Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C17H14N6.C2HF3O2 |
| Molecular Weight | 416.3566 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
OC(=O)C(F)(F)F.NC1=C(NC2=CC3=C(NC=C3)C=C2)N=C(C=N1)C4=CC=NC=C4
InChI
InChIKey=FWEYJLNSAWCAPA-UHFFFAOYSA-N
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)
| Molecular Formula | C2HF3O2 |
| Molecular Weight | 114.0233 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
| Molecular Formula | C17H14N6 |
| Molecular Weight | 302.3333 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
AKN-028 is an orally bioavailable protein tyrosine kinase inhibitor for FMS-related tyrosine kinase 3 (IC(50)=6 nM) and stem cell factor receptor (SCFR; KIT), with potential antineoplastic activity. FLT3/KIT kinase inhibitor AKN-028 binds to and inhibits both the wild-type and mutated forms of FLT3 and SCFR. Akinion Pharmaceuticals is developing AKN-028 for the treatment of acute myeloid leukaemia. AKN-028 is presently undergoing investigation in a phase I/II study.
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| AKN-028 induces cell cycle arrest, downregulation of Myc associated genes and dose dependent reduction of tyrosine kinase activity in acute myeloid leukemia. | 2014-01-15 |
|
| The novel tyrosine kinase inhibitor AKN-028 has significant antileukemic activity in cell lines and primary cultures of acute myeloid leukemia. | 2012-08-03 |
Patents
Sample Use Guides
Acute Myelogenous Leukemia: Part 1 of the study is a sequential dose-escalation evaluation of AKN-028. Part 1 started as an accelerated intra-patient dose escalation design in one patient at a time (the N=1 portion), and has switched to standard 3 + 3 design with inter-cohort dose escalation when AUC of 12 uM*hrs has been reached. Starting dose of AKN-028 was 60 mg twice a day.
Route of Administration:
Oral
| Substance Class |
Chemical
Created
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admin
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Edited
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Mon Mar 31 22:38:40 GMT 2025
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| Record UNII |
S21H29542Y
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| Record Status |
Validated (UNII)
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