产品描述
ALV2 is a potent and selective Helios degrader. ALV2 binds CRBN, with an IC 50 of 0.57 μM. Helios is the zinc-finger transcription factor that can maintain a stable T reg cell phenotype in the inflammatory tumor microenvironment.
体外活性
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].
体内活性
ALV2 (100 mg/kg; i.p. twice daily for 7 days) induces selective Helios degradation in vivo[1]. Animal Model: Crbn I391V/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.
Cas No.
2438124-95-7
分子式
C26H26ClN5O5
分子量
523.97
别名
ALV2
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years