产品说明书
FIDAS-5
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同义名 : | - |
| CAS号 : | 1391934-98-7 | |
| 货号 : | A1328405 | |
| 分子式 : | C15H13ClFN | |
| 纯度 : | 98%+ | |
| 分子量 : | 261.722 | |
| MDL号 : | MFCD32671894 | |
| 存储条件： |
粉末 Keep in dark place,Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 120 mg/mL(458.5 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Methionine adenosyltransferases (MATs) are essential enzymes for life as they produce S-adenosylmethionine (SAMe), the biological methyl donor required for a plethora of reactions within the cell[1]. S-adenosylmethionine (SAM) is a central metabolite since it is used as a methyl group donor in many different biochemical reactions[2]. Induction of MAT2A/MAT2B confers growth and survival advantage to cancerous cells, enhancing tumor migration[3]. FIDAS-5 is a potent and orally active methionine S-adenosyltransferase 2A (MAT2A) inhibitor with an IC50 of 2.1 μM. It effectively competes against S-adenosylmethionine (SAM) for MAT2A binding. FIDAS-5 shows anticancer activities. It induces the expression of p21WAF1/CIP1, a cell cycle inhibitor， after 36-hour treatment at 3 μM with both reduced level of SAM and SAH observed in LS174T cells. 7-day treatment with FIDAS-5 at 3 μM significantly inhibits the proliferation of LS174T cells, accompanied with reduced expression of c-Myc and cyclinD1. The liver SAM levels are significantly reduced in mice treated with FIDAS-5 at dose of 20 mg/kg for 1 week. Treatment with FIDAS-5 at 20 mg/kg, p.o., daily, for 2 weeks, significantly inhibits the growth of xenograft tumors of athymic nude mice, without obvious difference in body weight[4]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
3.82mL 0.76mL 0.38mL |
19.10mL 3.82mL 1.91mL |
38.21mL 7.64mL 3.82mL |
| 参考文献 |
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