Tag Archives: kinase inhibition assays @de

BÜHLMANN announces new Microsite for Kinase Inhibition Assay

BÜHLMANN’s Kinase Inhibition Assay Testing Potency and Efficacy of Inhibitors of PI3K δ, PI3K γ, BTK and SYK Activity Biomarker assays are developed specifically for pharmacokinetic and pharmacodyamic (PK/PD) models during drug discovery and are often used to test efficacy and toxicity. Inhibitors of PI3K, BTK and SYKpathways are a large focus for pharmaceutical companies

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Discovery of PI3K Delta Inhibitors for the Treatment of Inflammatory and Autoimmune Disease

Flow CAST® – Kinase Inhibtion Assay Citation: Matthews, D.J. et al. Discovery of PI3K delta inhibitors for the treatment of inflammatory and autoimmune disease. 2012 New York Academy of Sciences Meeting Poster.  "Importantly, PWT143 inhibits basophil activation (as measured by surface CD63 expression in a whole blood assay) with subnanomolar potency in response to anti-IgE stimulation
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TGR-1202 Suppresses Acute Myeloid Leukemia (AML) and Acute Lymphoblastic Leukemia (ALL) Cells via Selective Inhibition of PI3Kδ Kinase

Flow CAST® – Kinase Inhibtion Assay Citation: VakkalankaS. et al. TGR-1202 suppresses acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL) cells via selective inhibition of PI3Kδ kinase. 2012 ASH Meeting Poster. "TGR-1202 demonstrated significant potency against PI3Kδ (22.2 nM) with several fold selectivity over the α (>10000), β (>50), and γ (>48) isoforms. Additionally, the
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Brutontyrosine Kinase Inhibitor Ibrutinib(PCI-32765) has Significant Activity in Patients with Relapsed/Refractory B-cell Malignancies

Flow CAST® – Kinase Inhibtion Assay Citation: Advani, R.H. et al. Brutontyrosine kinase inhibitor ibrutinib(PCI-32765) has significant activity in patients with relapsed/refractory B-cell malignancies. J ClinOncol. 2013 Jan 1; 31(1): 88-94. PMID: 23045577 "A decrease in anti–IgE-stimulated basophil degranulation was observed, consistent with the role of BTK downstream of the high-affinity IgE receptor."
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