1. Protein Tyrosine Kinase/RTK Stem Cell/Wnt MAPK/ERK Pathway PI3K/Akt/mTOR Apoptosis
  2. FLT3 ERK Akt Apoptosis
  3. FLT3-IN-34

FLT3-IN-34 是一种 FLT3 抑制剂,具有 IC50 值为 1.4 nM。FLT3-IN-34 阻断 FLT3 及其下游信号分子 AKTERK1/2 的磷酸化。FLT3-IN-34 在 FLT3-ITD 阳性的 MV4-11 细胞中诱导浓度依赖性的 G0/G1 期阻滞和轻度凋亡 ( apoptosis)。FLT3-IN-34 对 FLT3-ITD 阳性的 MV4-11 细胞 (IC50 = 14.95 nM) 和 MOLM-13 细胞 (IC50 = 18.5 nM) 显示出强效的抗增殖活性。FLT3-IN-34 可用于 FLT3 阳性急性髓系白血病 (AML) 的研究。

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FLT3-IN-34

FLT3-IN-34 Chemical Structure

CAS No. : 3020729-11-4

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生物活性

FLT3-IN-34 is a FLT3 inhibitor, with an IC50 value of 1.4 nM. FLT3-IN-34 blocks the phosphorylation of FLT3 and its downstream signaling molecules AKT and ERK1/2. FLT3-IN-34 induces concentration-dependent G0/G1 phase arrest and mild apoptosis in FLT3-ITD-positive MV4-11 cells. FLT3-IN-34 shows potent anti-proliferative activity against FLT3-ITD-positive MV4-11 cells (IC50 = 14.95 nM) and MOLM-13 (IC50 = 18.5 nM). FLT3-IN-34 can be used for the study of FLT3-positive acute myeloid leukemia (AML)[1].

体外研究
(In Vitro)

FLT3-IN-34 (Compound ZY12) 对 FLT3-ITD 激酶显示出极佳的抑制效能,其 IC50 值为 1.4 nM[1]
FLT3-IN-34 对 FLT3-ITD 阳性的 MV4-11 细胞 (IC50 = 14.95 nM) 和 MOLM-13 细胞 (IC50 = 18.5 nM) 显示出强效的抗增殖活性[1]
FLT3-IN-34 (5-20 nM, 24 h) 以浓度依赖方式诱导 MV4–11 细胞的 G0/G1 期阻滞,并诱导 MV4-11 细胞凋亡[1]
FLT3-IN-34 (5-20 nM) 显著阻断 MV4-11 和 MOLM-13 细胞中 FLT3、AKT 和 ERK1/2 的磷酸化,抑制 FLT3 信号通路[1]

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

Cell Cycle Analysis[1]

Cell Line: MV4-11 cells
Concentration: 5, 10, 20 nM
Incubation Time: 24 h
Result: Induced G0/G1 phase arrest of MV4–11 cells and decreases the percentage of cells in S and G2/M phases.

Apoptosis Analysis[1]

Cell Line: MV4-11 cells
Concentration: 5, 10, 20 nM
Incubation Time: 24 h
Result: Induced MV4–11 cell apoptosis.
体内研究
(In Vivo)

FLT3-IN-34 (Compound ZY12) (30 mg/kg,口服,每日一次,10 天) 未能在 4-6 周龄的 BALB/c-nu 小鼠中携带 MV4-11 皮下异种移植瘤的情况下明显抑制肿瘤生长[1]

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

Animal Model: MV4-11 cells was subcutaneously implanted into the mid-lateral axilla of 4-6 weeks old BALB/c-nu mice[1]
Dosage: 30 mg/kg
Administration: p.o., once daily, 10 days
Result: Failed to obviously inhibit tumor growth (TGI=8.55%) in mice bearing MV4-11 subcutaneous xenografts.
分子量

417.46

Formula

C23H23N5O3

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-34
目录号:
HY-178020
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