| Identification | Back Directory | [Name]
Urea, N-(3-chloro-4-methylphenyl)-N'-[1-[3-[[1-(2,6-dioxo-3-piperidinyl)-2,5-dihydro-2,5-dioxo-1H-pyrrol-3-yl]amino]phenyl]-1-methylethyl]- | [CAS]
2438124-95-7 | [Synonyms]
ALV2
Urea, N-(3-chloro-4-methylphenyl)-N'-[1-[3-[[1-(2,6-dioxo-3-piperidinyl)-2,5-dihydro-2,5-dioxo-1H-pyrrol-3-yl]amino]phenyl]-1-methylethyl]- | [Molecular Formula]
C26H26ClN5O5 | [MOL File]
2438124-95-7.mol | [Molecular Weight]
523.97 |
| Chemical Properties | Back Directory | [Boiling point ]
724.8±60.0 °C(Predicted) | [density ]
1.444±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 160 mg/mL (305.36 mM; Need ultrasonic)| | [form ]
Solid | [pka]
10.69±0.40(Predicted) | [color ]
White to yellow | [Water Solubility ]
Water : < 0.1 mg/mL (insoluble) |
| Hazard Information | Back Directory | [Uses]
ALV2 is a potent and selective Helios molecular glue 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]. | [Biological Activity]
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]. | [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.
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| [IC 50]
Cereblon | [References]
[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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| Company Name: |
ChemOrigin Pharm
|
| Telephone: |
15026428026 19002516454 |
| Website: |
www.chemorigin.com |
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