SJ1461

• 常用名: SJ1461
• 英文名: SJ1461
• CAS号: 2924546-70-1
• 分子量: 484.00
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₁H₁₈ClN₇OS₂
• 熔点: N/A
• 闪点: N/A

SJ1461用途

SJ1461是一种强效口服活性BET抑制剂。SJ1461分别以1.6nM、0.1nM、6.5nM和0.2nM的IC50值抑制BRD2(BD1),以及BRD2(BD 2)、BRD4(BD1。

SJ1461名称

• 英文名: SJ1461

SJ1461生物活性

• 描述: SJ1461是一种强效口服活性BET抑制剂。SJ1461分别以1.6nM、0.1nM、6.5nM和0.2nM的IC50值抑制BRD2(BD1),以及BRD2(BD 2)、BRD4(BD1。
• 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:

  BRD2 (BD1):1.6 nM (IC50)

  BRD2 (BD2):0.1 nM (IC50)

  BRD4 (BD1):6.5 nM (IC50)

  BRD4 (BD2):0.2 nM (IC50)

• 体外研究: SJ1461抑制 MV4-11、NALM-16、MOLM-13、HDMB03和 D283细胞的癌细胞生长,IC50分别为 20 nM、3.6 nM、10.2 nM、6.6 nM和 56.2 nM[1]
• 参考文献:

  [1]. Mladen Koravovic, et al. From PROTAC to inhibitor: Structure-guided discovery of potent and orally bioavailable BET inhibitors. Eur J Med Chem. 2023 May 5;251:115246.

SJ1461物理化学性质

• 分子式: C₂₁H₁₈ClN₇OS₂
• 分子量: 484.00

SJ1461靶点实验

查看更多实验

实验名称：Apparent volume of distribution during terminal phase in CD1 mouse at 10 mg/kg, po me... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5349039

实验名称：Oral bioavailability in CD1 mouse at 10 mg/kg measured upto 24 hrs by LC-MS/MS method 来源：ChEMBL 靶标：N/A External Id：CHEMBL5349037

实验名称：Apparent volume of distribution during terminal phase in CD1 mouse at 3 mg/kg, po mea... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5349038

实验名称：Unbound clearance in CD1 mouse at 10 mg/kg, po measured upto 24 hrs by LC-MS/MS metho... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5349035

实验名称：Oral bioavailability in CD1 mouse at 3 mg/kg measured upto 24 hrs by LC-MS/MS method 来源：ChEMBL 靶标：N/A External Id：CHEMBL5349036

实验名称：Unbound clearance in CD1 mouse at 1 mg/kg, iv measured upto 24 hrs by LC-MS/MS method 来源：ChEMBL 靶标：N/A External Id：CHEMBL5349033

实验名称：Unbound clearance in CD1 mouse at 3 mg/kg, po measured upto 24 hrs by LC-MS/MS method 来源：ChEMBL 靶标：N/A External Id：CHEMBL5349034

实验名称：Half life in CD1 mouse at 3 mg/kg, po measured upto 24 hrs by LC-MS/MS method 来源：ChEMBL 靶标：N/A External Id：CHEMBL5349031

实验名称：Half life in CD1 mouse at 10 mg/kg, po measured upto 24 hrs by LC-MS/MS method 来源：ChEMBL 靶标：N/A External Id：CHEMBL5349032

实验名称：AUClast in CD1 mouse at 10 mg/kg, po measured upto 24 hrs by LC-MS/MS method 来源：ChEMBL 靶标：N/A External Id：CHEMBL5349029

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