K-Ras-PDEδ-IN-1 |
| Catalog No.GC62024 |
K-Ras-PDEδ-IN-1 es un nuevo y potente competitivo K-Ras-PDEδ inhibidor K-Ras-PDEδ-IN-1 se une al bolsillo de uniÓn de farnesilo de PDEδ con una Kd nanomolar baja de 8 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1841464-21-8
Sample solution is provided at 25 µL, 10mM.
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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 Kd of 8 nM[1].
K-Ras-PDEδ-IN-1 exhibits an IC50 value of 12.3 μM in PaTu8902/Panc1 CTG assay[1].
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 (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[1].
[1]. Sandip Murarka, et al. Development of Pyridazinone Chemotypes Targeting the PDEδ Prenyl Binding Site. Chemistry. 2017 May 2;23(25):6083-6093.
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