2. Protein Tyrosine Kinase/RTK Apoptosis PI3K/Akt/mTOR Stem Cell/Wnt MAPK/ERK Pathway JAK/STAT Signaling
  3. FLT3 Apoptosis Akt ERK PI3K STAT
  4. FLT3-IN-36

FLT3-IN-36 是一种强效的 FLT3 抑制剂。FLT3-IN-36 对 FLT3 突变的急性髓系白血病 (AML) 细胞具有抗肿瘤活性。FLT3-IN-36 可诱导细胞周期阻滞、降低线粒体膜电位并诱导细胞凋亡 (apoptosis)，从而下调 FLT3 及其下游蛋白 (包括 AKT、ERK、PI3K 和 STAT5) 的表达。FLT3-IN-36 可用于 AML 研究。

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FLT3-IN-36

FLT3-IN-36 Chemical Structure

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FLT3-IN-36 相关抗体

Top Publications Citing Use of Products

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STAT3 STAT5 STAT6 STAT1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FLT3-IN-36 is a potent FLT3 inhibitor. FLT3-IN-36 exhibits antitumor activity against FLT3-mutated acute myeloid leukemia (AML) cells. FLT3-IN-36 induces cell cycle arrest, reduces mitochondrial membrane potential, and induces apoptosis, downregulating FLT3 and downstream protein expression (including AKT, ERK, PI3K, and STAT5). FLT3-IN-36 can be used for AML research[1].

体外研究
(In Vitro)

FLT3-IN-36 (compound 8h) (24 小时) 对 FLT3 突变型 AML 细胞表现出选择性抗增殖活性，IC50 值分别为 2.04 μM (MV4-11) 和 3.25 μM (MOLM-13)，而对 FLT3 野生型细胞 (如 THP-1、U937 和 OCI-AML2) 的抑制作用则显著较弱 (IC50 值分别为 19.59 μM、91.49 μM 和 55.38 μM)[1]。
FLT3-IN-36 (0.1-100 μM，24 小时) 以时间和剂量依赖的方式抑制 MV4-11 细胞的生长，同时对正常 HK-2 和 HepRG 细胞的细胞毒性较低[1]。
FLT3-IN-36 (1-10 μM，24 小时) 以剂量依赖的方式诱导 MV4-11 细胞凋亡、G2/M 期细胞周期阻滞并降低线粒体膜电位[1]。
FLT3-IN-36 (0-10 μM，24 小时) 通过下调 FLT3 蛋白水平并抑制其下游信号通路 (包括 AKT、ERK、PI3K 和 STAT5 等关键效应分子) 来抑制 MV4-11 细胞的生长[1]。
FLT3-IN-36 与 FLT3 的 ATP 结合口袋结合良好，并且仅与活性构象铰链区的 Glu692 和 Cys694 残基相互作用[1]。
FLT3-IN-36 (1-10 μM) 直接靶向 FLT3 激酶，在 10 μM 时对 FLT3-ITD 激酶活性表现出 58% 的抑制作用[1]。

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

FLT3-IN-36 相关抗体:

Cell Cycle Analysis[1]

Cell Line: MV4-11 cells
Concentration: 1, 2.5 and 5 μM
Incubation Time: 24 h
Result: Significantly increased the G2/M phase arrest in MV4-11.
Induced the G2/M phase arrest at moderate concentration with a dose-dependent manner after treatment for 24 h.

Cell Viability Assay[1]

Cell Line: MV4-11, HK-2 and HepRG cells
Concentration: 0.1, 1, 2, 4, 8, 10, 16, 50, and 100 μM
Incubation Time: 24 and 48 h
Result: Decreased MV4-11 cell viability in a time- and dose-dependent manner.
Showed low cytotoxicity in normal HK-2 and HepRG cells.

Western Blot Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0, 2.5, 5, and 10 μM
Incubation Time: 24 h
Result: Promoted the cleavage and activation of Caspase-3 (evidenced by increased levels of cleaved Caspase-3).
Resulted in no obvious changes for the levels of Bcl-2 and Bax.
Caused the decrease of the downstream-related protein levels, including AKT, ERK, PI3K and STAT5.

Apoptosis Analysis[1]

Cell Line: MV4-11 cells
Concentration: 1, 2.5 and 5 μM
Incubation Time: 24 h
Result: Induced apoptosis in MV4-11 cells with a dose-dependent manner.
分子量

331.36

Formula

C21H17NO3
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-36 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • 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-36FLT3ApoptosisAktERKPI3KSTATCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3PKBProtein kinase BExtracellular signal regulated kinasesPhosphoinositide 3-kinaseantitumorAMLTHP-1U937OCI-AML2MV4-11MOLM-13Inhibitorinhibitorinhibit

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