Formononetin(Synonyms: 刺芒柄花素; Biochanin B; Flavosil; Formononetol)

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Formononetin (Synonyms: 刺芒柄花素; Biochanin B; Flavosil; Formononetol) 纯度: 99.88%

Formononetin 是一种有效的 FGFR2 抑制剂,IC50 为 ~4.31 μM。 Formononetin 有效抑制血管生成和肿瘤生长。

Formononetin(Synonyms: 刺芒柄花素; Biochanin B;  Flavosil;  Formononetol)

Formononetin Chemical Structure

CAS No. : 485-72-3

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生物活性

Formononetin is a potent FGFR2 inhibitor with an IC50 of ~4.31 μM. Formononetin potently inhibits angiogenesis and tumor growth[1].

IC50 & Target[1]

FGFR2

4.31 μM (IC50)

体外研究
(In Vitro)

Formononetin is one of the major isoflavonoid constituents isolated from Astragalus membranaceus and has been demonstrated diverse pharmacological benefits. Formononetin possesses anti-angiogenic activity in human colon cancer cells. Formononetin also promotes cell cycle arrest via downregulation of Akt/Cyclin D1/CDK4 in human prostate cancer cells[1].
Formononetin (25 to 150 μM) markedly decreases the proliferation of endothelial cells stimulated by FGF2[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: HUVECs
Concentration: 0, 10, 25, 50, 75, 100, and 150 μM
Incubation Time:
Result: Significantly decreased the proliferation of HUVECs stimulated by FGF2 in a dose-dependent manner, while had little inhibitory effects on HUVECs that were not stimulated by FGF2.

体内研究
(In Vivo)

Formononetin dramatically suppresses tumor volumes and the Formononetin-treated group tumor weight are significantly inhibited compared with the vehicle group . Formononetin treatment is well tolerated, and there is no significant difference in weight between vehicle group and formononetin treated groups[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: BALB/c nude mice bearing MDA-MB-231 xenografts[1]
Dosage: 100 mg/kg
Administration: Treated daily by intragastric administration for 25 days
Result: Inhibited breast cancer growth and angiogenesis in vivo.

分子量

268.26

Formula

C16H12O4

CAS 号

485-72-3

中文名称

刺芒柄花素;生原禅宁 B;素普拉脑

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
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 35 mg/mL (130.47 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.7277 mL 18.6386 mL 37.2773 mL
5 mM 0.7455 mL 3.7277 mL 7.4555 mL
10 mM 0.3728 mL 1.8639 mL 3.7277 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。-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 (9.32 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (9.32 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    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% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (9.32 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (9.32 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    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 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
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (9.32 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.32 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 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Xiao Yu Wu,et al. Formononetin, a novel FGFR2 inhibitor, potently inhibits angiogenesis and tumor growth in preclinical models. Oncotarget. 2015 Dec 29;6(42):44563-78.

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