Estramustine (CAS 2998-57-4)

Estramustine, also known as estracyt or leo 275, is a synthetic molecule that acts as a microtubule assembly inhibitor. It inhibits endothelial cell proliferation (IC50 = 4.5 μM) and down-regulates prostate-specific antigen expression (IC50 = 10.97 μM). As an alkylating and antitumor agent, it demonstrates activity both in vitro and in vivo.This compound is a carbamate ester formed by combining estradiol and nornitrogen mustard. It binds to microtubule-associated proteins (MAPs) and tubulin, thereby hindering microtubule dynamics and inducing dose-dependent anaphase arrest. Additionally, estramustine possesses anti-androgenic effects. It is classified as an estrane steroid, belonging to the group of organic compounds with a structure based on the estrane skeleton, making it a steroid lipid molecule.This compound is involved in several enzymatic reactions and can be biosynthesized from 17beta-estradiol. It can also be converted into estramustine phosphate. With its role as an antineoplastic agent, alkylating agent, and radiation protective agent, estramustine acts as a carbamate ester, a 17beta-hydroxy steroid, and an organochlorine compound.