Cbl-b-IN-2
Based on 1 Customer Validation
Cbl-b-IN-2 (Example 8) is an orally bioavailable compound, can inhibit the E3 enzyme Casitas B-lineage lymphoma proto-oncogene-b (Cbl-b) in the ubiquitin proteasome pathway. Cbl-b-IN-2 can be used to modulate the immune system and diseases amenable to immune system modulation. Cbl-b-IN-2 (Example 8) also may be administered to an individual with cancer, either alone or as part of a combination, with one or more of an immune checkpoint inhibitor, an anti-neoplastic agent, and radiation agent.
For research use only. We do not sell to patients.
- CAS No.: 2503325-21-9
- Formula: C29H30F5N5O2
- Molecular Weight:575.57
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
Cbl-b-IN-2 (Example 8) is a Cbl-b inhibitor with IC50 values range of 5.1-100 nM and <1 nM in high and low concentration of Cbl-b, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Immune cell
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Concentration:0.125 nM, 0.15 nM
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Incubation Time:1 h
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Result:Showed Cbl-b activity with an with IC50 values range of 5.1-100 nM and ﹤1 nM in high and low concentration of Cbl-b, respectively.
Chemical Information
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CAS No. 2503325-21-9
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Appearance Solid
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Molecular Weight 575.57
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Formula C29H30F5N5O2
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Color Off-white to light yellow
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SMILES
O=C1N(C2=CC=CC(C3(CC4=NN=CN4C)COC3)=C2)CC5=C1C=C(CN6C[C@@H](C)C(F)(F)CC6)C=C5C(F)(F)F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 140 mg/mL (243.24 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 3.5 mg/mL (6.08 mM); Clear solution
This protocol yields a clear solution of ≥ 3.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (35.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 3.5 mg/mL (6.08 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 3.5 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 (35.0 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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.
Purity & Documentation
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Data Sheet (273 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
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 | 1.7374 mL | 8.6870 mL | 17.3741 mL | 43.4352 mL |
| 5 mM | 0.3475 mL | 1.7374 mL | 3.4748 mL | 8.6870 mL | |
| 10 mM | 0.1737 mL | 0.8687 mL | 1.7374 mL | 4.3435 mL | |
| 15 mM | 0.1158 mL | 0.5791 mL | 1.1583 mL | 2.8957 mL | |
| 20 mM | 0.0869 mL | 0.4344 mL | 0.8687 mL | 2.1718 mL | |
| 25 mM | 0.0695 mL | 0.3475 mL | 0.6950 mL | 1.7374 mL | |
| 30 mM | 0.0579 mL | 0.2896 mL | 0.5791 mL | 1.4478 mL | |
| 40 mM | 0.0434 mL | 0.2172 mL | 0.4344 mL | 1.0859 mL | |
| 50 mM | 0.0347 mL | 0.1737 mL | 0.3475 mL | 0.8687 mL | |
| 60 mM | 0.0290 mL | 0.1448 mL | 0.2896 mL | 0.7239 mL | |
| 80 mM | 0.0217 mL | 0.1086 mL | 0.2172 mL | 0.5429 mL | |
| 100 mM | 0.0174 mL | 0.0869 mL | 0.1737 mL | 0.4344 mL |