AKN-028 acetate

• CAT Number: I042851
• Molecular Formula: C19H18N6O2
• Molecular Weight: 362.39
• Purity: ≥95%
• Synonyms: acetic acid;3-N-(1H-indol-5-yl)-5-pyridin-4-ylpyrazine-2,3-diamine
• InChI: InChI=1S/C17H14N6.C2H4O2/c18-16-17(22-13-1-2-14-12(9-13)5-8-20-14)23-15(10-21-16)11-3-6-19-7-4-11;1-2(3)4/h1-10,20H,(H2,18,21)(H,22,23);1H3,(H,3,4)
• InChIKey: KMFGKUDUSUBTMI-UHFFFAOYSA-N
• SMILES: CC(=O)O.C1=CC2=C(C=CN2)C=C1NC3=NC(=CN=C3N)C4=CC=NC=C4

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).
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].
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].

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.
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