2. Protein Tyrosine Kinase/RTK Epigenetics Cell Cycle/DNA Damage Apoptosis Metabolic Enzyme/Protease Immunology/Inflammation NF-κB
  3. FLT3 HDAC Apoptosis Reactive Oxygen Species (ROS)
  4. FLT3/HDAC-IN-3

FLT3/HDAC-IN-3 是一种 FLT3 和 HDAC 的双重抑制剂。FLT3/HDAC-IN-3 能强力抑制 FLT3 (IC50 = 14 nM)、HDAC1 (IC50 = 27 nM)、HDAC6 (IC50 = 20 nM) 以及 FLT3D853Y(IC50 = 55 nM)，对 HDAC8 表现出弱活性，但对 HDAC4 无活性。FLT3/HDAC-IN-3 具有激酶选择性、血浆稳定性以及在人肝微粒体中的稳定性。FLT3/HDAC-IN-3 在多种血液恶性肿瘤细胞系中表现出抗增殖作用。在 Jeko-1 异种移植模型中，FLT3/HDAC-IN-3 显示出抑制效果，且未观察到显著毒性。FLT3/HDAC-IN-3 可用于血液系统恶性肿瘤的研究。

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FLT3/HDAC-IN-3

FLT3/HDAC-IN-3 Chemical Structure

CAS No. : 2864394-30-7

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FLT3/HDAC-IN-3 相关抗体

Top Publications Citing Use of Products

查看 HDAC 亚型特异性产品:

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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FLT3/HDAC-IN-3 is a dual inhibitor of FLT3 and HDAC. FLT3/HDAC-IN-3 potently inhibits FLT3 (IC50 = 14 nM), HDAC1 (IC50 = 27 nM), HDAC6 (IC50 = 20 nM), and FLT3D853Y (IC50 = 55 nM), exhibits weak activity against HDAC8, and shows no activity against HDAC4. FLT3/HDAC-IN-3 possesses kinase selectivity, plasma stability, and stability in human liver microsomes. FLT3/HDAC-IN-3 demonstrates anti-proliferative effects in a variety of hematological malignancy cell lines. FLT3/HDAC-IN-3 shows efficacy in the Jeko-1 xenograft model without observed significant toxicity. FLT3/HDAC-IN-3 can be used in the study of hematological malignancies[1].

IC50 & Target

FLT3

14 nM (IC50)

HDAC6

20 nM (IC50)

HDAC1

27 nM (IC50)

FLT3D835Y

55 nM (IC50)

HDAC8

2800 nM (IC50)

HDAC4

>10000 nM (IC50)

体外研究
(In Vitro)

FLT3/HDAC-IN-3 (compound 6s) (作用 72 小时) 可强效抑制 MV-4-11 细胞 (IC50 = 29 nM) 和 Jeko-1 细胞 (IC50 = 99 nM) 的增殖，且具有良好的肿瘤细胞选择性 (在 HaCaT 细胞中 IC50 = 80 μM)[1]。
FLT3/HDAC-IN-3 (0-1000 nM；作用 72 h) 以剂量依赖的方式抑制 FLT3 和 STAT5 的磷酸化，提高 H3Ac 水平，并在 MV-4-11 细胞中上调 Bax[1]。
FLT3/HDAC-IN-3 (0-1000 nM; 72 h) 可在 MV-4-11 和 Jeko-1 细胞中诱导剂量依赖性细胞死亡、ROS 蓄积并降低线粒体膜电位[1]。
FLT3/HDAC-IN-3 (0-1000 nM；作用 48 h 或 72 h) 可在 MV-4-11 和 Jeko-1 细胞中诱导时间和剂量依赖性的细胞凋亡[1]。
FLT3/HDAC-IN-3 (0-1000 nM；作用 72 h) 以剂量依赖的方式将 MV-4-11 细胞的细胞周期阻滞于 G2 期[1]。
FLT3/HDAC-IN-3 (200 μM；0–72 h) 在大鼠血浆中表现出良好的血浆稳定性，72 h 后保留率为 67.8%[1]。
FLT3/HDAC-IN-3 在人肝微粒体中表现出良好的代谢稳定性，其半衰期为 165 min，内在清除率为 7.56 mL/min/kg[1]。

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

FLT3/HDAC-IN-3 相关抗体:

Western Blot Analysis[1]

Cell Line: MV-4-11 cells
Concentration: 0 nM, 50 nM, 250 nM, 1000 nM
Incubation Time: 72 h
Result: Dose-dependently inhibited phosphorylated FLT3 and p-STAT5; increased acetylated histone H3 (H3Ac) levels in a concentration-dependent manner, with higher H3Ac accumulation at 250 nM compared to SAHA at the same concentration; upregulated pro-apoptotic protein Bax in a dose-dependent manner.

