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Image Search Results
Journal: PLoS ONE
Article Title: Preclinical Activity of ARQ 087, a Novel Inhibitor Targeting FGFR Dysregulation
doi: 10.1371/journal.pone.0162594
Figure Lengend Snippet: (A) ARQ 069. (B) ARQ 087. (C) Enzyme kinetic analysis was performed to determine the mode of inhibition of ARQ 087 with FGFR1 and FGFR2. Concentrations of ATP [ATP] and ARQ 087 [I] are indicated on the graphs. The rate plotted is the AlphaScreen ™ signal obtained from the plate reader with background correction. The experiments were conducted in triplicates and the means and the standard deviations were plotted. The number of parameter ( n p ), the sum of squares rel ( SS rel ), Akaike information criterion ( AIC ), weight of AIC ( w (AIC) ), Bayesian information criterion ( BIC ) and the weight of BIC ( w (BIC) ) for each binding mode were determined by the DynaFit software and are summarized below the plots. The dissociation constant ( K i) of ARQ 087 for FGFR1 and FGFR2 are shown. (D) The effect of ARQ 087 on the activation of FGFR1 and FGFR2 was examined in a continuous autophosphorylation assay.
Article Snippet: Kinase inhibitory activity of ARQ 087 was determined for the
Techniques: Inhibition, Amplified Luminescent Proximity Homogenous Assay, Binding Assay, Software, Activation Assay
Journal: PLoS ONE
Article Title: Preclinical Activity of ARQ 087, a Novel Inhibitor Targeting FGFR Dysregulation
doi: 10.1371/journal.pone.0162594
Figure Lengend Snippet: ARQ 087 biochemical activity.
Article Snippet: Kinase inhibitory activity of ARQ 087 was determined for the
Techniques: Activity Assay
Journal: PLoS ONE
Article Title: Preclinical Activity of ARQ 087, a Novel Inhibitor Targeting FGFR Dysregulation
doi: 10.1371/journal.pone.0162594
Figure Lengend Snippet: COS-1 cells ectopically expressing FGFR1, FGFR2, FGFR3 or FGFR4 were treated with the indicated concentrations of ARQ 087 for 2 hours followed by stimulation with 100 pM of FGF1/2/7 for 15 minutes. Total and phospho-FGFR was assessed by Western blot analyses. β-Actin was used as a loading control. The EC 50 values of individual FGFR family members are shown.
Article Snippet: Kinase inhibitory activity of ARQ 087 was determined for the
Techniques: Expressing, Western Blot
Journal: PLoS ONE
Article Title: Preclinical Activity of ARQ 087, a Novel Inhibitor Targeting FGFR Dysregulation
doi: 10.1371/journal.pone.0162594
Figure Lengend Snippet: ARQ 087 GI 50 in Ba/F3 transfected cell lines.
Article Snippet: Kinase inhibitory activity of ARQ 087 was determined for the
Techniques: Transfection
Journal: PLoS ONE
Article Title: Preclinical Activity of ARQ 087, a Novel Inhibitor Targeting FGFR Dysregulation
doi: 10.1371/journal.pone.0162594
Figure Lengend Snippet: ARQ 087 activity in FGFR dysregulated cell lines.
Article Snippet: Kinase inhibitory activity of ARQ 087 was determined for the
Techniques: Activity Assay, Amplification, Over Expression