1. PROTAC
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    Epigenetic Reader Domain
  3. A1874

A1874 

目录号: HY-114305 纯度: 98.38%
产品使用指南

A1874 是一种以nutlin 为基础的、BRD4-降解的 PROTACDC50 值为 32 nM (诱导细胞内的BRD4降解)。有效抑制多种癌细胞增殖。

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A1874 Chemical Structure

A1874 Chemical Structure

CAS No. : 2064292-12-0

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Size Price Stock Quantity
10 mM * 1 mL in DMSO ¥12264 In-stock
5 mg ¥6500 In-stock
10 mg ¥9500 In-stock
25 mg ¥19500 In-stock
50 mg   Get quote  
100 mg   Get quote  

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Description

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].

IC50 & Target[1]

BRD4

 

In Vitro

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].

Western Blot Analysis[1]

Cell 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.
Storage

4°C, stored under nitrogen

Solvent & Solubility
In Vitro: 

DMSO : 150 mg/mL (127.81 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.8521 mL 4.2604 mL 8.5209 mL
5 mM 0.1704 mL 0.8521 mL 1.7042 mL
10 mM 0.0852 mL 0.4260 mL 0.8521 mL
*请根据产品在不同溶剂中的溶解度,选择合适的溶剂配制储备液。
In Vivo:
  • 1.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (2.13 mM); Clear solution

  • 2.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (2.13 mM); Clear solution

*以上所有助溶剂都可在 MCE 网站选购。
References
Molecular Weight

1173.59

Formula

C₅₈H₆₂Cl₃F₂N₉O₇S

CAS No.

2064292-12-0

SMILES

ClC(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

Shipping

Room temperature in continental US; may vary elsewhere

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产品名称:
A1874
目录号:
HY-114305
需求量:

A1874

Cat. No.: HY-114305