Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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Other Sizes |
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Targets |
IC50: 0.57 μM (CRBN)[1]
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ln Vitro |
In the TR-FRET test, ALV2 (10 nM-100 μM) causes CRBN-Helios dimerization[1]. In Jurkat cells, ALV2 (0.1–10 μM) primarily stimulates Helios degradation[1]. In Jurkat cells, ALV2 (1 μM) pretreatment for 18 hours increases IL-2 secretion[1].
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ln Vivo |
In vitro, ALV2 (100 mg/kg; intraperitoneally twice daily for seven days) selectively degrades Helios[1].
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Animal Protocol |
Animal/Disease Models: CrbnI391V/I391V mice
Doses: 100 mg/kg Route of Administration: Ip twice (two times) daily for 7 days Experimental Results: decreased Helios, but not Ikaros, levels in splenic CD4+FoxP3+ Treg cells. |
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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Molecular Formula |
C26H26CLN5O5
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Molecular Weight |
523.97
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CAS # |
2438124-95-7
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO :~160 mg/mL (~305.36 mM)
H2O :< 0.1 mg/mL |
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Solubility (In Vivo) |
Solubility in Formulation 1: 4 mg/mL (7.63 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 40.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 4 mg/mL (7.63 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 40.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.9085 mL | 9.5425 mL | 19.0851 mL | |
5 mM | 0.3817 mL | 1.9085 mL | 3.8170 mL | |
10 mM | 0.1909 mL | 0.9543 mL | 1.9085 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.