Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AKN-028 acetate, a novel tyrosine kinase (TK) inhibitor, is a potent, orally active FMS-like receptor tyrosine kinase 3 (FLT3) inhibitor with an IC 50 value of 6 nM. AKN-028 acetate inhibits FLT3 autophosphorylation. AKN-028 acetate induces dose-dependent cytotoxic response (mean IC 50 =1 μM). AKN-028 acetate induces apoptosis by activation of caspase 3. AKN-028 acetate can be used in research of acute myeloid leukemia (AML) [1].
Pack Size | Availability | Price/USD | Quantity |
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500 mg | 10-14 weeks | $ 1,986.00 |
Description | AKN-028 acetate, a novel tyrosine kinase (TK) inhibitor, is a potent, orally active FMS-like receptor tyrosine kinase 3 (FLT3) inhibitor with an IC 50 value of 6 nM. AKN-028 acetate inhibits FLT3 autophosphorylation. AKN-028 acetate induces dose-dependent cytotoxic response (mean IC 50 =1 μM). AKN-028 acetate induces apoptosis by activation of caspase 3. AKN-028 acetate can be used in research of acute myeloid leukemia (AML) [1]. |
In vitro | AKN-028 (0.1 nM-100 μM; 15 h; mouse embryonal fibroblasts and human acute megakaryoblastic leukemia M07 cells) acetate inhibits FLT3 and KIT autophosphorylation in a dose-dependent manner [1]. AKN-028 (10 μM; 72 h; tumor cell lines) acetate is cytotoxic to AML cell lines and induces apoptosis in the AML cell line MV4-11 [1]. Cell Cytotoxicity Assay [1] Cell Line: Tumor cell lines Concentration: 10 μM Incubation Time: 72 hours Result: Had cytotoxic activity was highest in MV4-11 and MOLM-13 (IC 50 <50 nM), followed by the three other AML cell lines (IC 50 =0.5-6 μM). Western Blot Analysis [1] Cell Line: Mouse embryonal fibroblasts either overexpressing FLT-wt, FLT3-TKD or FLT3-ITD and human acute megakaryoblastic leukemia M07 cells overexpressing KIT Concentration: 0.1 nM-100 μM Incubation Time: 15 hours Result: Inhibited FLT3 and KIT autophosphorylation. |
In vivo | AKN-028 acetate, administered at a dosage of 15 mg/kg via subcutaneous injection twice daily for a duration of six days, effectively inhibits the growth of primary AML and MV4-11 cells in male C57 black mice with MV4-11 xenografts, without impacting the animals' body weight [1]. |
Molecular Weight | 362.39 |
Formula | C19H18N6O2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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AKN-028 acetate inhibitor inhibit