tcsc2224 Busulfan

Busulfan is a potent alkylator, with chemotherapeutic activity.

IC50 & Target: DNA Alkylator^[1]

In Vitro: Busulfan is a potent alkylating agent, and used as a chemotherapeutic agent. Busulfan (120 μM) results in premature senescence in WI38 cells via the Erk and p38 MAPK pathway, reduces GSH and increases ROS production, but the production can be suppressed by NADPH oxidase^[1].

In Vivo: Busulfan (40 mg/kg, i.p) increases apoptosis and decreases the testis weight in mice. The testes of Busulfan-treated mice exhibits higher level of pRB expression, inhibits Rb phosphorylation and PCNA expression compared to the control^[2]. Busulfan (2.5, 5.0 mg/kg, i.p.) causes earlier occurrence of persistent esturs in a dose dependent manner in rats. Busulfan (5.0 mg/kg) also increases the incidence of uterine adenocarcinomas and multiplicity of uterine neoplastic lesions. In addition, Busulfan decreases the serum 17β-estradiol(E2), progesterone and inhibin levels in rats, and elevates the E2/progesterone ratio only at 5.0 mg/kg^[3].