7‐Fluoro‐2‐aminophenazine 5,10‐dioxide, 1, has displayed in vitro bioreductive selective cytotoxicity, which could acts towards tumors containing hypoxic regions. In this work, we describe some preclinical studies of compound 1 confirming its in vivo antitumor activity. The synthesis of compound 1 was scaled up to 3 g improving the micro‐scale yield. Some drug‐like properties for compound 1 were theoretically‐predicted and others, i. e. aqueous‐solubility and toxicity ‐mutagenicity, in vivo chromosomal‐aberrations and ip acute LD50‐, were experimentally confirmed. Antitumoral activity was studied in mice bearing hypoxic 4T1‐breast‐tumor by assessing evolution of the tumor‐sizes, animal‐survival and bio‐chemical/hematological. Compound 1 in vivo efficacy, with the absence of systemic toxicity, was confirmed.. Results highlight the potential of 7‐fluoro‐2‐aminophenazine 5,10‐dioxide as promissory therapeutic agent for solid tumors.