A1874

Catalog No.S8785 Batch:S878501

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Technical Data

Formula

C58H62Cl3F2N9O7S
Molecular Weight 1173.59 CAS No. 2064292-12-0
Solubility (25°C)* In vitro DMSO 100 mg/mL (85.2 mM)
Ethanol 100 mg/mL (85.2 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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]

Protocol (from reference)

Cell Assay:

[1]
  • 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.

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.