| 产品描述: | 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 |
| 靶点: |
IC50: 2.1 μM (Methionine S-adenosyltransferase 2A (MAT2A)) |
| 体外研究: |
FIDAS-5 (3 μM; 7 days; LS174T cells) treatment significantly inhibits the proliferation of LS174T cells.
FIDAS-5 (3 μM) treatment inhibits the expression of c-Myc and cyclinD1 in LS174T CRC cells. And FIDAS-5 induces the expression of cell cycle inhibitor, p21WAF1/CIP1.
FIDAS-5 (3 μM; 36 h) treatment reduces the levels of both S-adenosylmethionine (SAM) and S-adenosylhomocysteine (SAH) in LS174T cells. |
| 体内研究: |
FIDAS-5 (20 mg/kg; oral gavage; daily; for two weeks; athymic nude mice) treatment significantly inhibits the growth of xenograft tumors, with minimal difference in body weight. Mice are treated with FIDAS-5 (20 mg/kg) for 1 week. The liver SAM levels are significantly reduced. Animal Model: 16 athymic nude mice injected with HT29 CRC cells Dosage: 20 mg/kg Administration: Oral gavage; daily; for two weeks Result: Significantly inhibited the growth of xenograft tumors. |
| 参考文献: |
1. Zhang W, et al. Fluorinated N,N-dialkylaminostilbenes repress colon cancer by targeting methionine S-adenosyltransferase 2A. ACS Chem Biol. 2013 Apr 19;8(4):796-803. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 备注: |
1. Zhang W, et al. Fluorinated N,N-dialkylaminostilbenes repress colon cancer by targeting methionine S-adenosyltransferase 2A. ACS Chem Biol. 2013 Apr 19;8(4):796-803. |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
3.821 ml |
19.104 ml |
38.209 ml |
| 5 mM |
0.764 ml |
3.821 ml |
7.642 ml |
| 10 mM |
0.382 ml |
1.91 ml |
3.821 ml |
| 50 mM |
0.076 ml |
0.382 ml |
0.764 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |