TGR-1202 Suppresses Acute Myeloid Leukemia (AML) and Acute Lymphoblastic Leukemia (ALL) Cells via Selective Inhibition of PI3Kδ Kinase

Oktober 11, 2016 Tagged with: B cell proliferation @de, B-cell malignancies @de, basophil @de, basophil activation test @de, CD63 @de, FcεR1 @de, Flow CAST Kinase Inhibition Assay @de, kinase inhibition assays @de, kinase signaling pathway @de, Pharmacodynamics @de, PI3Kδ @de, small-molecule kinase inhibitor @de, TGR-1202 @de

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 compound inhibited B-cell proliferation (24.3 nM) and FcεR1 induced CD63 expression in human whole blood basophils (68.2 nM) indicating specificity towards the delta isoform.“