PT2399

Validation in Cells and Model Organisms

In vitro validation

On target activity

Potency: 

IC50, KD

< 5 nM (SPA), 42 nM (ITC)

Potency assay: 

Scintillation Proximity Assay (SPA), Isothermal Calorimetry (ITC)

PDB ID for probe-target interaction (3D structure): 

5UFP

Structure-activity relationship: 

yes

In cell validation

On target activity in cells

Potency in cells: 

EC50

6 nM Luciferase14 nM VEGFA

Potency assay (cells): 

Luciferase Assay, VEGF ELISA Assay

In vivo validation

Organism: 

male CD1 micemale Sprague-Dawley rats

Dose: 

10 mg/Kg PO3 mg/Kg IV

Route of delivery: 

OralIntravenous

Plasma half life: 

7.3 (m) 2.9 (r) h

Systemic clearance: 

34.3 (m) 57.6 (r) mL min–1 kg–1

Fraction of probe bound to plasma protein: 

67 (m) 32 (r) %