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CPI-637 是一种选择性和细胞活性的苯二氮卓 CBP/EP300 溴结构域抑制剂,其对 CBP、EP300和 BRD4 BD-1的 IC50值分别为 0.03、0.051 和 11.0 μM,对 CBP 的 EC50值为 0.3 μM。
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CPI-637 是一种选择性和细胞活性的苯二氮卓 CBP/EP300 溴结构域抑制剂,其对 CBP、EP300和 BRD4 BD-1的 IC50值分别为 0.03、0.051 和 11.0 μM,对 CBP 的 EC50值为 0.3 μM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 283 | 现货 | |
2 mg | ¥ 395 | 现货 | |
5 mg | ¥ 647 | 现货 | |
10 mg | ¥ 913 | 现货 | |
25 mg | ¥ 1,770 | 现货 | |
50 mg | ¥ 3,230 | 现货 | |
100 mg | ¥ 4,780 | 现货 | |
500 mg | ¥ 9,870 | 现货 |
产品描述 | CPI-637 is a selective and cell-active benzodiazepinone CBP/EP300 bromodomain inhibitor. |
靶点活性 | CBP:0.03 μM, EP300:0.051 μM |
体外活性 | CPI-637 inhibits MYC expression in AMO-1 cells (EC50=0.60 μM)[1]. |
激酶实验 | Ki Determination: Inhibition of human full-length recombinant PARP-1 by [32P]NAD+ incorporation is measured. The [32P]ADP-ribose incorporated into acid insoluble material is quantified using a PhosphorImager. Ki is calculated by nonlinear regression analysis. |
细胞实验 | AMO-1 cells (DSMZ) were plated at 20,000 cells/well in 96-well plates in Iscove's Modified Dulbecco's Medium supplemented with 10% fetal calf serum. Cells were treated for 6 h with a dose titration of CPI-637 starting from a 5 μM top concentration. After 6 h, cells were lysed and processed for QuantiGene Plex expression analysis and data were collected on a MAGPIX multiplex Luminex instrument.(Only for Reference) |
别名 | CPI 637 |
分子量 | 386.45 |
分子式 | C22H22N6O |
CAS No. | 1884712-47-3 |
Smiles | C[C@@H]1CC(=O)Nc2cccc(-c3ccc4n(C)nc(-c5cnn(C)c5)c4c3)c2N1 |
密度 | 1.38 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: 3.87 mg/mL (10 mM), Sonication is recommended. Ethanol: < 1 mg/mL (insoluble or slightly soluble) H2O: < 1 mg/mL (insoluble or slightly soluble) | ||||||||||||||||||||
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