Art. -Nr.: HY-118304B

AKN-028 acetate

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AKN-028 acetate, a novel tyrosine kinase (TK) inhibitor, is a potent, orally active FMS-like receptor tyrosine kinase 3 (FLT3) inhibitor with an IC50 value of 6 nM. AKN-028 acetate inhibits FLT3 autophosphorylation. AKN-028 acetate induces dose-dependent cytotoxic response (mean IC50=1 μM). AKN-028 acetate induces apoptosisby activation of caspase 3. AKN-028 acetate can be used in research of acute myeloid leukemia (AML).

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Reinheit: 98.38%
Formel: C₁₉H₁₈N₆O₂
Molecular Weight:362.39

Speicherung:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

AKN-028 acetate Chemical Structure

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Verfügbarkeit

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 6 nM (FLT3), 140 nM (CLK1), 220 nM (RPS6KA), 520 nM (VEGFR2), and 120 nM (FGFR2)^[1]

Alle Caspase Isoform-spezifische Produkte anzeigen :

In Vitro

AKN-028 (0.1 nM-100 μM; 15 h; mouse embryonal fibroblasts and human acute megakaryoblastic leukemia M07 cells) acetate inhibits FLT3 and KIT autophosphorylation in a dose-dependent manner^[1].
AKN-028 (10 μM; 72 h; tumor cell lines) acetate is cytotoxic to AML cell lines and induces apoptosis in the AML cell line MV4-11^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay^[1]

Cell Line:

Tumor cell lines
Concentration:

10 μM
Incubation Time:

72 hours
Result:

Had cytotoxic activity was highest in MV4-11 and MOLM-13 (IC₅₀<50 nM), followed by the three other AML cell lines (IC₅₀=0.5-6 μM).

Western Blot Analysis^[1]

Cell Line:

Mouse embryonal fibroblasts either overexpressing FLT-wt, FLT3-TKD or FLT3-ITD and human acute megakaryoblastic leukemia M07 cells overexpressing KIT
Concentration:

0.1 nM-100 μM
Incubation Time:

15 hours
Result:

Inhibited FLT3 and KIT autophosphorylation.

In Vivo

AKN-028 (15 mg/kg; i.h.; twice daily, for 6 days; male C57 black mice with MV4-11 xenografts) acetate inhibits growth of primary AML and MV4-11 cells in mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Male C57 black mice with MV4-11 xenografts^[1]
Dosage:

15 mg/kg
Administration:

Subcutaneous injection; twice daily, for 6 days
Result:

Inhibited tumor growth and did not affect body weight.

Chemical Information

Appearance Solid
Molecular Weight 362.39
Formel C₁₉H₁₈N₆O₂
Color Brown to orange
SMILES

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

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (275.95 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.7595 mL

13.7973 mL

27.5946 mL

5 mM

0.5519 mL

2.7595 mL

5.5189 mL

10 mM

0.2759 mL

1.3797 mL

2.7595 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.7595 mL	13.7973 mL	27.5946 mL	68.9864 mL
	5 mM	0.5519 mL	2.7595 mL	5.5189 mL	13.7973 mL
	10 mM	0.2759 mL	1.3797 mL	2.7595 mL	6.8986 mL
	15 mM	0.1840 mL	0.9198 mL	1.8396 mL	4.5991 mL
	20 mM	0.1380 mL	0.6899 mL	1.3797 mL	3.4493 mL
	25 mM	0.1104 mL	0.5519 mL	1.1038 mL	2.7595 mL
	30 mM	0.0920 mL	0.4599 mL	0.9198 mL	2.2995 mL
	40 mM	0.0690 mL	0.3449 mL	0.6899 mL	1.7247 mL
	50 mM	0.0552 mL	0.2759 mL	0.5519 mL	1.3797 mL
	60 mM	0.0460 mL	0.2300 mL	0.4599 mL	1.1498 mL
	80 mM	0.0345 mL	0.1725 mL	0.3449 mL	0.8623 mL
	100 mM	0.0276 mL	0.1380 mL	0.2759 mL	0.6899 mL

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AKN-028 acetate

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Cytokine Inhibitors Library

Cell Death Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Apoptosis Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Alle Caspase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AKN-028 acetate

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Cytokine Inhibitors Library

Cell Death Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Apoptosis Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Alle Caspase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AKN-028 acetate Related Classifications

HY-118304B Related Classifications