1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)
  3. K-Ras-PDEδ-IN-1

K-Ras-PDEδ-IN-1 

Cat. No.: HY-115555
Handling Instructions

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.

For research use only. We do not sell to patients.

K-Ras-PDEδ-IN-1 Chemical Structure

K-Ras-PDEδ-IN-1 Chemical Structure

CAS No. : 1841464-21-8

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Description

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].

IC50 & Target[1]

PDE4

8.3 nM (Kd)

In Vitro

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

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[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].

Molecular Weight

447.50

Formula

C₂₅H₂₆FN₅O₂

CAS No.

1841464-21-8

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

K-Ras-PDEδ-IN-1Phosphodiesterase (PDE)pyrazolopyridazinone-basedK-Ras-PDEδcancerPDEδInhibitorinhibitorinhibit

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