FIDAS-5

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FIDAS-5  纯度: 98.10%

FIDAS-5 是一种有效的口服活性的甲硫氨酸腺苷转移酶 2A (MAT2A) 抑制剂，IC50 为 2.1 μM。FIDAS-5 与 S-腺苷甲硫氨酸 (SAM) 有效竞争 MAT2A 结合，并具有抗癌活性。

FIDAS-5

FIDAS-5 Chemical Structure

CAS No. : 1391934-98-7

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FIDAS-5 相关产品

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生物活性

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].

IC50 & Target

IC50: 2.1 μM (Methionine S-adenosyltransferase 2A (MAT2A))[1]
体外研究
(In Vitro)

FIDAS-5 (3 μM; 7 days; LS174T cells) treatment significantly inhibits the proliferation of LS174T cells[1].
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[1].
FIDAS-5 (3 μM; 36 h) treatment reduces the levels of both S-adenosylmethionine (SAM) and S-adenosylhomocysteine (SAH) in LS174T cells[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.

Cell Viability Assay[1]

Cell Line: LS174T colorectal cancer (CRC) cells
Concentration: 3 μM
Incubation Time: 7 days
Result: Significantly inhibited the proliferation of LS174T cells.

体内研究
(In Vivo)

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[1].
Mice are treated with FIDAS-5 (20 mg/kg) for 1 week. The liver SAM levels are significantly reduced[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.

Animal Model: 16 athymic nude mice injected with HT29 CRC cells[1]
Dosage: 20 mg/kg
Administration: Oral gavage; daily; for two weeks
Result: Significantly inhibited the growth of xenograft tumors.

分子量

261.72

Formula

C15H13ClFN
CAS 号

1391934-98-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years

*该产品在溶液状态不稳定，建议您现用现配，即刻使用。
溶解性数据
In Vitro: 

DMSO : 125 mg/mL (477.61 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.8209 mL 19.1044 mL 38.2088 mL
5 mM 0.7642 mL 3.8209 mL 7.6418 mL
10 mM 0.3821 mL 1.9104 mL 3.8209 mL

*

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；该产品在溶液状态不稳定，建议您现用现配，即刻使用。

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
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (7.95 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (7.95 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (7.95 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (7.95 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
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.

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