ALV1
Based on 1 Customer Validation
ALV1 is a molecular glue degrader for Ikaros (IKZF1) and Helios (IKZF2) with DC50 of 2.5 nM and 10.3 nM respectively. ALV1 bind CRBN with an IC50 of 0.55 μM, and induces CRBN-Helios dimerization. ALV1 can be used to study the properties and functions of regulatory T cells.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.62%
- CAS. Nr.: 2438124-79-7
- Formel: C25H23ClN4O5
- Molecular Weight:494.93
-
Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biologische Aktivität
|
IKZF1 2.5 nM (DC50) |
IZKF2 10.3 nM (DC50) |
Cereblon |
ALV1 (0-10 μM, 4-18 h) induces Ikaros and Helios degradation and promotes IL-2 secretion in Jurkat cells[1].
ALV1 (1 μM, 24 h) effectively induces Ikaros and Helios degradation in Treg cells isolated from human peripheral blood[1].
ALV1 (0.1-10 μM, 4 h) induces degradation of both Ikaros and Helios but does not affect the stability of GSPT1 in Jurkat cells[1].
ALV1 (1 μM, 4 h) induces Helios degradation without unexpected off-target activity in Jurkat cells [1].
ALV1 (1 μM, 18 h) promotes IL-2 secretion to a greater extent than Lenalidomide (HY-A0003) in Jurkat cells, suggesting Helios more strongly represses IL-2 production in this context[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:Jurkat
-
Concentration:0.1, 1 and 10 μM
-
Incubation Time:4 h
-
Result:Significantly reduced the levels of Ikaros and Helios.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS. Nr. 2438124-79-7
-
Appearance Solid
-
Molecular Weight 494.93
-
Formel C25H23ClN4O5
-
Color Light yellow to green yellow
-
SMILES
O=C(NC1=CC=C(C)C(Cl)=C1)CCC2=CC=CC(NC3=CC(N(C(CC4)C(NC4=O)=O)C3=O)=O)=C2
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : 50 mg/mL (101.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (5.05 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
-
Data Sheet (271 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Handling Instructions (2659 KB)
Verweise
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0205 mL | 10.1024 mL | 20.2049 mL | 50.5122 mL |
| 5 mM | 0.4041 mL | 2.0205 mL | 4.0410 mL | 10.1024 mL | |
| 10 mM | 0.2020 mL | 1.0102 mL | 2.0205 mL | 5.0512 mL | |
| 15 mM | 0.1347 mL | 0.6735 mL | 1.3470 mL | 3.3675 mL | |
| 20 mM | 0.1010 mL | 0.5051 mL | 1.0102 mL | 2.5256 mL | |
| 25 mM | 0.0808 mL | 0.4041 mL | 0.8082 mL | 2.0205 mL | |
| 30 mM | 0.0673 mL | 0.3367 mL | 0.6735 mL | 1.6837 mL | |
| 40 mM | 0.0505 mL | 0.2526 mL | 0.5051 mL | 1.2628 mL | |
| 50 mM | 0.0404 mL | 0.2020 mL | 0.4041 mL | 1.0102 mL | |
| 60 mM | 0.0337 mL | 0.1684 mL | 0.3367 mL | 0.8419 mL | |
| 80 mM | 0.0253 mL | 0.1263 mL | 0.2526 mL | 0.6314 mL | |
| 100 mM | 0.0202 mL | 0.1010 mL | 0.2020 mL | 0.5051 mL |