1. Protein Tyrosine Kinase/RTK
    Apoptosis
  2. FLT3
    Caspase
  3. AKN-028

AKN-028 

Cat. No.: HY-118304
Handling Instructions

AKN-028 is an orally active and potent FLT3 tyrosine kinase inhibitor (IC50 = 6 nM). AKN-028 causes dose-dependent inhibition of FLT3 autophosphorylation.

For research use only. We do not sell to patients.

AKN-028 Chemical Structure

AKN-028 Chemical Structure

CAS No. : 1175017-90-9

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Description

AKN-028 is an orally active and potent FLT3 tyrosine kinase inhibitor (IC50 = 6 nM). AKN-028 causes dose-dependent inhibition of FLT3 autophosphorylation[1].

IC50 & Target

FLT3

6 nM (IC50)

CLK1

140 nM (IC50)

RPS6KA

220 nM (IC50)

VEGFR2

520 nM (IC50)

FGFR2

1200 nM (IC50)

Caspase 3

 

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

SMILES

NC1=NC=C(N=C1NC2=CC3=C(C=C2)NC=C3)C4=CC=NC=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

AKN-028AKN028AKN 028FLT3CaspaseCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3AMLacutemyeloidleukemiaTKIInhibitorinhibitorinhibit

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AKN-028
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HY-118304
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