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AKN-028 is an orally active and potent FLT3 tyrosine kinase inhibitor ( IC 50 = 6 nM). AKN-028 causes dose-dependent inhibition of FLT3 autophosphorylation.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $53 | In Stock | |
10 mg | $88 | In Stock | |
25 mg | $187 | In Stock | |
50 mg | $294 | In Stock | |
100 mg | $429 | In Stock |
Description | AKN-028 is an orally active and potent FLT3 tyrosine kinase inhibitor ( IC 50 = 6 nM). AKN-028 causes dose-dependent inhibition of FLT3 autophosphorylation. |
Targets&IC50 | FGFR2:1200 nM (IC50), VEGFR2:520 nM (IC50), RPS6KA:220 nM (IC50), CLK1:140 nM (IC50), FLT3:6 nM (IC50) |
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. |
Molecular Weight | 302.33 |
Formula | C17H14N6 |
Cas No. | 1175017-90-9 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 20 mg/mL 66.15 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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