Cell Cytotoxicity Assay[1]

Cell Line: MV-4-11, Jeko-1 cells
Concentration: 0 nM, 50 nM, 250 nM, 1000 nM
Incubation Time: 72 h
Result: Induced a dose-dependent increase in red fluorescence (dead cells) and decrease in green fluorescence (live cells) in both MV-4-11 and Jeko-1 cells.

Apoptosis Analysis[1]

Cell Line: MV-4-11, Jeko-1 cells
Concentration: 0 nM, 50 nM, 250 nM, 1000 nM
Incubation Time: 48 h or 72 h
Result: Induced apoptosis in a time- and dose-dependent manner; at 72 h, induced 47.7% apoptosis at 250 nM and up to 75% apoptosis at 1000 nM in MV-4-11 cells, with effects comparable to SAHA + Tandutinib combination treatment; also induced dose-dependent apoptosis in Jeko-1 cells.

Cell Cycle Analysis[1]

Cell Line: MV-4-11 cells
Concentration: 0 nM, 50 nM, 250 nM, 1000 nM
Incubation Time: 72 h
Result: Effectively arrested the cell cycle in the G2 phase in a dose-dependent manner
药代动力学
(Parmacokinetics)
Species Dose Route Indicator value
Rat[1] 5 mg/kg i.v. T1/2 0.54 h
Rat[1] 5 mg/kg i.v. Tmax 0.083 h
Rat[1] 5 mg/kg i.v. Cmax 86.00 ng/mL
Rat[1] 5 mg/kg i.v. AUC0-t 48.70 ng·h/mL
Rat[1] 5 mg/kg i.v. AUC0-∞ 52.20 ng·h/mL
Rat[1] 5 mg/kg i.v. MRT0-t 0.48 h
Rat[1] 5 mg/kg i.v. MRT0-∞ 0.63 h
Rat[1] 30 mg/kg p.o. T1/2 2.21 h
Rat[1] 30 mg/kg p.o. Tmax 0.50 h
Rat[1] 30 mg/kg p.o. Cmax 17.80 ng/mL
Rat[1] 30 mg/kg p.o. AUC0-t 33.90 ng·h/mL
Rat[1] 30 mg/kg p.o. AUC0-∞ 60.90 ng·h/mL
Rat[1] 30 mg/kg p.o. MRT0-t 1.68 h
Rat[1] 30 mg/kg p.o. MRT0-∞ 4.49 h
Rat[1] 30 mg/kg p.o. F 19.50 %
Rat[1] 30 mg/kg i.p. T1/2 1.14 h
Rat[1] 30 mg/kg i.p. Tmax 0.33 h
Rat[1] 30 mg/kg i.p. Cmax 137 ng/mL
Rat[1] 30 mg/kg i.p. AUC0-t 148 ng·h/mL
Rat[1] 30 mg/kg i.p. AUC0-∞ 153 ng·h/mL
Rat[1] 30 mg/kg i.p. MRT0-t 0.96 h
Rat[1] 30 mg/kg i.p. MRT0-∞ 1.09 h
Rat[1] 30 mg/kg i.p. F 49.00 %
体内研究
(In Vivo)

FLT3/HDAC-IN-3 (compound 6s) (15-30 mg/kg；腹腔注射；每日一次；连续 15 天) 在 Jeko-1 异种移植小鼠中呈剂量依赖性地抑制套细胞淋巴瘤生长，在 30 mg/kg 剂量下的肿瘤生长抑制率 (TGI) 达 53.34%，且未观察到毒性[1]。

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

Animal Model: NOD/SCID mice injected with Jeko-1 cells[1]
Dosage: 15 mg/kg; 30 mg/kg
Administration: i.p.; daily; 15 days
Result: Achieved 37.14% TGI and 0.47 g average tumor weight at 15 mg/kg; achieved 53.34% TGI and 0.39 g average tumor weight at 30 mg/kg.
Induced more severe tumor cell necrosis than control or SAHA groups at 30 mg/kg.
Caused no significant weight loss or abnormalities in drinking, diet, or activity at 30 mg/kg.
分子量

445.53

Formula

C22H32FN7O2
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

FLT3/HDAC-IN-3 相关分类

  • 摩尔计算器

  • 稀释计算器

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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/HDAC-IN-32864394-30-7FLT3HDACApoptosisReactive Oxygen Species (ROS)Cluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Histone deacetylasesHDAC4xenograft modelJeko-1 cellsHDAC6FLT3D835YMV-4-11 cellshematologic malignanciesHDAC1HDAC8Inhibitorinhibitorinhibit

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