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A1874 

Cat. No.: HY-114305 Purity: 98.38%
Handling Instructions

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.

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

A1874 Chemical Structure

A1874 Chemical Structure

CAS No. : 2064292-12-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 1226 In-stock
Estimated Time of Arrival: December 31
5 mg USD 650 In-stock
Estimated Time of Arrival: December 31
10 mg USD 950 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1950 In-stock
Estimated Time of Arrival: December 31
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100 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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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.
Molecular Weight

1173.59

Formula

C₅₈H₆₂Cl₃F₂N₉O₇S

CAS No.

2064292-12-0

SMILES

ClC(C=C1)=CC=C1C2=N[[email protected]](C3=NN=C(C)N3C4=C2C(C)=C(C)S4)CC(NCCOCCOCCOCCNC(C5=CC(OC)=C(NC([[email protected]]6[[email protected]](C7=C(F)C(Cl)=CC=C7)[[email protected]](C8=CC=C(Cl)C=C8F)(C#N)[[email protected]](CC(C)(C)C)N6)=O)C=C5)=O)=O

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)

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
*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 provided by MCE.
References
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A1874
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HY-114305
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