2. PROTAC
  3. Ligands for E3 Ligase Molecular Glues
  4. ALV2

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.

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ALV2 Chemical Structure

ALV2 Chemical Structure

CAS No. : 2438124-95-7

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Based on 1 publication(s) in Google Scholar

ALV2 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

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].

IC50 & Target

IC50: 0.57 μM (CRBN)[1]
In Vitro

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

ALV2 Related Antibodies
In Vivo

ALV2 (100 mg/kg; i.p. twice daily for 7 days) induces selective Helios degradation in vivo[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

523.97

Formula

C26H26ClN5O5
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

O=C(NC(C)(C1=CC=CC(NC2=CC(N(C(CC3)C(NC3=O)=O)C2=O)=O)=C1)C)NC4=CC=C(C)C(Cl)=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 160 mg/mL (305.36 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 4 mg/mL (7.63 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 4 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 (40.0 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 4 mg/mL (7.63 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 4 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 (40.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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 1.9085 mL 9.5425 mL 19.0851 mL 47.7127 mL
5 mM 0.3817 mL 1.9085 mL 3.8170 mL 9.5425 mL
10 mM 0.1909 mL 0.9543 mL 1.9085 mL 4.7713 mL
15 mM 0.1272 mL 0.6362 mL 1.2723 mL 3.1808 mL
20 mM 0.0954 mL 0.4771 mL 0.9543 mL 2.3856 mL
25 mM 0.0763 mL 0.3817 mL 0.7634 mL 1.9085 mL
30 mM 0.0636 mL 0.3181 mL 0.6362 mL 1.5904 mL
40 mM 0.0477 mL 0.2386 mL 0.4771 mL 1.1928 mL
50 mM 0.0382 mL 0.1909 mL 0.3817 mL 0.9543 mL
60 mM 0.0318 mL 0.1590 mL 0.3181 mL 0.7952 mL
80 mM 0.0239 mL 0.1193 mL 0.2386 mL 0.5964 mL
100 mM 0.0191 mL 0.0954 mL 0.1909 mL 0.4771 mL
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ALV2 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ALV22438124-95-7ALV 2ALV-2Ligands for E3 LigaseMolecular GluesE3 ligase-recruiting MoietyHeliosCRBNzinc-fingertranscriptiontumorInhibitorinhibitorinhibit

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