We have obtained a new water-soluble form of boron(III) dipyrromethene luminophores using the example of 3,3',5,5'-tetraphenyl-ms-aza-2,2'-dipyrromethenate boron(III) (BODIPY) and Cremophor® (polyethylene glycol, PEG-40). The results of a study of the spectral-luminescent properties of the studied BODIPY–Cremophor®–aqueous–alcohol medium system are presented. It is found that Cremophor® is the only one of a series of investigated excipients (PEG-400, PEG-1000, polyvinylpyrrolidone, bovine serum albumin, sodium carboxymethylcellulose) providing solubilization of BODIPY in an aqueous medium, while maintaining its intense spectral characteristics, including fluorescence and luminophore, in the red region of the spectrum. The BODIPY–Cremophor® system is tested on two mouse cell lines: metastatic breast cancer and non-metastatic skin cancer. It is shown that the introduction of the BODIPY–Cremophor® system into both cell lines of mice leads to the detachment of cell cultures from the substrate and suppression of the development of cancerous tumors. The results obtained show that immobilization of BODIPY in PEG-40 in an aqueous-alcoholic medium makes it possible to obtain preparations with prolonged action, which can be used as photosensitizers (PSs) in photodynamic therapy and for bioimaging in cell biology.