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K-Ras-PDEδ-IN-1

產(chǎn)品活性：K-Ras-PDEδ-IN-1 是一種新穎的、有效的 K-Ras-PDEδ 抑制劑。K-Ras-PDEδ-IN-1 以低納摩爾 K_d 8 nM 與 PDEδ 的法尼基結(jié)合袋競(jìng)爭(zhēng)性結(jié)合。

研究領(lǐng)域：Metabolic Enzyme/Protease

作用靶點(diǎn)：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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