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2064292-12-0

2064292-12-0 structure
2064292-12-0 structure
  • Name: A1874
  • Chemical Name: A1874
  • CAS Number: 2064292-12-0
  • Molecular Formula: C58H62Cl3F2N9O7S
  • Molecular Weight: 1173.59
  • Catalog: Signaling Pathways Epigenetics Epigenetic Reader Domain
  • Create Date: 2019-03-30 12:17:33
  • Modify Date: 2024-01-09 18:18:37
  • 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].

Name A1874
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.

Molecular Formula C58H62Cl3F2N9O7S
Molecular Weight 1173.59
Storage condition 2-8℃
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