5-fluoro 203
(Synonyms: 4-(5-氟-1,3-苯并噻唑-2-基)-2-甲基苯胺,5F-203,NSC 703786) 目录号 : GC12209
An AhR and CYP1A1 activator
Cas No.:260443-89-8
Sample solution is provided at 25 µL, 10mM.
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5-fluoro 203 (5F-203) is an antitumor agent and cytotoxic compound that acts as a potent AhR agonist [1][2][3].
The aryl hydrocarbon receptor (AhR) is a ligand-activated transcription factor involved in regulating xenobiotic-metabolizing enzymes such as cytochrome P450.
5-fluoro 203 (5F-203) is an antitumor agent that acts as a potent AhR agonist. In MCF-7 breast cancer cell, 5-fluoro 203 inhibited cell growth in part by activating the aryl hydrocarbon receptor (AhR) signaling pathway. 5-fluoro 203 increased protein-DNA complex formation on the NF-kB-responsive element and also increased NF-kB-dependent transcriptional activity [1]. In sensitive MCF-7 cells, 1.0 μM 5F-203 induced CYP1A1 gene expression [2]. In IGROV-1 cells, 5F203 induced enhanced CYP1A1 expression, AhR translocation and ROS formation, accompanied by JNK, ERK and P38 MAPK phosphorylation, DNA damage and cell cycle arres. In cells isolated from ovarian cancer ascites, 5F203 also induced CYP1A1 expression, AhR translocation and ROS formation [3].
In nude mice bearing human tumor xenografts, 5F-203 induced CYP1A1 gene expression, which was correlated with in vivo sensitivity. Therefore, induction of CYP1A1 mRNA in response to 5F-203 treatments may provide a possible surrogate marker for determination of drug-sensitive tumors in patients [2].
References:
[1]. Brantley E, Patel V, Stinson SF, et al. The antitumor drug candidate 2-(4-amino-3-methylphenyl)-5-fluorobenzothiazole induces NF-kappaB activity in drug-sensitive MCF-7 cells. Anticancer Drugs. 2005 Feb;16(2):137-43.
[2]. Hose CD, Hollingshead M, Sausville EA, et al. Induction of CYP1A1 in tumor cells by the antitumor agent 2-[4-amino-3-methylphenyl]-5-fluoro-benzothiazole: a potential surrogate marker for patient sensitivity. Mol Cancer Ther. 2003 Dec;2(12):1265-72.
[3]. Callero MA, Luzzani GA, De Dios DO, et al. Biomarkers of sensitivity to potent and selective antitumor 2-(4-amino-3-methylphenyl)-5-fluorobenzothiazole (5F203) in ovarian cancer. J Cell Biochem. 2013 Oct;114(10):2392-404.
| Cas No. | 260443-89-8 | SDF | |
| 别名 | 4-(5-氟-1,3-苯并噻唑-2-基)-2-甲基苯胺,5F-203,NSC 703786 | ||
| 化学名 | 4-(5-fluoro-2-benzothiazolyl)-2-methyl-benzenamine | ||
| Canonical SMILES | FC1=CC=C(SC(C2=CC=C(N)C(C)=C2)=N3)C3=C1 | ||
| 分子式 | C14H11FN2S | 分子量 | 258.3 |
| 溶解度 | ≤2mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | 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 | 3.8715 mL | 19.3573 mL | 38.7147 mL |
| 5 mM | 0.7743 mL | 3.8715 mL | 7.7429 mL |
| 10 mM | 0.3871 mL | 1.9357 mL | 3.8715 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet