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Description: Prodrug of the antitumor agent 5F 203
Chemical Name: (2S)-2,6-Diamino-N-[4-(5-fluoro-2-benzothiazolyl)-2-methylphenyl]hexanamide dihydrochloride
Purity: ≥98% (HPLC)

Biological Activity for Phortress

Phortress is a prodrug of the antitumor agent 5F 203, which acts via binding to aryl hydrocarbon receptors. Induces expression of CYP1A1 and generates adducts in the DNA of sensitive MCF7 and IGROV-1 cells.

Technical Data for Phortress

M. Wt 459.41
Formula C20H23FN4OS.2HCl
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 328087-38-3
PubChem ID 9804228
Smiles FC1=CC=C2C(N=C(C3=CC=C(NC([C@H](CCCCN)N)=O)C(C)=C3)S2)=C1.Cl.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Phortress

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 100

Preparing Stock Solutions for Phortress

The following data is based on the product molecular weight 459.41. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.18 mL 10.88 mL 21.77 mL
5 mM 0.44 mL 2.18 mL 4.35 mL
10 mM 0.22 mL 1.09 mL 2.18 mL
50 mM 0.04 mL 0.22 mL 0.44 mL

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References for Phortress

References are publications that support the biological activity of the product.

Leong et al (2003) Antitumour 2-(4-aminophenyl)benzothiazoles generate DNA adducts in sensitive tumour cells in vitro and in vivo. Br.J.Cancer 88 470 PMID: 12569393

Leong et al (2004) In vitro, in vivo and in silico analyses of the antitumor activity of 2(-4-amino-3-methylphenyl)-5-fluorobenzothiazoles. Mol.Cancer Ther. 3 1565 PMID: 15634650

Trapani et al (2003) DNA damage and cell cycle arrest induced by 2-(4-amino-3-methylphenyl)-5-fluorobenzothiazole (5F 203, NSC 703786) is attenuated by aryl hydrocarbon receptor deficient MCF-7 cells. Br.J.Cancer 88 599 PMID: 12592376

Bradshaw and Westwell (2004) The development of the antitumour benzothiazole prodrug, phortress, as a clinical candidate. Curr.Med.Chem. 11 1241 PMID: 15078163

If you know of a relevant reference for Phortress, please let us know.

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Keywords: Phortress, Phortress supplier, antitumor, antitumour, cytotoxic, prodrug, aryl, hydrocarbon, receptors, AhRs, Aryl, Hydrocarbon, Receptors, 4995, Tocris Bioscience

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