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A1874

SKU: orb1225722

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.

Images & Validation

Key Properties

CAS Number2064292-12-0
MW1173.597
Purity>98% (HPLC)
FormulaC58H62Cl3F2N9O7S
SMILESO=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
TargetPROTAC
SolubilityDMSO : 150 mg/mL 127.81 mM;H2O : < 0.1 mg/mL

Bioactivity

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.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

A-1874

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  • A1874 [orb1301788]

    99.52% (May vary between batches)

    2064292-12-0

    1173.59

    C58H62Cl3F2N9O7S

    10 mg, 1 mg, 5 mg, 25 mg, 50 mg, 100 mg
Quality Guarantee

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Protocol Information

Available Sizes

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500 mg
200 mg
2 mg
$ 500.00
5 mg
$ 760.00
10 mg
$ 1,070.00
25 mg
$ 1,680.00
50 mg
$ 2,260.00
100 mg
$ 3,040.00