K-Ras-PDEδ-IN-1 

K-Ras-PDEδ-IN-1 is a novel and potent competitive K-Ras-PDEδ inhibitor. K-Ras-PDEδ-IN-1 binds to the farnesyl binding pocket of PDEδ with a low nanomolar K_d of 8 nM^[1].

K-Ras-PDEδ-IN-1 exhibits an IC₅₀ value of 12.3 μM in PaTu8902/Panc1 CTG assay^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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^[1].
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^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

447.50

Solid

C₂₅H₂₆FN₅O₂

1841464-21-8

O=C(NCCC1=CC=C(F)C=C1)CCCN2N=C(C)C3=CN(C4=CC=C(C)C=C4)N=C3C2=O

Room temperature in continental US; may vary elsewhere.

• [1]. Sandip Murarka, et al. Development of Pyridazinone Chemotypes Targeting the PDEδ Prenyl Binding Site. Chemistry. 2017 May 2;23(25):6083-6093.  [Content Brief]