| Identification | Back Directory | [Name]
AKN-028 | [CAS]
1175017-90-9 | [Synonyms]
AKN-028
2,3-Pyrazinediamine, N3-1H-indol-5-yl-5-(4-pyridinyl)-
inhibit,Cluster of differentiation antigen 135,Inhibitor,Fms like tyrosine kinase 3,Caspase,acute myeloid leukemia,CD135,AKN 028,Apoptosis,AKN-028,FLT3,AKN028,AML cell lines,cytotoxic,FLT3 autophosphorylation | [Molecular Formula]
C17H14N6 | [MOL File]
1175017-90-9.mol | [Molecular Weight]
302.33 |
| Hazard Information | Back Directory | [Uses]
AKN-028, 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 inhibits FLT3 autophosphorylation. AKN-028 induces dose-dependent cytotoxic response (mean IC50=1?μM). AKN-028 induces apoptosisby activation of caspase 3. AKN-028 can be used in research of acute myeloid leukemia (AML)[1]. | [in vivo]
AKN-028 (15?mg/kg; i.h.; twice daily, for 6 days; male C57 black mice with MV4-11 xenografts) inhibits growth of primary AML and MV4-11 cells in mice[1]. | Animal Model: | Male C57 black mice with MV4-11 xenografts[1] | | Dosage: | 15 mg/kg | | Administration: | Subcutaneous injection; twice daily, for 6 days | | Result: | Inhibited tumor growth and did not affect body weight. |
| [References]
[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. DOI:10.1038/bcj.2012.28 |
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| Company Name: |
BOC Sciences
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| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
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