A1874( A-1874 )

Catalog No. M13210 CAS No. 2064292-12-0

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Datasheet

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Product Name

A1874
Note

Research use only, not for human use.
Brief Description

A1874 (A-1874) is a nutlin-based and BRD4-degrading PROTAC with DC50 of 32 nM (induce BRD4 degradation in cells).
Description

A1874 (A-1874) is a nutlin-based and BRD4-degrading PROTAC with DC50 of 32 nM (induce BRD4 degradation in cells); A1874 is more effective in inhibiting proliferation of many cancer cell lines with wild type p53 than was a corresponding VHL-utilizing PROTAC with similar potency and efficacy to degrade BRD4; demonstrates synergistic antiproliferative effect via simultaneous degradation of BRD4 and stabilization of p53.
In Vitro

Western Blot Analysis 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.
In Vivo

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Synonyms

A-1874
Pathway

PROTACs
Target

PROTAC
Recptor

PROTAC
Research Area

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Indication

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CAS Number

2064292-12-0
Formula Weight

1173.597
Molecular Formula

C58H62Cl3F2N9O7S
Purity

>98% (HPLC)
Solubility

DMSO : 150 mg/mL 127.81 mM;H2O : < 0.1 mg/mL
SMILES

O=C([C@@H]1N[C@@H](CC(C)(C)C)[C@](C#N)(C2=CC=C(Cl)C=C2F)[C@H]1C3=CC=CC(Cl)=C3F)NC4=CC=C(C(NCCOCCOCCOCCNC(C[C@H]5C6=NN=C(C)N6C7=C(C(C)=C(C)S7)C(C8=CC=C(Cl)C=C8)=N5)=O)=O)C=C4OC
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-5-neopentylpyrrolidine-2-carboxamide

1. Hines J, et al. Cancer Res. 2018 Nov 1. pii: canres.2918.2018.

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