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2438124-95-7

2438124-95-7 structure
2438124-95-7 structure
  • Name: ALV2
  • Chemical Name: ALV2
  • CAS Number: 2438124-95-7
  • Molecular Formula: C26H26ClN5O5
  • Molecular Weight: 523.97
  • Catalog: Research Areas Cancer
  • Create Date: 2022-01-17 18:02:03
  • Modify Date: 2024-01-07 06:40:23
  • ALV2 is a potent and selective Helios degrader. ALV2 binds CRBN, with an IC50 of 0.57 μM. Helios is the zinc-finger transcription factor that can maintain a stable Treg cell phenotype in the inflammatory tumor microenvironment[1].

Name ALV2
Description ALV2 is a potent and selective Helios degrader. ALV2 binds CRBN, with an IC50 of 0.57 μM. Helios is the zinc-finger transcription factor that can maintain a stable Treg cell phenotype in the inflammatory tumor microenvironment[1].
Related Catalog
Target

IC50: 0.57 μM (CRBN)[1]

In Vitro ALV2 (10 nM-100 μM) induces CRBN-Helios dimerization in the TR-FRET assay[1]. ALV2 (0.1-10 μM) preferentially promotes Helios degradation in Jurkat cells[1]. ALV2 (1 μM; pretreated for 18 h) promotes IL-2 secretion in Jurkat cells[1].
In Vivo ALV2 (100 mg/kg; i.p. twice daily for 7 days) induces selective Helios degradation in vivo[1]. Animal Model: CrbnI391V/I391V mice Dosage: 100 mg/kg Administration: I.p. twice daily for 7 days Result: Reduced Helios, but not Ikaros, levels in splenic CD4+FoxP3+ Treg cells.
References

[1]. Wang ES, et, al. Acute pharmacological degradation of Helios destabilizes regulatory T cells. Nat Chem Biol. 2021 Jun;17(6):711-717.

Molecular Formula C26H26ClN5O5
Molecular Weight 523.97