PDEδ-IN-99

Research use only, not for human use.

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.

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