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A1874
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
A1874图片
CAS NO:2064292-12-0
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议

产品介绍

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。

Cas No.2064292-12-0
Canonical SMILESClC(C=C1)=CC=C1C2=N[C@H](C3=NN=C(C)N3C4=C2C(C)=C(C)S4)CC(NCCOCCOCCOCCNC(C5=CC(OC)=C(NC([C@H]6[C@H](C7=C(F)C(Cl)=CC=C7)[C@](C8=CC=C(Cl)C=C8F)(C#N)[C@H](CC(C)(C)C)N6)=O)C=C5)=O)=O
分子式C58H62Cl3F2N9O7S
分子量1173.59
溶解度DMSO : 150 mg/mL (127.81 mM);Water :< 0.1 mg/mL (insoluble)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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[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].

Reference：
[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.