| Bioactivity | AKN-028 acetate, a novel tyrosine kinase (TK) inhibitor, is a potent, orally active FMS-like receptor tyrosine kinase 3 (FLT3) inhibitor with an IC50 value of 6 nM. AKN-028 acetate inhibits FLT3 autophosphorylation. AKN-028 acetate induces dose-dependent cytotoxic response (mean IC50=1 μM). AKN-028 acetate induces apoptosisby activation of caspase 3. AKN-028 acetate can be used in research of acute myeloid leukemia (AML)[1]. |
| Target | IC50: 6 nM (FLT3), 140 nM (CLK1), 220 nM (RPS6KA), 520 nM (VEGFR2), and 120 nM (FGFR2) |
| Invitro | AKN-028 (0.1 nM-100 μM; 15 h; mouse embryonal fibroblasts and human acute megakaryoblastic leukemia M07 cells) acetate inhibits FLT3 and KIT autophosphorylation in a dose-dependent manner[1].AKN-028 (10 μM; 72 h; tumor cell lines) acetate is cytotoxic to AML cell lines and induces apoptosis in the AML cell line MV4-11[1]. Cell Cytotoxicity Assay[1] Cell Line: |
| In Vivo | AKN-028 (15 mg/kg; i.h.; twice daily, for 6 days; male C57 black mice with MV4-11 xenografts) acetate inhibits growth of primary AML and MV4-11 cells in mice[1]. Animal Model: |
| Name | AKN-028 acetate |
| Formula | C19H18N6O2 |
| Molar Mass | 362.39 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [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. |