2. Protein Tyrosine Kinase/RTK Stem Cell/Wnt JAK/STAT Signaling PI3K/Akt/mTOR MAPK/ERK Pathway Apoptosis
  3. FLT3 STAT Akt ERK Apoptosis
  4. FLT3-IN-41

FLT3-IN-41 是一种高效的 FLT3 抑制剂。FLT3-IN-41 对人源 FLT3-ITD 和 FLT3-WT 的 IC50 值分别为 3.16 nM 和 294.7 nM。FLT3-IN-41 通过结合 FLT3-ITD 和 FLT3-WT 的 ATP 结合口袋，与铰链区残基及 Phe830 形成氢键，从而抑制 STAT5、Akt 和 Erk 信号通路。FLT3-IN-41 能够诱导 FLT3-ITD 阳性的急性髓系白血病细胞在 G2/M 期阻滞并促进细胞凋亡 (apoptosis)，展现出显著的抗增殖活性。FLT3-IN-41 可作为研究急性髓系白血病的重要工具。

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FLT3-IN-41

FLT3-IN-41 Chemical Structure

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FLT3-IN-41 相关抗体

Top Publications Citing Use of Products

查看 STAT 亚型特异性产品:

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STAT3 STAT5 STAT6 STAT1

查看 Akt 亚型特异性产品:

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Akt Akt1 Akt2 Akt3

查看 ERK 亚型特异性产品:

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ERK ERK1 ERK2 ERK5 ERK8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FLT3-IN-41 is a highly potent FLT3 inhibitor. The IC50 values of FLT3-IN-41 against human FLT3-ITD and FLT3-WT are 3.16 nM and 294.7 nM, respectively. By binding to the ATP-binding pockets of FLT3-ITD and FLT3-WT and forming hydrogen bonds with hinge region residues and Phe830, FLT3-IN-41 inhibits the STAT5, Akt and Erk signaling pathways. FLT3-IN-41 induces G2/M phase arrest and promotes apoptosis (apoptosis) in FLT3-ITD-positive acute myeloid leukemia cells, exhibiting significant antiproliferative activity. FLT3-IN-41 serves as a valuable tool for the study of acute myeloid leukemia[1].

IC50 & Target

STAT5

 

体外研究
(In Vitro)

FLT3-IN-41 (compound 35) (1-100 nM；24 h) 剂量依赖性诱导 FLT3-ITD 突变的 MV4-11 细胞发生 G2/M 期细胞周期阻滞[1]。
FLT3-IN-41 (1-100 nM；24 h) 剂量依赖性诱导 FLT3-ITD 突变的 MV4-11 细胞凋亡[1]。
FLT3-IN-41 (400 nM；0-24 h) 时间依赖性下调 FLT3-ITD 突变的 MV4-11 细胞中 STAT5 下游靶基因 Osm、Bcl-2、Pim-1 和 Cis 的 mRNA 表达水平[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

FLT3-IN-41 相关抗体:

Cell Cycle Analysis[1]

Cell Line: FLT3-ITD mutant MV4-11 cells
Concentration: 1 nM, 10 nM, 100 nM
Incubation Time: 24 h
Result: Induced a dose-dependent increase in the G2/M population in MV4-11 cells.
Resulted in 1.39-, 1.81-, and 3.72-fold increases in the percentage of cells in G2/M phase compared with the untreated controls, respectively.
This effect was distinct from that of midostaurin, which showed different cell cycle arrest patterns in previous reports.

Real Time qPCR[1]

Cell Line: FLT3-ITD mutant MV4-11 cells
Concentration: 400 nM
Incubation Time: 0 h, 2 h, 24 h
Result: Significantly reduced the mRNA expression levels of STAT5 transcriptionally regulated genes in a time-dependent manner.
The expression levels of Osm, Bcl-2, Pim-1, and Cis were markedly downregulated after 2 h and 24 h.
分子量

469.45

Formula

C26H19N3O6
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.
纯度 & 产品资料
参考文献

FLT3-IN-41 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

FLT3-IN-41FLT3STATAktERKApoptosisCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3PKBProtein kinase BExtracellular signal regulated kinasesPhe830acute myeloid leukemia cellsATP-binding pocketErkG2/M cell-cycle arrestSTAT5hinge region residuesFLT3-WTFLT3-ITDInhibitorinhibitorinhibit

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