PDEδ-IN-99

K-Ras-PDEδ-IN-1 exhibits an IC ₅₀ value of 12.3 μM in PaTu8902/Panc1 CTG assay.

K-Ras-PDEδ-IN-1 (oral or intraperitoneal injection; 10 mg/kg; single dose) is in different vehicles (A=5% Tween-80, 50% NaCl, 45% H2O; B=20% DMSO, 80% PEG200; C=15% DMSO, 9.5% Cremophor EL/EtOH (1:1), 75.5 % H2O) for oral and intraperitoneal (IP) administration.whereas only very low compound levels are found in plasma after oral dosage, but significantly higher plasma concentrations are found after IP administration in vehicle A, B or C at 10 mg kg.K-Ras-PDEδ-IN-1 (intravenous injection; 3 mg kg; single dose; 24 hours) shows a significant increase of the plasma exposure as well as the terminal half-life (t _1/2 =0.4 hours)when compares to compound 93,exhibits a t _1/2 , CO, AUC _0-tz , AUC _0.inf-obs , Cl _obs , and Vss _0-inf-obs values of 4.1 hours, 2790.9 ng/ml, 1646.4 h.ng/ml, 1662.5 h.ng/ml, 1.8 L/h/kg, 5.9 l/kg.