A1874CAS号： 2064292-12-0分子式： C58H62Cl3F2N9O7S分子量： 1173.59描述纯度储存/保存方法可溶性/溶解性In vitro(体外研究)
| 产品描述 | |
| 描述 |
A1874 is a nutlin-based and BRD4-degrading PROTAC with a DC50 of 32 nM (induce BRD4 degradation in cells). Effective in inhibiting many cancer cell lines proliferation.
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| 纯度 |
98%
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| 储存/保存方法 |
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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| 基本信息 | |
| 可溶性/溶解性 |
DMSO : 150 mg/mL (127.81 mM; Need ultrasonic)
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| 生物活性 | |
| In vitro(体外研究) |
Treatment of HCT116 cells of A1874 (0-10 μM, 24 hours) induces a dose-dependent knockdown of BRD4 levels, with near-maximum knockdown by 100 nmol/L and a maximum degradation (Dmax) of BRD4 of 98% of the levels in control (0.1% DMSO-treated) cells.Treatment of HCT116 cells of A1874 (0-10 μM, 24 hours) increases p53 levels in the HCT116 cells and showed dose-dependent p53 stabilization.Western Blot AnalysisCell Line:HCT116 cells.Concentration:0-10 μM.Incubation Time:24 hours.Result:Induced a dosedependent knockdown of BRD4 levels, with near-maximum knockdown by 100 nM.Increased p53 levels and showed dose-dependent p53 stabilization.
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分子结构图
