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AKN-028

SKU: orb1303656

Description

AKN-028 is a potent and orally bioavailable small molecule inhibitor of FLT3 tyrosine kinase, demonstrating an IC50 of 6 nM. It effectively suppresses FLT3 autophosphorylation in a dose-dependent manner and is utilized in preclinical research for investigating acute myeloid leukemia (AML) in both cellular and animal models.

Research Area

Cardiovascular Research, Cell Biology, Protein Biochemistry, Signal Transduction

Images & Validation

Key Properties

CAS Number1175017-90-9
MW302.33
Purity99.88% (May vary between batches)
FormulaC17H14N6
SMILESN(C=1N=C(C=NC1N)C=2C=CN=CC2)C=3C=C4C(=CC3)NC=C4
TargetApoptosis,Caspase,FLT
SolubilityDMSO:20 mg/mL (66.15 mM)

Bioactivity

Target IC50
FLT3:6 nM (IC50)|CLK1:140 nM (IC50)|RPS6KA:220 nM (IC50)|FGFR2:1200 nM (IC50)|VEGFR2:520 nM (IC50)
In Vivo
AKN-028 (15 mg/kg, Subcutaneously injection twice daily) exhibits anti-tumor activities for acute myeloid leukemia (AML) models . Animal Model: Mice based AML and MV4-11 cells . 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.
In Vitro
AKN-028 triggers apoptosis in MV4-11 by activation of caspase 3 . AKN-028 (10 μM) is cytotoxic to AML cell lines and induces apoptosis in the AML cell line MV4-11 . Cell Cytotoxicity Assay 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.

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

Fms like tyrosine kinase 3, FLT3 autophosphorylation, FLT3, inhibit, Inhibitor, CD135, Cluster of differentiation antigen 135, cytotoxic, Apoptosis, AML cell lines, Caspase, AKN 028, AKN028, AKN-028, acute myeloid leukemia

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Key Properties

No computed properties available.

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AKN-028 (orb1303656)

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5 mg
¥ 1,300.00
10 mg
¥ 1,690.00
25 mg
¥ 2,990.00
50 mg
¥ 4,420.00
100 mg
¥ 6,110.00
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