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A1874

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.

Product Specifications

CAS Number

2064292-12-0

Product Name Alternative

A-1874

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

Molecular Formula

C58H62Cl3F2N9O7S

Molecular Weight

1173.597

Storage Conditions

Storage temperature: -20°C. Stability: ≥ 2 years

Notes

For research use only.

Other Product Names

(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

Available Sizes

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