化学性质:
规格 | 5 mg 10 mg 25 mg |
CAS | 2438124-95-7 |
别名 | N/A |
化学名 | N/A |
分子式 | C26H26ClN5O5 |
分子量 | 523.97 |
溶解度 | DMSO : 160 mg/mL (305.36 mM; Need ultrasonic)|H2O : < 0.1 mg/mL (insoluble) |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
产品描述:
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].
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].
ALV2 (100 mg/kg; i.p. twice daily for 7 days) induces selective Helios degradation in vivo[1].
[1]. Wang ES, et, al. Acute pharmacological degradation of Helios destabilizes regulatory T cells. Nat Chem Biol. 2021 Jun;17(6):711-717
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标签:ALV2
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