1807523-99-4

IACS-010759 hydrochloride (5, 10, 25mg/kg/day; oral; for 21 d) results in tumor regression with minimal body weight loss at the 5 or 10mg/kg dose in mice bearing NB-1 (PGD-null) subcutaneous xenografts. IACS-010759 at the 25mg/kg dose is not tolerated^[1].
IACS-010759 HCl (10mg/kg; orally; QD (daily) or QD×5 (5 d on/2 d off); for 35 d) increases median survival from 28 d to longer than 60 d, whereas less-frequent dosing schedules (Q2D or Q3D) enhances survival to a lesser extent^[1].
IACS-010759 hydrochloride (0.3mg/kg for iv; 1mg/kg for oral) has low plasma clearance with a high volume of distribution, resulting in a prolonged terminal half-life (>24h)^[1].