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CAS No.: 1391934-98-7

FIDAS-5 Catalog No. CSN26788

FIDAS-5 is a potent and orally active methionine S-adenosyltransferase 2A (MAT2A) inhibitor with an IC50 of 2.1 μM. FIDAS-5 effectively competes against S-adenosylmethionine (SAM) for MAT2A binding. FIDAS-5 has anticancer activities[1].

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技术信息

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].
参考文献

[1] Ben Murray,et al. Methionine adenosyltransferases in liver cancer. World J Gastroenterol. 2019. 25(31), 4300-4319.
[2] A Katharina Weickhmann,et al. The structure of the SAM/SAH-binding riboswitch. Nucleic Acids Res. 2019. 47(5), 2654-2665.
[3] Lauren Y Maldonado, et al. Methionine adenosyltransferases in cancers: Mechanisms of dysregulation and implications for therapy. Exp Biol Med (Maywood). 2018. 243(2), 107-117.
[4] Zhang W, et al. Fluorinated N,N-dialkylaminostilbenes repress colon cancer by targeting methionine S-adenosyltransferase 2A. ACS Chem Biol. 2013. 8(4), 796-803.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.8209 mL
- 19.1043 mL
- 38.2085 mL
- 5 mM
- 0.7642 mL
- 3.8209 mL
- 7.6417 mL
- 10 mM
- 0.3821 mL
- 1.9104 mL
- 3.8209 mL

技术信息

CAS号	1391934-98-7	储存条件	粉末 Keep in dark place,Sealed in dry,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C15H13ClFN	运输	蓝冰
分子量	261.72	别名

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