VPC03090

VPC03090 is an orally active prodrug of S1P1/3 antagonist. VPC03090 is phosphorylated by sphingosine kinase 2 (SK2) to form its active form VPC03090-P. VPC03090 reduces tumor volume in mouse breast cancer models. VPC03090 can be used in research related to breast cancer^[1][2]. In Vivo:When administered starting on the day of tumor cell injection, VPC03090 (6.2 mg/kg/day; intraperitoneal injection; daily dosing for 14 consecutive days) significantly reduces the median tumor volume to 1/3 of the original level in the orthotopic syngeneic 4T1 mouse breast cancer model^[1].
VPC03090 (10 mg/kg; p.o.; single administration) is rapidly phosphorylated to VPC03090-P in C57BL/6J mice^[1].
VPC03090 (30 mg/kg; i.p.; single administration) results in undetectable plasma levels of VPC03090-P in sphingosine kinase 2 gene knockout mice, which confirms that sphingosine kinase 2 is essential for the phosphorylation of VPC03090 in vivo^[1].