A1874

Modify Date: 2025-08-25 07:41:27

A1874 Structure
A1874 structure
Common Name A1874
CAS Number 2064292-12-0 Molecular Weight 1173.59
Density N/A Boiling Point N/A
Molecular Formula C58H62Cl3F2N9O7S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of A1874


A1874 is a nutlin-based and BRD4-degrading PROTAC with a DC50 of 32 nM (induce BRD4 degradation in cells). Effective in inhibiting many cancer cell lines proliferation[1].

 Names

Name A1874

 A1874 Biological Activity

Description A1874 is a nutlin-based and BRD4-degrading PROTAC with a DC50 of 32 nM (induce BRD4 degradation in cells). Effective in inhibiting many cancer cell lines proliferation[1].
Related Catalog
Target

BRD4

In Vitro Treatment of HCT116 cells of A1874 (0-10 μM, 24 hours) induces a dose-dependent knockdown of BRD4 levels, with near-maximum knockdown by 100 nmol/L and a maximum degradation (Dmax) of BRD4 of 98% of the levels in control (0.1% DMSO-treated) cells[1]. Treatment of HCT116 cells of A1874 (0-10 μM, 24 hours) increases p53 levels in the HCT116 cells and showed dose-dependent p53 stabilization[1]. Western Blot Analysis[1] 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.
References

[1]. Hines J, et al. MDM2-Recruiting PROTAC Offers Superior, Synergistic Antiproliferative Activity via Simultaneous Degradation of BRD4 and Stabilization of p53. Cancer Res. 2019 Jan 1;79(1):251-262.

 Chemical & Physical Properties

Molecular Formula C58H62Cl3F2N9O7S
Molecular Weight 1173.59
InChIKey IPNTVOAQOGRLQB-JJMBTQCASA-N
SMILES COc1cc(C(=O)NCCOCCOCCOCCNC(=O)CC2N=C(c3ccc(Cl)cc3)c3c(sc(C)c3C)-n3c(C)nnc32)ccc1NC(=O)C1NC(CC(C)(C)C)C(C#N)(c2ccc(Cl)cc2F)C1c1cccc(Cl)c1F
Storage condition 2-8℃
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