5F-203 (NSC-703786) is a cytotoxic molecule that forms DNA adducts and causes cell cycle arrest. 5F-203 induces aryl hydrocarbon receptor (AhR) signaling and increases CYP1A1 expression. 5F-203 also increases reactive oxygen species levels and activates JNK, ERK, and p38.

Physicochemical Properties

Molecular Formula	C14H11N2FS
Molecular Weight	258.31394
Exact Mass	258.063
CAS #	260443-89-8
PubChem CID	396813
Appearance	Off-white to light yellow solid powder
LogP	4.574
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	4
Rotatable Bond Count	1
Heavy Atom Count	18
Complexity	302
Defined Atom Stereocenter Count	0
InChi Key	IFWLHIIUGSEKKE-UHFFFAOYSA-N
InChi Code	InChI=1S/C14H11FN2S/c1-8-6-9(2-4-11(8)16)14-17-12-7-10(15)3-5-13(12)18-14/h2-7H,16H2,1H3
Chemical Name	4-(5-fluoro-1,3-benzothiazol-2-yl)-2-methylaniline
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

References

[1]. Antitumor benzothiazoles. 16. Synthesis and pharmaceutical properties of antitumor 2-(4-aminophenyl)benzothiazole amino acid prodrugs. J Med Chem. 2002 Jan 31;45(3):744-7. [2]. 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]. 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.

Solubility Data

Solubility (In Vitro)

DMSO : ~100 mg/mL (~387.13 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (9.68 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	3.8713 mL	19.3566 mL	38.7132 mL
	5 mM	0.7743 mL	3.8713 mL	7.7426 mL
	10 mM	0.3871 mL	1.9357 mL	3.8713 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.