Luxeptinib

Luxeptinib (CG-806) is an orally active, reversible, first-in-class, non-covalent and potent pan-FLT3/pan-BTK inhibitor. Luxeptinib induces cell cycle arrest, apoptosis or autophagy in acute myeloid leukemia cells[1][2][3][4].

Research Areas >> Cancer

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> FLT3

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Btk

Pan-FLT3/Pan-BTK[1]

Luxeptinib (MEC-1 CLL cells; 0.1~10 µM; 72 hours) inhibits cells proliferation with an IC50 of 32 nM[1]. Luxeptinib inhibits BCR signaling-induced phosphorylation of BTK, PLCg2, AKT, ERK1/2, S6 ribosomal protein and strongly suppresses SYK phosphorylation in primary chronic lymphocytic leukemia (CLL) cells[1]. Luxeptinib (MV4-11 cells; 500 pM; 1 hour) completely inhibits phosphorylation of FLT3 and STAT5[2]. Cell Proliferation Assay[1] Cell Line: MEC-1 CLL cells Concentration: 0.1~10 µM Incubation Time: 72 hours Result: Inhibited cells proliferation with an IC50 of 32 nM.

[1]. Ekaterina Kim MS, et al. CG-806, a First-in-Class Pan-FLT3/Pan-BTK Inhibitor, Exhibits Broad Signaling Inhibition in Chronic Lymphocytic Leukemia Cells. bloodjournal Blood blood (2019). 134 (Supplement_1) : 3051.

[2]. Abstract 44: CG′806, a first-in-class FLT3/BTK inhibitor, exhibits potent activity against AML patient samples with mutant or wild type FLT3, as well as other hematologic malignancy subtypes

[3]. Guopan Yu,et al.CG '806, a Novel Pan-FLT3/BTK Multi-Kinase Inhibitor, Induces Cell Cycle Arrest, Apoptosis or Autophagy in AML Cells Depending on FLT3 Mutation Status. Blood blood (2017).130 (Suppl_1) : 462

[4]. Aptose Biosciences to Present CG’806 Data at AACR Hematologic Malignancies Meeting