AKN-028
產品名稱:AKN-028
產品描述:
產品描述 | AKN-028 is an orally active andpotent FLT3 tyrosine kinase inhibitor ( IC 50 = 6 nM). AKN-028 causes dose-dependent inhibition of FLT3 autophosphorylation. |
靶點活性 | FLT3:6 nM (IC50), CLK1:140 nM (IC50), FGFR2:1200 nM (IC50), RPS6KA:220 nM (IC50), VEGFR2:520 nM (IC50) |
體外活性 | 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. |
體內活性 | 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. |
分子量 | 302.341 |
分子式 | C17H14N6 |
CAS No. | 1175017-90-9 |
存儲
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 3.02 mg/mL (10 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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