Nifuroxazide
(Synonyms: 硝呋齐特) 目录号 : GC14170
A nitrofuran antibiotic
Cas No.:965-52-6
Sample solution is provided at 25 µL, 10mM.
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Nifuroxazide is an effective inhibitor of STAT3, also exerts potent anti-tumor and anti-metastasis activity.
When U266 cells are incubated with Nifuroxazide, a significant dose-dependent decrease in STAT3 tyrosine phosphorylation is observed. This inhibition of STAT3 tyrosine phosphorylation is rapid, occurring as early as 1 h after treatment, and is sustained for at least 24 h. Treatment of U266 or INA6 cells with Nifuroxazide for 48 hours result in a dose-dependent loss of cell viability with an EC50 of approximately 4.5 μM in both cell types. Notably, the MM cells lacking constitutive STAT3 activation show little toxicity to Nifuroxazide[1].
Compared with the vehicle group, treatment with Nifuroxazide could inhibit tumor growth and tumor weight in a dose-dependent manner, with the inhibition rate of tumor volumes being 43.0% and 62.1% at 25 mg/kg and 50 mg/kg, respectively. It is also shown that Nifuroxazide significantly inhibits the proliferation of nuclear Ki-67-positive cells and induces apoptosis cells of cleaved caspase-3-positive cells. Besides, it is found that treatment with Nifuroxazide could inhibit the expression of MMP-2, MMP-9 and p-Stat3 in A375 tumor tissues. What’s more, Nifuroxazide inhibits the infiltration of MDSCs into the lung, which might be associated with suppression of distant colonization of tumor cells in B16-F10 melanoma metastasis model[2].
References:
[1]. Nelson EA, et al. Nifuroxazide inhibits survival of multiple myeloma cells by directly inhibiting STAT3. Blood. 2008 Dec 15;112(13):5095-102.
[2]. Zhu Y, et al. Nifuroxazide exerts potent anti-tumor and anti-metastasis activity in melanoma. Sci Rep. 2016 Feb 2;6:20253.
| Cell experiment [1]: | |
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Cell lines |
U266 myeloma cells |
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Preparation method |
The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
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Reacting condition |
0 ~ 10 μM; 0 ~ 24 hrs |
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Applications |
In U266 myeloma cells, Nifuroxazide significantly inhibited STAT3 tyrosine phosphorylation in a dose-dependent manner, with an IC50 value of 10 μM. The inhibitory effect of Nifuroxazide on STAT3 tyrosine phosphorylation was rapid, occurring as early as 1 hr after treatment and sustained for at least 24 hrs. In addition, Nifuroxazide did not affect STAT3 serine (727) phosphorylation. |
| Animal experiment [2]: | |
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Animal models |
4T1 tumor-bearing mice |
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Dosage form |
10 or 50 mg/kg; i.p.; q.d., for 24 days |
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Applications |
In 4T1 tumor-bearing mice, Nifuroxazide significantly reduced tumor outgrowth and tumor weight, without causing any significant change in body weight. The immunohistochemical staining results of 4T1 tumors collected on day 31 showed that Nifuroxazide substantially reduced Ki-67-positive cells and increased CC-3-positive cells, indicating that Nifuroxazide inhibited cell proliferation and induced apoptosis in breast tumor tissues by inhibiting Ki-67 and activating caspase-3. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Nelson EA, Walker SR, Kepich A, Gashin LB, Hideshima T, Ikeda H, Chauhan D, Anderson KC, Frank DA. Nifuroxazide inhibits survival of multiple myeloma cells by directly inhibiting STAT3. Blood. 2008 Dec 15;112(13):5095-102. [2]. Yang F, Hu M, Lei Q, Xia Y, Zhu Y, Song X, Li Y, Jie H, Liu C, Xiong Y, Zuo Z, Zeng A, Li Y, Yu L, Shen G, Wang D, Xie Y, Ye T, Wei Y. Nifuroxazide induces apoptosis and impairs pulmonary metastasis in breast cancer model. Cell Death Dis. 2015 Mar 26;6:e1701. | |
| Cas No. | 965-52-6 | SDF | |
| 别名 | 硝呋齐特 | ||
| 化学名 | 4-hydroxy-N-[(E)-(5-nitrofuran-2-yl)methylideneamino]benzamide | ||
| Canonical SMILES | C1=CC(=CC=C1C(=O)NN=CC2=CC=C(O2)[N+](=O)[O-])O | ||
| 分子式 | C12H9N3O5 | 分子量 | 275.22 |
| 溶解度 | ≥ 27.5mg/mL in DMSO | 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 3.6335 mL | 18.1673 mL | 36.3346 mL |
| 5 mM | 0.7267 mL | 3.6335 mL | 7.2669 mL |
| 10 mM | 0.3633 mL | 1.8167 mL | 3.6335 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 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 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % 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，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet