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A1874 

Cat. No.: HY-114305
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

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  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

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.
References
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

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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A1874
Cat. No.:
HY-114305
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A1874

Cat. No.: HY-114305