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AKN-028

Catalog No. T38562   CAS 1175017-90-9

AKN-028 is an orally active and potent FLT3 tyrosine kinase inhibitor ( IC 50 = 6 nM). AKN-028 causes dose-dependent inhibition of FLT3 autophosphorylation.

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AKN-028 Chemical Structure
AKN-028, CAS 1175017-90-9
Pack Size Availability Price/USD Quantity
1 mg In stock $ 41.00
5 mg In stock $ 89.00
10 mg In stock $ 151.00
25 mg In stock $ 312.00
50 mg In stock $ 490.00
100 mg In stock $ 715.00
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Purity: 97.3%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description AKN-028 is an orally active and potent FLT3 tyrosine kinase inhibitor ( IC 50 = 6 nM). AKN-028 causes dose-dependent inhibition of FLT3 autophosphorylation.
Targets&IC50 FLT3:6 nM (IC50), CLK1:140 nM (IC50), FGFR2:1200 nM (IC50), RPS6KA:220 nM (IC50), VEGFR2:520 nM (IC50)
In vitro AKN-028 triggers apoptosis in MV4-11 by activation of caspase 3 [1] . AKN-028 (10 μM) is cytotoxic to AML cell lines and induces apoptosis in the AML cell line MV4-11 [1] . Cell Cytotoxicity Assay [1] Cell Line: AML cell line MV4-11. Concentration: 10 μM. Incubation Time: 24 h. Result: Was cytotoxic to primary AML cells, irrespective of FLT3 mutation status and quantitative FLT3 expression.
In vivo AKN-028 (15?mg/kg, Subcutaneously injection twice daily) exhibits anti-tumor activities for acute myeloid leukemia (AML) models [1] . Animal Model: Mice based AML and MV4-11 cells [1] . Dosage: 15?mg/kg. Administration: Subcutaneously injection twice daily. Result: Inhibited net growth of one of the primary AML samples (UPN26) in vivo and furthermore reduced the tumor mass of MV4-11 cell line.
Molecular Weight 302.33
Formula C17H14N6
CAS No. 1175017-90-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 1.43 mg/mL (4.73 mM), Sonification is recommended

TargetMolReferences and Literature

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.

Related compound libraries

This product is contained In the following compound libraries:
Tyrosine Kinase Inhibitor Library Bioactive Compound Library Clinical Compound Library Inhibitor Library Kinase Inhibitor Library Drug Repurposing Compound Library Bioactive Compounds Library Max

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Keywords

AKN-028 1175017-90-9 Angiogenesis Tyrosine Kinase/Adaptors FLT inhibit Cluster of differentiation antigen 135 Inhibitor Fms like tyrosine kinase 3 Caspase acute myeloid leukemia CD135 Apoptosis FLT3 AKN028 AML cell lines cytotoxic FLT3 autophosphorylation AKN 028 inhibitor

 

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