| 5-fluoro 203AhR signaling activator |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
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- Purity = 98.00%
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| Cas No. | 260443-89-8 | SDF | Download SDF |
| Synonyms | 5F-203,NSC 703786 | ||
| Chemical Name | 4-(5-fluoro-2-benzothiazolyl)-2-methyl-benzenamine | ||
| Canonical SMILES | FC1=CC=C(SC(C2=CC=C(N)C(C)=C2)=N3)C3=C1 | ||
| Formula | C14H11FN2S | M.Wt | 258.3 |
| Solubility | ≤2mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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.
