Synonym
AKN-028 trifluoroacetate; AKN 028 trifluoroacetate; AKN028 trifluoroacetate
IUPAC/Chemical Name
2,3-Pyrazinediamine, N3-1H-indol-5-yl-5-(4-pyridinyl)-, 2,2,2-trifluoroacetate (1:1)
InChi Key
FWEYJLNSAWCAPA-UHFFFAOYSA-N
InChi Code
InChI=1S/C17H14N6.C2HF3O2/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;3-2(4,5)1(6)7/h1-10,20H,(H2,18,21)(H,22,23);(H,6,7)
SMILES Code
NC1=NC=C(C2=CC=NC=C2)N=C1NC3=CC4=C(NC=C4)C=C3.O=C(O)C(F)(F)F
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.03.00
Preparing Stock Solutions
The following data is based on the
product
molecular weight
416.36
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
1: Eriksson A, Kalushkova A, Jarvius M, Hilhorst R, Rickardson L, Kultima HG, de Wijn R, Hovestad L, Fryknäs M, Öberg F, Larsson R, Parrow V, Höglund M. AKN-028 induces cell cycle arrest, downregulation of Myc associated genes and dose dependent reduction of tyrosine kinase activity in acute myeloid leukemia. Biochem Pharmacol. 2014 Jan 15;87(2):284-91. doi: 10.1016/j.bcp.2013.10.022. Epub 2013 Nov 4. PubMed PMID: 24200998.
2: Eriksson A, Hermanson M, Wickström M, Lindhagen E, Ekholm C, Jenmalm Jensen A, Löthgren A, Lehmann F, Larsson R, Parrow V, Höglund M. 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:e81. doi: 10.1038/bcj.2012.28. PubMed PMID: 22864397; PubMed Central PMCID: PMC3432483.