Category: BÜHLMANN Kinase Inhibition Assays Citations

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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PI3K-δ and PI3K-γ Inhibition by IPI-145 Abrogates Immune Responses and Suppresses Activity in Autoimmune and Inflammatory Disease Models

Flow CAST® – Kinase Inhibtion Assay Citation: Winkler, DG et al. PI3K-δ and PI3K-γ inhibition by IPI-145 abrogates immune responses and suppresses activity in autoimmune and inflammatory disease models. Chem Biol. 2013 Nov 21;20(11):1364-74. doi: 10.1016/j.chembiol.2013.09.017. Epub 2013 Nov 7. PMID: 24211136. "These studies demonstrate that IPI-145 exerts profound effects on adaptive and innate immunity by inhibiting
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CAL-101, A p110delta Selective Phosphatidylinositol-3-Kinase Inhibitor for the Treatment of B-cell Malignancies, Inhibits PI3K Signaling and Cellular Viability

Flow CAST® - Kinase Inhibtion Assay Citation: Lannutti, B.J. et al. CAL-101, a p110δ selective phosphatidylinositol-3-kinase inhibitor for the treatment of B-cell malignancies, inhibits PI3K signaling and cellular viability. Blood. 2011 Jan 13; 117(2): 591-594. PMID: 20959606. "We have thus described the biochemical and cellular activity of CAL-101, a selective and potent inhibitor of p110δ; such targeted
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