FD1024

• 常用名: FD1024
• 英文名: FD1024
• CAS号: 1422456-47-0
• 分子量: 430.47
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₁H₂₀F₂N₄O₂S
• 熔点: N/A
• 闪点: N/A

FD1024用途

FD1024是PIM抑制剂(PIM1、2、3的IC50s:1.96、38.9、4.17 nM)。FD1024可用于急性粒细胞白血病的研究。FD1024对AML细胞株具有较强的抗增殖活性,对EOL-1、MV-4-11、KG-1、MOLM-16细胞的抗增殖能力分别为0.16μM、0.12μM、1.05μM和1.39μM。FD1024在小鼠中也具有抗肿瘤功效[1]。

FD1024名称

• 英文名: FD1024

FD1024生物活性

• 描述: FD1024是PIM抑制剂(PIM1、2、3的IC50s:1.96、38.9、4.17 nM)。FD1024可用于急性粒细胞白血病的研究。FD1024对AML细胞株具有较强的抗增殖活性,对EOL-1、MV-4-11、KG-1、MOLM-16细胞的抗增殖能力分别为0.16μM、0.12μM、1.05μM和1.39μM。FD1024在小鼠中也具有抗肿瘤功效[1]。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> JAK/STAT信号通路 >> 皮姆
• 靶点实验:

  1.96, 38.9, 4.17 nM for PIM1, 2, 3[1]

• 参考文献:

  [1]. Xiang R, et al. Discovery of a high potent PIM kinase inhibitor for acute myeloid leukemia based on N-pyridinyl amide scaffold by optimizing the fragments toward to Lys67 and Asp128/Glu171. Eur J Med Chem. 2023 Sep 5;257:115514.

FD1024物理化学性质

• 分子式: C₂₁H₂₀F₂N₄O₂S
• 分子量: 430.47
• InChIKey: SYEYZQUZNVVCNN-UHFFFAOYSA-N
• SMILES: NC1CCC(Oc2ccncc2NC(=O)c2csc(-c3c(F)cccc3F)n2)CC1

FD1024靶点实验

查看更多实验

实验名称：Inhibition of S6 phosphorylation in human EOL1 cells incubated for 24 hrs by Western ... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5621638

实验名称：Inhibition of 4EBP1 phosphorylation in human EOL1 cells incubated for 24 hrs by Weste... 来源：ChEMBL 靶标：Eukaryotic translation initiation factor 4E-binding protein 1 External Id：CHEMBL5621639

实验名称：Inhibition of BAD phosphorylation in human EOL1 cells incubated for 24 hrs by Western... 来源：ChEMBL 靶标：Bcl2-associated agonist of cell death External Id：CHEMBL5621640

实验名称：Inhibition of wild type full length N-terminal his-tagged PIM1 (1 to 313 residues) (u... 来源：ChEMBL 靶标：Serine/threonine-protein kinase pim-1 External Id：CHEMBL5621598

实验名称：Antiproliferative activity against human EOL1 cells assessed as reduction in cell via... 来源：ChEMBL 靶标：EOL1 External Id：CHEMBL5621599

实验名称：Inhibition of N-terminal GST-tagged PIM2 (1 to 311 residues) (unknown origin) express... 来源：ChEMBL 靶标：Serine/threonine-protein kinase pim-2 External Id：CHEMBL5621600

实验名称：Inhibition of wild type N-terminal GST-tagged PIM3 (1 to 326 residues) (unknown origi... 来源：ChEMBL 靶标：Serine/threonine-protein kinase pim-3 External Id：CHEMBL5621601

实验名称：Half life in Sprague-Dawley rat at 1 mg/kg, iv measured upto 24 hrs by LC/MS-MS analy... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5621605

实验名称：Clearance in Sprague-Dawley rat at 1 mg/kg, iv measured upto 24 hrs by LC/MS-MS analy... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5621606

实验名称：Volume of distribution at steady state in Sprague-Dawley rat at 1 mg/kg, iv measured ... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5621607

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