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A1874

Chemical Structure : A1874

CAS No.: 2064292-12-0

A1874 (A-1874)

Catalog No.: PC-35762Not For Human Use, Lab Use Only.

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

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.
A1874 demonstrates synergistic antiproliferative effect via simultaneous degradation of BRD4 and stabilization of p53.

Physicochemical Properties

M.Wt 1173.597
Formula C58H62Cl3F2N9O7S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(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

References

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

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