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ALV2
🥰Excellent
Catalog No. T40099Cas No. 2438124-95-7
ALV2 is a potent and selective Helios degrader that binds to CRBN protein, with an IC50 of 0.57 μM. Helios, a zinc-finger transcription factor, is essential for maintaining a stable T reg cell phenotype in the inflammatory tumor microenvironment.
ALV2
🥰Excellent
Catalog No. T40099Cas No. 2438124-95-7
ALV2 is a potent and selective Helios degrader that binds to CRBN protein, with an IC50 of 0.57 μM. Helios, a zinc-finger transcription factor, is essential for maintaining a stable T reg cell phenotype in the inflammatory tumor microenvironment.
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Product Introduction
Bioactivity
Chemical Properties
| Description | ALV2 is a potent and selective Helios degrader that binds to CRBN protein, with an IC50 of 0.57 μM. Helios, a zinc-finger transcription factor, is essential for maintaining a stable T reg cell phenotype in the inflammatory tumor microenvironment. |
| Targets&IC50 | CRBN:0.57 μM (IC50) |
| In vitro | ALV2, within a concentration range of 10 nM to 100 μM, initiates CRBN-Helios dimerization as evidenced by the TR-FRET assay[1]. At lower concentrations (0.1-10 μM), ALV2 specifically facilitates the degradation of Helios in Jurkat cells[1]. Moreover, when pre-administered for 18 hours at a concentration of 1 μM, ALV2 enhances IL-2 secretion in Jurkat cells[1]. |
| In vivo | ALV2, administered intraperitoneally at a dosage of 100 mg/kg twice daily for 7 days, selectively induces Helios degradation in vivo in Crbn I391V/I391V mouse models. This treatment specifically reduced Helios levels without affecting Ikaros in splenic CD4 + FoxP3 + T regulatory cells. |
| Molecular Weight | 523.97 |
| Formula | C26H26ClN5O5 |
| Cas No. | 2438124-95-7 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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