MN-029 di-hydrochloride (MN-029.2HCl, Formula 2) is a potent vascular targeting agent.The present invention focuses on the synthesis and characterization of the di-hydrochloride salt MN-029 and the preparation of pharmaceutically acceptable formulations thereof. Methods are disclosed of using the compound and formulations thereof in the treatment of diseases that rely on the generation of neovasculature by angiogenesis for disease progression.