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