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CPI-637

更新时间:2025-09-06 11:06:27 采购访问:18次

常用名 CPI-637 CAS号 1884712-47-3
价格 纯度 98.0%
备货期 10天 库存 现货
 产品详情(用途,包装等)
用途:
CPI-637 is a potent and selective CBP/EP300 bromodomains inhibitor with IC50 of 0.03±0.01μM and 11.0±0.6 μM for CBP/EP300 and BRD4, respectively.IC50:0.03±0.01μM (CBP/EP300)[1]IC50:11.0±0.6 μM(BRD4)[1]CPI-637, which demonstrated substantial biochemical potency that was confirmed by isothermal titration calorimetry. A cocrystal structure of CPI-637 in the CBP bromodomain indicated that the compound recapitulated the key hydrogen bonding interactions observed with the parent compound, with the substituted indazole filling space above Pro1110 and the Pro/Arg cleft . As expected, CPI-637 was also potent against EP300, and its opposite enantiomer displayed a >200-fold loss in potency. The biochemical potency of CPI-637 translated well into cells (CBP BRET EC50 = 0.3 μM), and the compound demonstrated a >700-fold selectivity over the BET family of bromodomains (BRD4 IC50 = 11.0 ± 0.6 μM).CPI-637 was also highly selective against other bromodomains (detailed list in the Supporting Information), displaying substantial biochemical activity only against BRD9, which is acceptable, since inhibition of the BRD9 bromodomain has not been shown to produce a pronounced cellular phenotype . In a cellular assay, CPI-637 inhibits the expression of MYC, a transcription factor widely expressed in human cancer,with an EC50 of 0.60 μM, providing an orthogonal measure of the target engagement of the compound .The inactive enantiomer of CPI-637 displayed an EC50 in the same assay of >10 μM.[1]
物理化学性质:
CAS号:1884712-47-3
常用中文名:CPI-637
常用英文名:CPI-637
分子式:C22H22N6O
分子量:386.450
密度:1.4±0.1 g/cm3
沸点:689.2±55.0 °C at 760 mmHg
熔点:N/A
闪点:370.6±31.5 °C
储存条件:-20℃

供应商信息

上海化源世纪贸易有限公司 认证供应商

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参考价格:$106/10mM*1mLinDMSO
其他供应商价格:
2024-03-12 CPI-637
价格:¥885.9
2023-09-22 CPI-637
价格:¥需询单
2020-12-08 CPI-637
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2018-05-13 CPI-637
价格:¥需询单
2022-05-12 CPI-637
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2021-05-10 CPI-637
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