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

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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AKN-028 acetate Chemical Structure

AKN-028 acetate Chemical Structure

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Based on 1 publication(s) in Google Scholar

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AKN-028 acetate Related Antibodies

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Description

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).

IC50 & Target

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

AKN-028 acetate Related Antibodies

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.
Clinical Trial
Molecular Weight

362.39

Formula

C19H18N6O2
Appearance

Solid

Color

Brown to orange

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7595 mL 13.7973 mL 27.5946 mL
5 mM 0.5519 mL 2.7595 mL 5.5189 mL
View the Complete Stock Solution Preparation Table

* 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.

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

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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

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 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AKN-028AKN028AKN 028FLT3ApoptosisCaspaseCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3FLT3 autophosphorylationacute myeloid leukemiacytotoxicAML cell linesInhibitorinhibitorinhibit

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