[CAS NO. 2064292-12-0]  A1874

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PRODUCTS SPECIFICATIONS [2064292-12-0]

Distributor
Catalog
AS893452
Brand
Arctom Scientific
CAS
2064292-12-0

DESCRIPTION [2064292-12-0]

Overview

MDLMFCD31813733
Molecular Weight1173.59
Molecular FormulaC58H62Cl3F2N9O7S
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

For research use only. We do not sell to patients.

Summary

A1874 is a nutlin-based ( MDM2 ligand) and BRD4 -degrading PROTAC with a DC 50 of 32 nM (induce BRD4 degradation in cells). Effective in inhibiting many cancer cell lines proliferation [1] .


IC50 & Target

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] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

4°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)


Solvent & Solubility

In Vitro:

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

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
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

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

  • 2.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

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

* All of the co-solvents are available by MCE.