FIDAS-3

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

FIDAS-3  纯度: 99.12%

FIDAS-3 是一种二苯乙烯衍生物,也是一种强效的 Wnt 抑制剂,对甲硫氨酸腺苷转移酶 2A (MAT2A) 的 IC50 为 4.9 μM。FIDAS-3 与 S-腺苷甲硫氨酸 (SAM) 有效竞争 MAT2A 结合,并具有抗癌活性。

FIDAS-3

FIDAS-3 Chemical Structure

CAS No. : 1266684-01-8

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FIDAS-3 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Stem Cell Signaling Compound Library
  • Wnt/Hedgehog/Notch Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Differentiation Inducing Compound Library
  • Cytoskeleton Compound Library
  • Neuroprotective Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

FIDAS-3 is a stilbene derivative and is a potent Wnt inhibitor with an IC50 of 4.9 μM for methionine S-adenosyltransferase 2A (MAT2A). FIDAS-3 effectively competes against S-adenosylmethionine (SAM) for MAT2A binding. FIDAS-3 has anticancer activities[1][2].

IC50 & Target

IC50: 4.9 μM (Methionine S-adenosyltransferase 2A (MAT2A))[1]

体外研究
(In Vitro)

FIDAS-3 (3 μM; 7 days; LS174T cells) treatment significantly inhibits the proliferation of LS174T cells[1].
FIDAS-3 (3-10 μM) treatment inhibits the expression of c-Myc and cyclinD1 in LS174T CRC cells. And FIDAS-3 induces the expression of cell cycle inhibitor, p21WAF1/CIP1[1].
FIDAS-3 (10 μM; 36 h) treatment reduces the levels of both S-adenosylmethionine (SAM) and S-adenosylhomocysteine (SAH) in LS174T cells[1].

Shanghai Jinpan Biotech Co Ltd 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-3 (20 mg/kg; intraperitoneal injection; daily; for one months; C57BL/6J athymic nude mice) treatment significantly inhibits the growth of xenograft tumors[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J athymic nude mice (6-8 week) injected with LS174 cells[2]
Dosage: 20 mg/kg
Administration: Intraperitoneal injection; daily; for one months
Result: Significantly inhibited the growth of xenograft tumors.

分子量

259.29

Formula

C16H15F2N

CAS 号

1266684-01-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO : 100 mg/mL (385.67 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.8567 mL 19.2834 mL 38.5669 mL
5 mM 0.7713 mL 3.8567 mL 7.7134 mL
10 mM 0.3857 mL 1.9283 mL 3.8567 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;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

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: ≥ 2.5 mg/mL (9.64 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.64 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 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% corn oil

    Solubility: ≥ 2.5 mg/mL (9.64 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.64 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 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.

    [2]. Zhang W, et al. Fluorinated N,N-dialkylaminostilbenes for Wnt pathway inhibition and colon cancer repression. J Med Chem. 2011 Mar 10;54(5):1288-97.

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