AKN-028


CAS No. : 1175017-90-9

1175017-90-9
Price and Availability of CAS No. : 1175017-90-9
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Cat. No. : HY-118304
M.Wt: 302.33
Formula: C17H14N6
Purity: >98 %
Solubility: DMSO : 125 mg/mL (ultrasonic)
Introduction of 1175017-90-9 :

AKN-028, 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 inhibits FLT3 autophosphorylation. AKN-028 induces dose-dependent cytotoxic response (mean IC50=1?μM). AKN-028 induces apoptosisby activation of caspase 3. AKN-028 can be used in research of acute myeloid leukemia (AML)[1]. IC50 & Target:IC50: 6 nM (FLT3), 140 nM (CLK1), 220 nM (RPS6KA), 520 nM (VEGFR2), and 120 nM (FGFR2)[1] In Vitro:AKN-028 (0.1 nM-100 μM; 15 h; mouse embryonal fibroblasts and human acute megakaryoblastic leukemia M07 cells) inhibits FLT3 and KIT autophosphorylation in a dose-dependent manner[1].
AKN-028 (10 μM; 72 h; tumor cell lines) is cytotoxic to AML cell lines and induces apoptosis in the AML cell line MV4-11[1].
In Vivo:AKN-028 (15?mg/kg; i.h.; twice daily, for 6 days; male C57 black mice with MV4-11 xenografts) inhibits growth of primary AML and MV4-11 cells in mice[1].

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