AKN-028

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

AKN-028 

AKN-028 是具有口服活性的酪氨酸激酶的抑制剂 (TKI)，是 FLT3 的抑制剂，其 IC50 值为 6 nM。AKN-028 可剂量依赖性的诱导 FLT3 的自磷酸化。

AKN-028

AKN-028 Chemical Structure

CAS No. : 1175017-90-9

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生物活性

AKN-028 is an orally active and potent FLT3 tyrosine kinase inhibitor (IC50 = 6 nM). AKN-028 causes dose-dependent inhibition of FLT3 autophosphorylation[1].

IC50 & Target

Caspase 3

 

FLT3

6 nM (IC50)

CLK1

140 nM (IC50)

RPS6KA

220 nM (IC50)

FGFR2

1200 nM (IC50)

VEGFR2

520 nM (IC50)

体外研究
(In Vitro)

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究
(In Vivo)

AKN-028 (15 mg/kg, Subcutaneously injection twice daily) exhibits anti-tumor activities for acute myeloid leukemia (AML) models[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Clinical Trial

分子量

302.33

Formula

C17H14N6
CAS 号

1175017-90-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. A Eriksson, et al. The Novel Tyrosine Kinase Inhibitor AKN-028 Has Significant Antileukemic Activity in Cell Lines and Primary Cultures of Acute Myeloid Leukemia. Blood Cancer J. 2012 Aug 3;2(8):e81.

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