A1874

Research use only, not for human use.

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

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.

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.

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A-1874

PROTACs

PROTAC

PROTAC

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2064292-12-0

1173.597

C58H62Cl3F2N9O7S

>98% (HPLC)

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

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

(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

(-20℃)

With Ice Pack

≥ 2 years