Formononetin
(Synonyms: 刺芒柄花素: Biochanin B: Flavosil; Formononetol) 目录号 : GN10527
Formononetin是一种强效的FGFR2抑制剂，其IC50值约为4.31μM。Formononetin能有效抑制血管生成和肿瘤生长。
Cas No.:485-72-3
Sample solution is provided at 25 µL, 10mM.
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Formononetin is a potent FGFR2 inhibitor with an IC50 of 4.3μM. Formononetin potently inhibits angiogenesis and tumor growth[1].
Formononetin (10, 80μM; 3d) inhibit Ishikawa, HEC-1A, and HEC-251 cells proliferation in a dose-dependent manner[2]. Formononetin (10, 25μM; 24h) is a potent protectant against cisplatin-induced cell death through inhibiting intracellular ROS accumulation in pig kidney epithelial LLC-PK1 cells[3]. Formononetin (0.1, 0.3, 1μM; 30-60min) increased CNE2 cell estrogen receptor-α (ERα) and bcl-2, but decreased protein-phosphatase and tensin homologue (PTEN) protein expression[4].
In mice hyperoxic acute lung injury, Formononetin (10, 100 mg/kg; ip; 72h) significantly attenuated hyperoxia-induced elevated lung water content, up-regulation of pro-inflammatory cytokine levels, and increased lung neutrophil infiltration[5]. In mice acute ischaemic injury model, formononetin (20mg/kg; po; 28d) promoted the expression of ER β and p53 in a dose-dependent manner[6].
References:
[1] Wu X Y, Xu H, Wu Z F, et al. Formononetin, a novel FGFR2 inhibitor, potently inhibits angiogenesis and tumor growth in preclinical models[J]. Oncotarget, 2015, 6(42): 44563.
[2]. Zhang Q, Huang X. The modulatory properties of Astragalus membranaceus treatment on endometrial cancer: an integrated pharmacological method[J]. PeerJ, 2021, 9: e11995.
[3] Lee H, Lee D, Kang K S, et al. Inhibition of intracellular ROS accumulation by Formononetin attenuates cisplatin-mediated apoptosis in LLC-PK1 cells[J]. International journal of molecular sciences, 2018, 19(3): 813.
[4] Guo Y H, Tang F Y, Wang Y, et al. Low concentration of Formononetin promotes proliferation of estrogen receptor-positive cells through an ERα-miR-375-PTEN-ERK1/2-bcl-2 pathway[J]. Oncotarget, 2017, 8(59): 100045.
[5]Chen Y, Wei D, Zhao J, et al. Reduction of hyperoxic acute lung injury in mice by Formononetin[J]. PloS one, 2021, 16(1): e0245050.
[6] Zhao L, Han J, Liu J, et al. A novel Formononetin derivative promotes anti-ischemic effects on acute ischemic injury in mice[J]. Frontiers in Microbiology, 2021, 12: 786464.
Formononetin是一种强效的FGFR2抑制剂，其IC50值约为4.31μM。Formononetin能有效抑制血管生成和肿瘤生长[1]。
Formononetin（10、80μM；3d）以剂量依赖的方式抑制Ishikawa，HEC-1A和HEC-251细胞的增殖[2]。Formononetin（10、25μM；24h）通过抑制猪肾上皮LLC-PK1细胞中细胞内ROS的积累，对顺铂诱导的细胞死亡具有有效的保护作用[3]。Formononetin（0.1、0.3、1μM；30-60min）可增加CNE2细胞中雌激素受体-α（ERα）和bcl-2的表达，但会降低蛋白磷酸酶和天丝同源物（PTEN）蛋白的表达[4]。
在小鼠高氧性急性肺损伤中，Formononetin（10、100mg/kg；ip；72h）显著减轻了高氧引起的肺水含量升高、促炎细胞因子水平上调和肺中性粒细胞浸润增加[5]。在小鼠急性缺血性损伤模型中，Formononetin（20mg/kg；po；28d）能以剂量依赖的方式促进ERβ和p53的表达[6]。
| Cell experiment [1]: | |
Cell lines | The Ishikawa, HEC-1A, and HEC-251 cell lines |
Preparation Method | The effect of Formononetin on the colony-forming ability of endometrial cancer cells was evaluated by colony formation assay. The Ishikawa, HEC-1A, and HEC-251 cell lines were seeded into 6-well plates at the concentration of 400 cells per well. After incubating for 24h at 37°C, the cells were incubated with Formononetin (40µM and 80µM). Three days later, most single colonies contain more than 50 cells. Cells were harvested and rinsed three times with distilled water, and images were obtained by a microscope. |
Reaction Conditions | 10, 80μM; 3d |
Applications | Formononetin inhibit Ishikawa, HEC-1A, and HEC-251 cells proliferation in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Hyperoxic acute lung injury Modle |
Preparation Method | Before the experiment, mice were housed in closed and individually ventilated cages under a 12h light:dark cycle for at least 1 week to acclimate to the environment. Mice had ad libitum access to standard chow and water. Mice were divided into a control group (room air+vehicle) and four other groups (room air+Formononetin, hyperoxia+vehicle, hyperoxia+Formononetin, and zinc protoporphyrin (ZnPP, an inhibitor of HO-1)+hyperoxia+Formononetin). To induce hyperoxic acute lung injury, mice were housed in closed cages and exposed to hyperoxia (>95% oxygen) for 72h. Room air exposure served as a control. |
Dosage form | 10, 100mg/kg; ip; 72h |
Applications | Formononetin pretreatment notably attenuated hyperoxia-induced elevating pulmonary water content, upregulation of proinflammatory cytokine levels and increasing infiltration of neutrophil in the lung. |
References: | |
| Cas No. | 485-72-3 | SDF | |
| 别名 | 刺芒柄花素: Biochanin B: Flavosil; Formononetol | ||
| 化学名 | 7-hydroxy-3-(4-methoxyphenyl)chromen-4-one | ||
| Canonical SMILES | COC1=CC=C(C=C1)C2=COC3=C(C2=O)C=CC(=C3)O | ||
| 分子式 | C16H12O4 | 分子量 | 268.27 |
| 溶解度 | DMF: 30 mg/ml,DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml,DMSO: 25 mg/ml | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.7276 mL | 18.6379 mL | 37.2759 mL |
| 5 mM | 0.7455 mL | 3.7276 mL | 7.4552 mL |
| 10 mM | 0.3728 mL | 1.8638 mL | 3.7276 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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1. 首先保证母液是澄清的；
2.
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Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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