DC Chemicals · Product datasheet

A1874 — Datasheet

CAT. NO. DC12702

Product page and current package options

ParameterValue
Chemical Name(2R,3S,4R,5S)-3-(3-chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-N-(4-((1-((S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-2-oxo-6,9,12-trioxa-3-azatetradecan-14-yl)carbamoyl)-2-methoxyphenyl)-4-cyano-
CAS No.2064292-12-0
SynonymsA-1874,A 1874
FormulaC58H62Cl3F2N9O7S
M.Wt1173.597
SMILESN1[C@H](CC(C)(C)C)[C@](C2=CC=C(Cl)C=C2F)(C#N)[C@H](C2=CC=CC(Cl)=C2F)[C@H]1C(NC1=CC=C(C(=O)NCCOCCOCCOCCNC(=O)C[C@H]2N=C(C3=CC=C(Cl)C=C3)C3C(C)=C(C)SC=3N3C(C)=NN=C32)C=C1OC)=O
Purity>98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

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].

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.

In Vivo

No in vivo data are provided in the current product source. Contact us for further information.

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

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