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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, CAS 1175017-90-9

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Purity: 98%

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	VEGFR2:520 nM (IC50), FLT3:6 nM (IC50), CLK1:140 nM (IC50), RPS6KA:220 nM (IC50), FGFR2:1200 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 2 years

Solubility Information

DMSO: <3.02 mg/mL (10 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References 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.

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

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 AKN 028 Apoptosis FLT3 AKN028 AML cell lines cytotoxic FLT3 autophosphorylation inhibitor

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