| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
In a dose-dependent manner, AKN-028 (0.1 nM-100 μM; 15 hours) suppresses FLT3 and KIT autophosphorylation in mouse embryonic fibroblasts and human acute megakaryocytic leukemia M07 cells [1]. AML cell lines are cytotoxic to AKN-028 (10 μM; 72 hours; malignant cell lines) and AKN-028 causes apoptosis in the AML cell line MV4-11 [1].
|
|---|---|
| ln Vivo |
Primary AML and MV4-11 cell proliferation in mice is inhibited by AKN-028 (15 mg/kg; IV; twice daily for 6 days; male C57 black mice with MV4-11 xenografts) [1].
|
| Cell Assay |
Western Blot Analysis[1]
Cell Types: mouse embryonic fibroblasts overexpressing FLT-wt, FLT3-TKD or FLT3-ITD and human acute megakaryocytic leukemia M07 cells overexpressing KIT Tested Concentrations: 0.1 nM-100 μM Incubation Duration:15 hrs (hours) Experimental Results: FLT3 is inhibited and KIT autophosphorylated. Cytotoxicity assay[1] Cell Types: Tumor cell line Tested Concentrations: 10 μM Incubation Duration: 72 hrs (hours) Experimental Results: MV4-11 and MOLM-13 had the highest cytotoxic activity (IC50<50 nM), followed by the other three AML cell lines (IC50=0.5-6 μM). |
| Animal Protocol |
Animal/Disease Models: Male C57 black mice with MV4-11 xenografts [1]
Doses: 15 mg/kg Route of Administration: subcutaneous injection; twice (two times) daily for 6 days Experimental Results: Inhibited tumor growth without affecting body weight . |
| References | |
| Additional Infomation |
AKN-028 has been used in trials studying the treatment of Acute Myeloid Leukemia.
FLT3/KIT Kinase Inhibitor AKN-028 is an orally bioavailable protein tyrosine kinase inhibitor for FMS-related tyrosine kinase 3 (FLT3; STK1) and stem cell factor receptor (SCFR; KIT), with potential antineoplastic activity. FLT3/KIT kinase inhibitor AKN-028 binds to and inhibits both the wild-type and mutated forms of FLT3 and SCFR. This may result in an inhibition of tumor cell proliferation in cancer cell types that overexpress these receptor tyrosine kinases. |
| Molecular Formula |
C17H14N6
|
|---|---|
| Molecular Weight |
302.33
|
| Exact Mass |
302.128
|
| CAS # |
1175017-90-9
|
| Related CAS # |
AKN-028 acetate
|
| PubChem CID |
44177328
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
3.348
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
23
|
| Complexity |
385
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1(N)=NC=C(C2C=CN=CC=2)N=C1NC1C=CC2=C(C=1)C=CN2
|
| InChi Key |
JLRIJKVMMZEKDF-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C17H14N6/c18-16-17(22-13-1-2-14-12(9-13)5-8-20-14)23-15(10-21-16)11-3-6-19-7-4-11/h1-10,20H,(H2,18,21)(H,22,23)
|
| Chemical Name |
3-N-(1H-indol-5-yl)-5-pyridin-4-ylpyrazine-2,3-diamine
|
| Synonyms |
AKN 028 AKN028AKN-028
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~413.46 mM)
|
|---|---|
| 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 | 3.3076 mL | 16.5382 mL | 33.0764 mL | |
| 5 mM | 0.6615 mL | 3.3076 mL | 6.6153 mL | |
| 10 mM | 0.3308 mL | 1.6538 mL | 3.3076 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
Copyright 2020 InvivoChem LLC | All Rights Reserved
