1841464-21-8
1841464-21-8 结构式
基本信息
K-Ras-PDEδ-IN-1
N-(4-fluorophenethyl)-4-(4-methyl-7-oxo-2-(p-tolyl)-2,7-dihydro-6H-pyrazolo[3,4-d]pyridazin-6-yl)butanamide
6H-Pyrazolo[3,4-d]pyridazine-6-butanamide, N-[2-(4-fluorophenyl)ethyl]-2,7-dihydro-4-methyl-2-(4-methylphenyl)-7-oxo-
物理化学性质
常见问题列表
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PDE4 8.3 nM (Kd) |
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.