| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
IC50: 6 nM (FLT3), 140 nM (CLK1), 220 nM (RPS6KA), 520 nM (VEGFR2), and 120 nM (FGFR2)[1]
FLT3 (FMS-like tyrosine kinase 3). |
|---|---|
| ln Vitro |
In a dose-dependent way, AKN-028 (0.1 nM-100 μM; 15 hours) acetate inhibits FLT3 and KIT autophosphorylation in mouse embryonic fibroblasts and human acute megakaryocytic leukemia M07 cells [1]. Tumor cell lines; AKN-028 (10 μM; 72 hours) Acetate is cytotoxic to AML cell lines and causes the MV4-11 AML cell line to undergo apoptosis [1].
AKN-028 acetate inhibits FLT3 autophosphorylation in a dose-dependent manner in mouse embryonal fibroblasts and M07 cells (0.1 nM-100 microM). It is cytotoxic to AML cell lines (e.g., MV4-11, MOLM-13) with IC50 <50 nM for the most sensitive lines. |
| ln Vivo |
AKN-028: male C57 black mice with MV4-11 xenografts, 15 mg/kg, ih, twice daily for 6 days) Acetate stops mouse primary AML and MV4-11 cells from growing [1].
Administered subcutaneously at 15 mg/kg twice daily for six days, AKN-028 acetate effectively inhibits the growth of primary AML and MV4-11 xenografts in male C57 black mice without affecting body weight, demonstrating significant in vivo antitumor efficacy. |
| Enzyme Assay |
A standard in vitro kinase assay is used. Purified FLT3 kinase, a peptide substrate, and ATP are incubated with varying concentrations of the inhibitor. The reaction is stopped, and the amount of phosphorylated substrate is quantified (e.g., by ELISA). IC50 values are calculated from the dose-response curve.
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| Cell Assay |
Cell Cytotoxicity Assay[1]
Cell Types: Tumor cell lines Tested Concentrations: 10 μM Incubation Duration: 72 hrs (hours) Experimental Results: Had cytotoxic activity was highest in MV4-11 and MOLM-13(IC50<50 nM), followed by the three other AML cells lines(IC50=0.5-6 μM). Western Blot Analysis[1] Cell Types: Mouse embryonal fibroblasts either overexpressing FLT-wt, FLT3-TKD or FLT3-ITD and human acute megakaryoblastic leukemia M07 cells overexpressing KIT Tested Concentrations: 0.1 nM-100 μM Incubation Duration: 15 hrs (hours) Experimental Results: Inhibited FLT3 and KIT autophosphorylation. For a cytotoxicity assay, AML cell lines (MV4-11, MOLM-13) are seeded in 96-well plates. They are treated with serial dilutions of AKN-028 (0.1 nM-100 microM) for 72 hours. Cell viability is measured using a CCK-8 or MTT assay. The IC50 is defined as the concentration that reduces viability by 50%. |
| Animal Protocol |
Animal/Disease Models: Male C57 black mice with MV4-11 xenografts[1]
Doses: 15 mg/kg Route of Administration: subcutaneous (sc) injection; twice (two times) daily, for 6 days Experimental Results: Inhibited tumor growth and did not affect body weight. Male C57 black mice with established MV4-11 xenografts are randomized. AKN-028 acetate (15 mg/kg) or vehicle is administered via subcutaneous injection twice daily for six days. Tumor volumes are measured with calipers every 2-3 days, and body weights are monitored. Tumor growth inhibition (TGI) is calculated at study endpoint. |
| ADME/Pharmacokinetics |
AKN-028 is orally active but specific PK parameters (e.g., half-life, bioavailability) are not published. Its pharmacokinetic properties in rodents are suitable for twice-daily subcutaneous dosing, as evidenced by its efficacy in xenograft models.
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| Toxicity/Toxicokinetics |
No specific toxicity studies are published for this research compound. As a tyrosine kinase inhibitor, potential toxicities may include gastrointestinal issues, myelosuppression, and off-target effects. In animal studies, no significant weight loss was observed in treated mice, suggesting good tolerability.
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| References | |
| Additional Infomation |
FLT3 mutations (ITD and TKD) are present in about 30% of AML patients and are associated with poor prognosis. AKN-028 acetate is a preclinical research compound used to study the therapeutic potential of FLT3 inhibition in AML. This product is for research use only and is not an approved drug.
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| Molecular Formula |
C19H18N6O2
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|---|---|
| Molecular Weight |
362.39
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| Related CAS # |
AKN-028;1175017-90-9
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| Appearance |
Brown to orange solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO :~100 mg/mL (~275.95 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.2759 mL | 1.3797 mL | 2.7595 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
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