guadecitabine sodium (SGI-110 sodium) at 10mg/kg is an effective dose at reducing DNA methylation and retarding tumor growth, and caused roughly the same level of toxicity as 5-Aza-CdR. Guadecitabine sodium is effective in vivo at reactivating the expression of the p16 gene, which is heavily methylated in the parent EJ6 cells. Guadecitabine sodium is effective in reducing the level of DNA methylation in vivo at the p16 promoter region. Guadecitabine sodium is better tolerated than 5-Aza-CdR in vivo, suggesting that it can be an attractive alternative for potential clinical use[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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Clinical Trial |
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分子量 |
579.39 |
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Formula |
C18H23N9NaO10P |
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CAS 号 |
929904-85-8 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
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溶解性数据 |
In Vitro:
DMSO : 50 mg/mL (86.30 mM; Need ultrasonic) H2O : 50 mg/mL (86.30 mM; Need ultrasonic and warming) 配制储备液
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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。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
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参考文献 |
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Cell Assay [1] |
T24 cells are plated at a low density (100 per 60-mm dish) and treated with varying concentrations of 5-aza-CdR and S-110 (0.1, 0.2, 10 μM. Colonies are allowed to form for 10 to 14 days, fixed with methanol, and stained with 10% Giemsa. The number of colonies from an untreated control plate is used to calculate the plating efficiency in percent at each concentration. Triplicate dishes are used, and error bars are represented by 1 SD of the mean[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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Animal Administration [2] |
Mouse: Athymic nu/nu mice are inoculated subcutaneously 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 received molar equivalents of either S-110 or 5-Aza-CdR. The agents are administered SQ once weekly at a dose of 12.2 mg/kg for S-110 and 5.0 mg/kg for 5-Aza-CdR 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[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
参考文献 |
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