A1874是一种以nutlin为基础的、BRD4-降解的PROTAC，DC50值为32nM(诱导细胞内的BRD4降解)。有效抑制多种癌细胞增殖。
货号:ajcx12960
CAS:2064292-12-0
分子式:C58H62Cl3F2N9O7S
分子量：1173.59
溶解度:DMSO : 150 mg/mL (127.81 mM);H2O :< 0.1 mg/mL (insoluble)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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[1].

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[1].
Treatment of HCT116 cells of A1874 (0-10 μM, 24 hours) increases p53 levels in the HCT116 cells and showed dose-dependent p53 stabilization[1].

参考文献：
[1]. Hines J, et al. MDM2-Recruiting PROTAC Offers Superior, Synergistic Antiproliferative Activity via Simultaneous Degradation of BRD4 and Stabilization of p53. Cancer Res. 2019 Jan 1;79(1):251-262.