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CPI203 (CPI 203) 是一种有效的 BET 溴结构域抑制剂(BRD4 的 IC50:37 nM)。
CPI203 (CPI 203) 是一种有效的 BET 溴结构域抑制剂(BRD4 的 IC50:37 nM)。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 193 | 现货 | |
5 mg | ¥ 416 | 现货 | |
10 mg | ¥ 736 | 现货 | |
25 mg | ¥ 1,160 | 现货 | |
50 mg | ¥ 2,130 | 现货 | |
100 mg | ¥ 3,850 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 416 | 现货 |
产品描述 | CPI203 (CPI 203) is an effective BET bromodomain inhibitor (IC50: 37 nM for BRD4). |
靶点活性 | BET BD:37 nM |
体外活性 | CPI203 在体外及细胞内抑制BRD4,而不影响其体外的激酶活性。[1] CPI203 在分析的所有9个MCL细胞系中显示出细胞静止效果,GI50范围从0.06到0.71 μM,对健康捐献者的正常PBMCs具有低细胞性毒性。此外,lenalidomide和CPI203通过靶向IRF4和MYC,有效激活对bortezomib有抵抗性的MCL细胞中的细胞死亡程序。[2] |
激酶实验 | BRD4 α-screen assay: The BRD4 α-screen assay is a proximity-based assay using a tetraacteylated H4 peptide and the isolated bromodomain 1 of human BRD4. IC50 values are calculated using a 10-point serial dilution of BET inhibitor. |
细胞实验 | MCL primary cells and cell lines are incubated as indicated with lenalidomide and/or CPI203. MTT is added for 2-6 additional hours before spectrophotometric measurement. Each measurement is made in triplicate. Values are represented using untreated control cells. The GI50 is calculated as the concentration that produced 50 % growth inhibition. Combination indexes (CIs) are calculated by using the Calcusyn software version 2.0. The interaction between two drugs is considered synergistic when CI <1. (Only for Reference) |
别名 | CPI-203, CPI 203 |
分子量 | 399.9 |
分子式 | C19H18ClN5OS |
CAS No. | 202591-23-9 |
Smiles | CC=1C2=C(N3C(C(CC(N)=O)N=C2C4=CC=C(Cl)C=C4)=NN=C3C)SC1C |
密度 | 1.51 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 200 mM | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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