AKN-028

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

AKN-028 是一种口服有效的 FLT3 酪氨酸激酶抑制剂 (IC 50 = 6 nM)。 AKN-028 会导致 FLT3 自磷酸化的剂量依赖性抑制。

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.(In Vitro):AKN-028 triggers apoptosis in MV4-11 by activation of caspase 3 . AKN-028 (10 μM) is cytotoxic to AML cell lines and induces apoptosis in the AML cell line MV4-11 . Cell Cytotoxicity Assay 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 . Animal Model: Mice based AML and MV4-11 cells . 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.

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.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. Western Blot Analysis 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.Cell Cytotoxicity Assay 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).

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. Animal Model:Male C57 black mice with MV4-11 xenografts Dosage:15 mg/kg Administration:Subcutaneous injection; twice daily, for 6 days Result:Inhibited tumor growth and did not affect body weight.

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Angiogenesis

FLT

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1175017-90-9

302.33

C17H14N6

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (413.46 mM)

NC1=NC=C(N=C1NC1=CC=C2NC=CC2=C1)C1=CC=NC=C1

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(-20℃)

With Ice Pack

≥ 2 years