BAZ2-ICR
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- CAS号:
- 1665195-94-7
- 英文名:
- 4-[4-(1-methyl-1H-pyrazol-4-yl)-1-[2-(1-methyl-1H-pyrazol-4-yl)ethyl]-1H-imidazol-5-yl]-benzonitrile
- 英文别名:
- CPD1614;BAZ2-ICR;BAZ2ICR; BAZ2 ICR;BAZ2ICR,BAZ-2-ICR,BAZ2 ICR;4-[4-(1-methyl-1H-pyrazol-4-yl)-1-[2-(1-methyl-1H-pyrazol-4-yl)ethyl]-1H-imidazol-5-yl]-benzonitrile;Benzonitrile, 4-[4-(1-methyl-1H-pyrazol-4-yl)-1-[2-(1-methyl-1H-pyrazol-4-yl)ethyl]-1H-imidazol-5-yl]-
- 中文名:
- BAZ2-ICR
- 中文别名:
- 化合物 T14512
- CBNumber:
- CB63054338
- 分子式:
- C20H19N7
- 分子量:
- 357.41
- MOL File:
- 1665195-94-7.mol
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BAZ2-ICR化学性质
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沸点:
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632.8±55.0 °C(Predicted)
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密度:
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1.26±0.1 g/cm3(Predicted)
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溶解度:
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DMSO:18.58(Max Conc. mg/mL);51.99(Max Conc. mM)
DMF:20.0(Max Conc. mg/mL);55.96(Max Conc. mM)
DMF:PBS (pH 7.2) (1:1):0.5(Max Conc. mg/mL);1.4(Max Conc. mM)
Ethanol:13.37(Max Conc. mg/mL);37.41(Max Conc. mM)-
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形态:
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A crystalline solid
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酸度系数(pKa):
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4.29±0.61(Predicted)
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BAZ2-ICR性质、用途与生产工艺
BAZ2-ICR 是一种有效的，选择性的，具有细胞活性和口服活性的 BAZ2A/B 溴结构域抑制剂，IC50 分别为 130 nM 和 180 nM，Kd 分别为 109 nM 和 170 nM。BAZ2-ICR 结合 BAZ2A/B 的选择性比 CECR2 高 10-15 倍，比其他溴结构域 高 100 倍以上。BAZ2-ICR 是一种表观遗传化学探针。
IC50: 130 nM (BAZ2A) and 180 nM (BAZ2B); Kd: 109 nM (BAZ2A) and 170 nM (BAZ2A)
To investigate whether BAZ2-ICR (Compound 13) can displace BAZ2 bromodomains from chromatin in living cells, a fluorescence recovery after photobleaching (FRAP) assay utilizing GFP-tagged BAZ2A full length protein transfected into human osteosarcoma cells (U2OS) are tested. 1 μM BAZ2-ICR reduces the recovery time of the wild-type (wt) construct to a level similar to the dominant negative mutant, confirming that BAZ2-ICR inhibits BAZ2A in cells.
BAZ2-ICR (Compound 13) shows very high solubility (25 mM in D2O), a measured log D of 1.05, high stability in mouse microsomes, and permeation in the CaCo-2 model and thus a suitable profile for oral and intravenous gavage. BAZ2-ICR (5 mg/kg) shows 70% bioavailability and moderate clearance (∼50% of mouse liver blood flow) and volume of distribution.
BAZ2-ICR
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上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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| 2024/04/30 | HY-19336 | BAZ2-ICR | | 1 mg | 1590元 |
| 2024/04/30 | HY-19336 | BAZ2-ICR
BAZ2-ICR | 1665195-94-7 | 5mg | 3500元 |
1665195-94-7, BAZ2-ICR 相关搜索:
- 化合物 T14512
- 1665195-94-7
- BAZ2ICR,BAZ-2-ICR,BAZ2 ICR
- Benzonitrile, 4-[4-(1-methyl-1H-pyrazol-4-yl)-1-[2-(1-methyl-1H-pyrazol-4-yl)ethyl]-1H-imidazol-5-yl]-
- BAZ2ICR; BAZ2 ICR
- CPD1614
- BAZ2-ICR
- 4-[4-(1-methyl-1H-pyrazol-4-yl)-1-[2-(1-methyl-1H-pyrazol-4-yl)ethyl]-1H-imidazol-5-yl]-benzonitrile