PDEδ-IN-99

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PDEδ-IN-99 是一种新型有效的 K-Ras-PDEδ 抑制剂，可与 PDEδ 的法呢基结合袋结合，Kd 为 8±4 nM。

PDEδ-IN-99 is a novel potent K-Ras-PDEδ inhibitor that binds to the farnesyl binding pocket of PDEδ with Kd of 8±4 nM.

K-Ras-PDEδ-IN-1 exhibits an IC50 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 (t1/2=0.4 hours)when compares to compound 93,exhibits a t1/2, CO, AUC0-tz, AUC0.inf-obs, Clobs, and Vss0-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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MAPK/ERK Signaling

Ras

Ras

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1841464-21-8

447.514

C25H26FN5O2

>98% (HPLC)

In Vitro:?DMSO : 12.5 mg/mL (27.93 mM)

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N-(4-fluorophenethyl)-4-(4-methyl-7-oxo-2-(p-tolyl)-2,7-dihydro-6H-pyrazolo[3,4-d]pyridazin-6-yl)butanamide

(-20℃)

With Ice Pack

≥ 2 years