BRD4 Inhibitor-28

• 常用名: BRD4 Inhibitor-28
• 英文名: BRD4 Inhibitor-28
• CAS号: 2468960-80-5
• 分子量: 387.43
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₃H₂₁N₃O₃
• 熔点: N/A
• 闪点: N/A

BRD4 Inhibitor-28用途

BRD4 Inhibitor-28 (Compound 18) 是一种口服活性的 BRD4 抑制剂。BRD4 Inhibitor-28 抑制 BRD40-BD1、BRD40-BD2,IC50 为 15、55 nM。 BRD4 Inhibitor-28 还抑制 BRD2-BD1、BRD3-BD1、BRDT-BD1,IC50 分别为 19、25、68 nM。BRD4 Inhibitor-28 具有抗黑色素瘤活性。

BRD4 Inhibitor-28名称

• 英文名: BRD4 Inhibitor-28

BRD4 Inhibitor-28生物活性

• 描述: BRD4 Inhibitor-28 (Compound 18) 是一种口服活性的 BRD4 抑制剂。BRD4 Inhibitor-28 抑制 BRD40-BD1、BRD40-BD2,IC50 为 15、55 nM。 BRD4 Inhibitor-28 还抑制 BRD2-BD1、BRD3-BD1、BRDT-BD1,IC50 分别为 19、25、68 nM。BRD4 Inhibitor-28 具有抗黑色素瘤活性。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> 表观遗传学 >> 表观遗传读者域
• 靶点实验:

  15, 55, 19, 25, 68 nM (BRD40-BD1, BRD40-BD2, BRD2-BD1, BRD3-BD1, BRDT-BD1BRD2-BD1, BRD3-BD1, BRDT-BD1)[1]

• 参考文献:

  [1]. Horai Y, et al. Discovery of a potent, orally available tricyclic derivative as a novel BRD4 inhibitor for melanoma. Bioorg Med Chem. 2023 Aug 26;93:117461.

BRD4 Inhibitor-28物理化学性质

• 分子式: C₂₃H₂₁N₃O₃
• 分子量: 387.43
• InChIKey: QTVSDAUHDJBCAA-UHFFFAOYSA-N
• SMILES: Cc1cc(-c2cc3c4c(c2)n(Cc2ccccc2)c(=O)n4CCO3)cn(C)c1=O

BRD4 Inhibitor-28靶点实验

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实验名称：Volume of distribution in Slc:ICR mouse at 0.5 mg/kg, iv measured for 4 to 8 hrs by L... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5372306

实验名称：Displacement of Biotin-tagged [Lys(5,8,12,16)Ac]H4(1 to 21) peptide from GST-tagged B... 来源：ChEMBL 靶标：Bromodomain-containing protein 4 External Id：CHEMBL5372307

实验名称：Oral bioavailability in Slc:ICR mouse at 1 mg/kg measured for 8 to 24 hrs by LC/MS/MS... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5372305

实验名称：AUC (0 to 24 hrs) in Slc:ICR mouse at 1 mg/kg, po measured for 8 to 24 hrs by LC/MS/M... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5372303

实验名称：Total clearance in Slc:ICR mouse at 0.5 mg/kg, iv measured for 4 to 8 hrs by LC/MS/MS... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5372300

实验名称：Stability in mouse liver microsomes assessed as intrinsic clearance measured per mg p... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5372301

实验名称：Antitumor activity against human A375.S2 cells xenografted CAnN.Cg-Foxnlnu/CrlCrlj mo... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5372314

实验名称：Apparent permeability of the compound across apical side to basolateral side in human... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5372298

实验名称：Toxicity in CAnN.Cg-Foxnlnu/CrlCrlj mouse xenografted with human A375.S2 cells assess... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5372315

实验名称：Half life in Slc:ICR mouse at 0.5 mg/kg, iv measured for 4 to 8 hrs by LC/MS/MS analy... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5372297

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