CPI-637

产品详情：

更新时间： 2024-09-30 22:37:11

CAS号：1884712-47-3

常用名： CPI-637

价格：
￥需询单/1kg

纯度： 98.0%

备货期： 需询单

库存： 现货

其他详情（用途，包装）：
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：

公司名：成都恒汇化成医药科技有限公司

认证状态： 未认证供应商

商品数： 94件

电话： +28-89481236

地址： 蓉台大道388号

地区： 成都市温江区

联系人： 邓琪山

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其他供应商价格：

2024-03-12 价格：￥885.9 CPI-637

2024-07-15 价格：需询单 CPI-637

2023-09-22 价格：￥需询单 CPI-637

2020-12-08 价格：￥需询单 CPI-637

2022-05-12 价格：$需询单 CPI-637

2021-05-10 价格：￥需询单 CPI-637

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CPI-637价格

CPI-637

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