AKN-028 structure
|
Common Name | AKN-028 | ||
---|---|---|---|---|
CAS Number | 1175017-90-9 | Molecular Weight | 302.33300 | |
Density | N/A | Boiling Point | N/A | |
Molecular Formula | C17H14N6 | Melting Point | N/A | |
MSDS | N/A | Flash Point | N/A |
Use of AKN-028AKN-028 is an orally active and potent FLT3 tyrosine kinase inhibitor (IC50 = 6 nM). AKN-028 causes dose-dependent inhibition of FLT3 autophosphorylation[1]. |
Name | 3-N-(1H-indol-5-yl)-5-pyridin-4-ylpyrazine-2,3-diamine |
---|---|
Synonym | More Synonyms |
Description | AKN-028 is an orally active and potent FLT3 tyrosine kinase inhibitor (IC50 = 6 nM). AKN-028 causes dose-dependent inhibition of FLT3 autophosphorylation[1]. |
---|---|
Related Catalog | |
Target |
FLT3:6 nM (IC50) CLK1:140 nM (IC50) RPS6KA:220 nM (IC50) VEGFR2:520 nM (IC50) FGFR2:1200 nM (IC50) Caspase 3 |
In Vitro | AKN-028 triggers apoptosis in MV4-11 by activation of caspase 3[1]. AKN-028 (10 μM) is cytotoxic to AML cell lines and induces apoptosis in the AML cell line MV4-11[1]. Cell Cytotoxicity Assay[1] Cell Line: AML cell line MV4-11. Concentration: 10 μM. Incubation Time: 24 h. Result: Was cytotoxic to primary AML cells, irrespective of FLT3 mutation status and quantitative FLT3 expression. |
In Vivo | AKN-028 (15 mg/kg, Subcutaneously injection twice daily) exhibits anti-tumor activities for acute myeloid leukemia (AML) models[1]. Animal Model: Mice based AML and MV4-11 cells[1]. Dosage: 15 mg/kg. Administration: Subcutaneously injection twice daily. Result: Inhibited net growth of one of the primary AML samples (UPN26) in vivo and furthermore reduced the tumor mass of MV4-11 cell line. |
References |
Molecular Formula | C17H14N6 |
---|---|
Molecular Weight | 302.33300 |
Exact Mass | 302.12800 |
PSA | 95.74000 |
LogP | 3.34880 |
akn-028 |
unii-y66is3cs0r |