AKN-028

AKN-028 is an orally active and potent FLT3 tyrosine kinase inhibitor (IC50 = 6 nM). AKN-028 causes dose-dependent inhibition of FLT3 autophosphorylation[1].

Research Areas >> Cancer

Signaling Pathways >> Apoptosis >> Caspase

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

FLT3:6 nM (IC50)

CLK1:140 nM (IC50)

RPS6KA:220 nM (IC50)

VEGFR2:520 nM (IC50)

FGFR2:1200 nM (IC50)

Caspase 3

AKN-028 triggers apoptosis in MV4-11 by activation of caspase 3[1]. AKN-028 (10 μM) is cytotoxic to AML cell lines and induces apoptosis in the AML cell line MV4-11[1]. Cell Cytotoxicity Assay[1] Cell Line: AML cell line MV4-11. Concentration: 10 μM. Incubation Time: 24 h. Result: Was cytotoxic to primary AML cells, irrespective of FLT3 mutation status and quantitative FLT3 expression.

AKN-028 (15 mg/kg, Subcutaneously injection twice daily) exhibits anti-tumor activities for acute myeloid leukemia (AML) models[1]. Animal Model: Mice based AML and MV4-11 cells[1]. Dosage: 15 mg/kg. Administration: Subcutaneously injection twice daily. Result: Inhibited net growth of one of the primary AML samples (UPN26) in vivo and furthermore reduced the tumor mass of MV4-11 cell line.

[1]. A Eriksson, et al. The Novel Tyrosine Kinase Inhibitor AKN-028 Has Significant Antileukemic Activity in Cell Lines and Primary Cultures of Acute Myeloid Leukemia. Blood Cancer J. 2012 Aug 3;2(8):e81.