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| | 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]- Basic information |
| Product 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]- | | Synonyms: | 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]-;3-(3-chloro-4-methylphenyl)-1-[2-(3-{[1-(2,6-dioxopiperidin-3-yl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino}phenyl)propan-2-yl]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]urea;Helios molecular glue degrader ALV2;ALV2 | | CAS: | 2438124-95-7 | | MF: | C26H26ClN5O5 | | MW: | 523.97 | | EINECS: | | | Product Categories: | | | Mol File: | 2438124-95-7.mol | ![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]- Structure](CAS/20210305/GIF/2438124-95-7.gif) |
| | 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]- Chemical Properties |
| 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)| | | pka | 10.69±0.40(Predicted) | | form | Solid | | color | White to yellow | | Water Solubility | Water : < 0.1 mg/mL (insoluble) |
| | 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]- Usage And Synthesis |
| 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. |
| | 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]- Preparation Products And Raw materials |
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