RBN013209
Based on 1 publication(s) in Google Scholar
RBN013209 is an orally active small molecule inhibitor of CD38 with an IC50 of 0.01 to 0.1 μM for human CD38. RBN013209 prevents the conversion of extracellular NAD+ to ADPR or cADPR in tumor cells and PBMCs. RBN013209 can be used in the study of tumor. In addition, RBN013209 enables CAR-T cells to maintain the naive state and central memory state, and decreases the expression of cell activation markers and exhaustion-related inhibitory receptors.
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- Reinheit: 98.63%
- CAS. Nr.: 2597933-17-8
- Formel: C19H24N6O3
- Molecular Weight:384.43
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
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Publications Citing Use of MedChemExpress (MCE) RBN013209
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Biologische Aktivität
RBN013209 (50 μM; 72 h) makes more CAR-T cells maintain the naive state and central memory state, and reduces the expression of CAR-T cell activation markers (CD25 and CD69) and exhaustion-related inhibitory receptors (LAG-3, TIM-3 and PD-1)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice[3]
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Dosage:/
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Administration:Oral administration
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Result:Resulted in dose-dependent elevation of NAD+ and reduction of ADPR in various tissues such as spleen and liver in naïve mice.
Had antitumor activity that was associated with changes in NAD+ and ADPR in MC38 tumor model.
Had antitumor activity in combinationwith anti-PD-L1 therapy in B16-F10 tumor-bearing mice.
Chemical Information
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CAS. Nr. 2597933-17-8
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Appearance Solid
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Molecular Weight 384.43
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Formel C19H24N6O3
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Color Off-white to light yellow
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SMILES
COCCO[C@@H](CC1)CC[C@H]1NC(C2=C3C(C=CN3)=NC(N4C=CN=C4)=N2)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell Rep Med
Inhibition of CD38 enzymatic activity enhances CAR-T cell immune-therapeutic efficacy by repressing glycolytic metabolism. [Abstract]2024 Feb 20;5(2):101400. PMID: 38307031
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (260.13 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: ≥ 2.08 mg/mL (5.41 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.41 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Reinheit & Dokumentation
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Data Sheet (274 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)
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 | 2.6013 mL | 13.0063 mL | 26.0125 mL | 65.0313 mL |
| 5 mM | 0.5203 mL | 2.6013 mL | 5.2025 mL | 13.0063 mL | |
| 10 mM | 0.2601 mL | 1.3006 mL | 2.6013 mL | 6.5031 mL | |
| 15 mM | 0.1734 mL | 0.8671 mL | 1.7342 mL | 4.3354 mL | |
| 20 mM | 0.1301 mL | 0.6503 mL | 1.3006 mL | 3.2516 mL | |
| 25 mM | 0.1041 mL | 0.5203 mL | 1.0405 mL | 2.6013 mL | |
| 30 mM | 0.0867 mL | 0.4335 mL | 0.8671 mL | 2.1677 mL | |
| 40 mM | 0.0650 mL | 0.3252 mL | 0.6503 mL | 1.6258 mL | |
| 50 mM | 0.0520 mL | 0.2601 mL | 0.5203 mL | 1.3006 mL | |
| 60 mM | 0.0434 mL | 0.2168 mL | 0.4335 mL | 1.0839 mL | |
| 80 mM | 0.0325 mL | 0.1626 mL | 0.3252 mL | 0.8129 mL | |
| 100 mM | 0.0260 mL | 0.1301 mL | 0.2601 mL | 0.6503 mL |
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