| CAS NO: | 1884712-47-3 |
| 包装 | 价格(元) |
| 10mg | 电议 |
| 50mg | 电议 |
| Cas No. | 1884712-47-3 |
| 化学名 | (S)-4-methyl-6-(1-methyl-3-(1-methyl-1H-pyrazol-4-yl)-1H-indazol-5-yl)-4,5-dihydro-1H-benzo[b][1,4]diazepin-2(3H)-one |
| Canonical SMILES | O=C1NC2=CC=CC(C3=CC4=C(N(C)N=C4C5=CN(C)N=C5)C=C3)=C2N[C@@H](C)C1 |
| 分子式 | C22H22N6O |
| 分子量 | 386.45 |
| 溶解度 | ≥ 19.3mg/mL in DMSO with gentle warming |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | IC50: 0.03 and 11.0 μM for CBP/EP300 and BRD4, respectively. CPI-637 is a CBP/EP300 bromodomain inhibitor. It has been reported that among bromodomain-containing proteins implicated in various disease pathways, cyclic-AMP response element binding protein (CBP) and adenoviral E1A binding protein of 300 kDa (EP300), which is a highly homologous pair of bromodomain-containing transcriptional coactivators, are of great interest as potential drug targets due to their reported involvement in a variety of disease states. In vitro: Previous study found that CPI-637 was potent against EP300, and its opposite enantiomer showed a over 200-fold loss in potency. Moreover, the biochemical potency of CPI-637 translated well into cells with CBP BRET EC50 of 0.3 μM, and CPI-637 demonstrated a more than 700-fold selectivity over the BET family of bromodomains. In addition, CPI-637 was also highly selective against other bromodomains, showing substantial biochemical activity only against BRD9. Furthermore, it was found that CPI-637 was able to inhibit the expression of MYC with an EC50 of 0.60 μM in a cellular assay,. [1]. In vivo: So far, there is no animal in vivo data reported. Clinical trial: Up to now, CPI-637 is still in the preclinical development stage. Reference: |
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