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

AKN-028, 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 inhibits FLT3 autophosphorylation. AKN-028 induces dose-dependent cytotoxic response (mean IC50=1 μM). AKN-028 induces apoptosisby activation of caspase 3. AKN-028 can be used in research of acute myeloid leukemia (AML).

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (AKN-028 acetate) usually boasts enhanced water solubility and stability.

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, 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 inhibits FLT3 autophosphorylation. AKN-028 induces dose-dependent cytotoxic response (mean IC50=1 μM). AKN-028 induces apoptosisby activation of caspase 3. AKN-028 can be used in research of acute myeloid leukemia (AML)[1].

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) inhibits FLT3 and KIT autophosphorylation in a dose-dependent manner[1].
AKN-028 (10 μM; 72 h; tumor cell lines) 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 Related Antibodies

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.

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).
In Vivo

AKN-028 (15 mg/kg; i.h.; twice daily, for 6 days; male C57 black mice with MV4-11 xenografts) 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

302.33

Formula

C17H14N6
CAS No.
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.
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (413.46 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 3.3076 mL 16.5382 mL 33.0764 mL
5 mM 0.6615 mL 3.3076 mL 6.6153 mL
View the Complete Stock Solution Preparation Table

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Purity & Documentation
References

Complete Stock Solution Preparation Table

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.3076 mL 16.5382 mL 33.0764 mL 82.6911 mL
5 mM 0.6615 mL 3.3076 mL 6.6153 mL 16.5382 mL
10 mM 0.3308 mL 1.6538 mL 3.3076 mL 8.2691 mL
15 mM 0.2205 mL 1.1025 mL 2.2051 mL 5.5127 mL
20 mM 0.1654 mL 0.8269 mL 1.6538 mL 4.1346 mL
25 mM 0.1323 mL 0.6615 mL 1.3231 mL 3.3076 mL
30 mM 0.1103 mL 0.5513 mL 1.1025 mL 2.7564 mL
40 mM 0.0827 mL 0.4135 mL 0.8269 mL 2.0673 mL
50 mM 0.0662 mL 0.3308 mL 0.6615 mL 1.6538 mL
60 mM 0.0551 mL 0.2756 mL 0.5513 mL 1.3782 mL
80 mM 0.0413 mL 0.2067 mL 0.4135 mL 1.0336 mL
100 mM 0.0331 mL 0.1654 mL 0.3308 mL 0.8269 mL
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AKN-028 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-0281175017-90-9AKN028AKN 028FLT3ApoptosisCaspaseCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3FLT3 autophosphorylationacute myeloid leukemiacytotoxicAML cell linesInhibitorinhibitorinhibit

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