Tag: B-cell malignancies

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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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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