AKN-028 acetate |
| Catalog No.GC66451 |
AKN-028 acetate, a novel tyrosine kinase (TK) inhibitor, is a potent, orally active FMS-like receptor tyrosine kinase 3 (FLT3) inhibitor with an IC50 value of 6nM. AKN-028 acetate inhibits FLT3 autophosphorylation. AKN-028 acetate induces dose-dependent cytotoxic response (mean IC50=1μM). AKN-028 acetate induces apoptosisby activation of caspase 3. AKN-028 acetate can be used in research of acute myeloid leukemia (AML).
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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IC50: 6 nM (FLT3), 140 nM (CLK1), 220 nM (RPS6KA), 520 nM (VEGFR2), and 120 nM (FGFR2)[1]
AKN-028 acetate, a novel tyrosine kinase (TK) inhibitor, is a potent, orally active FMS-like receptor tyrosine kinase 3 (FLT3) inhibitor with an IC50 value of 6 nM. AKN-028 acetate inhibits FLT3 autophosphorylation. AKN-028 acetate induces dose-dependent cytotoxic response (mean IC50=1 μM). AKN-028 acetate induces apoptosisby activation of caspase 3. AKN-028 acetate can be used in research of acute myeloid leukemia (AML)[1].
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 (IC50<50 nM), followed by the three other AML cell lines (IC50=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. |
AKN-028 (15 mg/kg; i.h.; twice daily, for 6 days; male C57 black mice with MV4-11 xenografts) acetate inhibits growth of primary AML and MV4-11 cells in mice[1].
| Animal Model: | Male C57 black mice with MV4-11 xenografts[1] |
| Dosage: | 15 mg/kg |
| Administration: | Subcutaneous injection; twice daily, for 6 days |
| Result: | Inhibited tumor growth and did not affect body weight. |
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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