A1874

For research use only.

Catalog No.S8785

A1874 Chemical Structure

CAS No. 2064292-12-0

A1874 is a much improved nutlin-based, BRD4-degrading PROTAC and is able to degrade its target protein by 98% with nanomolar potency.

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Biological Activity

Description A1874 is a much improved nutlin-based, BRD4-degrading PROTAC and is able to degrade its target protein by 98% with nanomolar potency.
Targets
BRD4 [1]
()
In vitro

In HCT116 cells, A1874 causes a 97% decrease in viability and in A375 cells, A1874 causes a 98% loss of viability.A1874 reduced viability of Daudi cells by 70% and of MOLM-13 cells by 95%.[1]

Assay
Methods Test Index PMID
Western blot
BRD4 / c-Myc / GAPDH / p53 / p21; 

PubMed: 30385614     


Representative immunoblots from HCT116 cells treated with increasing concentrations of A1874 (left panel) and quantified results (right panel).

30385614
Growth inhibition assay
Cell viability; 

PubMed: 30385614     


Comparative effectiveness of MDM2-recruiting PROTAC versus component ligands and VHL-recruiting PROTAC in cells with accentuated JQ1 sensitivity and/or elevated MDM2 levels. (A) Daudi lymphoma cells; (B) MOLM-13 myeloid leukemia cells; (C) SJSA-1 osteosarcoma cells.

Cell viability; 

PubMed: 30385614     


Cell viability assay of cell lines treated with A1874 compared to its component ligands. (A) HCT116 colorectal cancer cells; (B) A375 melanoma cells; (C) NCI-H2030 lung cancer cells; (D) HT29 colorectal cancer cells; (E) p53−/− HCT116 colorectal cancer cells (isogenic with panel (A)). A1874 data points that are asterisked exhibit synergistic activity compared to the sum of the component warhead activities at the same concentration according to Bliss Independence model (32).

30385614

Protocol

Cell Research:

[1]

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  • Cell lines: HCT116 cell lines
  • Concentrations: 0-10 μM
  • Incubation Time: 24 h
  • Method:

    Treatment of HCT116 cells for 24 hours with increasing concentrations of A1874 induced 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.


    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (85.2 mM)
Ethanol 100 mg/mL (85.2 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 1173.59
Formula

C58H62Cl3F2N9O7S

CAS No. 2064292-12-0
Storage powder
in solvent
Synonyms N/A
Smiles CC1=C(SC2=C1C(=NC(C3=NN=C(N32)C)CC(=O)NCCOCCOCCOCCNC(=O)C4=CC(=C(C=C4)NC(=O)C5C(C(C(N5)CC(C)(C)C)(C#N)C6=C(C=C(C=C6)Cl)F)C7=C(C(=CC=C7)Cl)F)OC)C8=CC=C(C=C8)Cl)C

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID