1. Protein Tyrosine Kinase/RTK
  2. FLT3
  3. FLT3-IN-40

FLT3-IN-40 (compound 1) 是一种 I 型 ATP 竞争性 FLT3 抑制剂,其 IC50 为 16.26 nM。FLT3-IN-40 可降低 FLT3 的自身磷酸化水平及下游 ERK 的磷酸化水平。FLT3-IN-40 具有抗增殖、细胞周期调节和诱导凋亡的活性。FLT3-IN-40 可用于急性髓系白血病的相关研究。

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FLT3-IN-40

FLT3-IN-40 Chemical Structure

CAS No. : 3075541-07-7

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FLT3-IN-40 (compound 1) is a type I ATP-competitive FLT3 inhibitor with an IC50 of 16.26 nM. FLT3-IN-40 reduces the autophosphorylation level of FLT3 and the phosphorylation level of downstream ERK. FLT3-IN-40 exhibits antiproliferative, cell cycle regulatory and apoptosis-inducing activities. FLT3-IN-40 can be used in research related to acute myeloid leukemia[1].

体外研究
(In Vitro)

FLT3-IN-40 (compound 1) (0.00001-100 nM; sufficient to measure antiproliferative effects) 可强效抑制 MV4-11 细胞增殖,其 IC50 为 0.0021 nM,呈现出渐进的双相剂量反应特征[1]
FLT3-IN-40 (0.001-10 nM) 是一种 ATP 竞争性 I 型 FLT3 抑制剂,可抑制纯化的 FLT3 激酶,其 IC50 为 16.26 nM;在抑制 p-ERK 时,对 MV4-11 细胞中 FLT3 通路信号传导的 IC50 为 0.80 nM[1]
FLT3-IN-40 (足以检测抗增殖效应) 可抑制 Molm14 细胞增殖,其 IC50 为 1.42 nM;而对缺乏 FLT3 激活突变的 K562 细胞 (IC50 1583 nM) 和 Ba/F3 细胞 (IC50 8467 nM),该化合物的抗增殖活性则弱得多[1]
FLT3-IN-40 (1 pM-10 nM; 72 h) 在皮摩尔浓度下对 MV4-11 细胞仅诱导极少量细胞凋亡,但在 10 nM 处理 72 h 后可显著触发早期 (17.3%) 和晚期 (10.3%) 细胞凋亡[1]
FLT3-IN-40 (1 pM-10 nM; 72 h) 会在皮摩尔浓度下诱导 MV4-11 细胞出现中度 G1 期阻滞稳定,并在 10 nM 处理 72 h 后诱导强烈的 G1 期细胞周期阻滞[1]
FLT3-IN-40 (1 nM; 10 nM) 具有高激酶选择性,在 1 nM 和 10 nM 浓度下测试的 96 种激酶中,仅与 FLT3 发生强结合[1]

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

Cell Proliferation Assay[1]

Cell Line: MV4-11 (FLT3-ITD positive acute myeloid leukemia) cells
Concentration: 0.00001-100 nM
Incubation Time: sufficient to measure antiproliferative effects
Result: Inhibited MV4-11 cell proliferation with an IC50 of 0.0021 nM (or 2.13 pM).
Achieved ~50% inhibition at 2 pM and >90% inhibition at 20 nM, with a gradual, biphasic dose-response curve.

Apoptosis Analysis[1]

Cell Line: MV4-11 cells
Concentration: 1 pM-10 nM
Incubation Time: 72 h
Result: Induced early apoptotic cell percentages of 2.1%, 2.3%, 3.4%, and 4.8% at 1 pM, 10 pM, 100 pM, and 1 nM respectively, with minimal late apoptosis.
Triggered early apoptotic cell percentage of 17.3% and late apoptotic cell percentage of 10.3% at 10 nM, showing a marked increase in apoptosis at nanomolar concentrations.

Cell Cycle Analysis[1]

Cell Line: MV4-11 cells
Concentration: 1 pM-10 nM
Incubation Time: 72 h
Result: Increased G1 phase cell percentages to 52.4%, 53.5%, and 54.5% at 1 pM, 10 pM, and 100 pM respectively (compared to 47.2% for DMSO control).
Increased G1 phase percentage to 58.1% at 1 nM, and to 68.7% at 10 nM with a corresponding decrease in G2 phase from 8.93% at 1 nM to 3.01% at 10 nM.
分子量

426.47

Formula

C24H22N6O2

CAS 号
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
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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.

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产品名称:
FLT3-IN-40
目录号:
HY-182004
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