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K-Ras-PDEδ-IN-1

CAS No. : 1841464-21-8

MCE 国际站：K-Ras-PDEδ-IN-1

产品活性：K-Ras-PDEδ-IN-1 是一种新颖的、有效的 K-Ras-PDEδ 抑制剂。K-Ras-PDEδ-IN-1 以低纳摩尔 K_d 8 nM 与 PDEδ 的法尼基结合袋竞争性结合。

研究领域：Metabolic Enzyme/Protease

作用靶点：Phosphodiesterase (PDE)

In Vitro: K-Ras-PDEδ-IN-1 exhibits an IC₅₀ value of 12.3 μM in PaTu8902/Panc1 CTG assay.

In Vivo: 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.

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