Elsubrutinib
Based on 2 publication(s) in Google Scholar
Elsubrutinib (ABBV-105) is an orally active, potent, selective and irreversible Bruton's tyrosine kinase (BTK) inhibitor. The IC50 of Elsubrutinib for BTK catalytic domain is 0.18 μM. Elsubrutinib can be used for the research of inflammatory disease.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 98.0%
- No. CAS: 1643570-24-4
- Fòrmula: C17H19N3O2
- Peso molecular:297.35
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Elsubrutinib
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Actividad biológica
Descripciòn
IC50 & Target
IC50: 0.18 μM (BTK)[1]
In Vitro
Elsubrutinib inhibits BTK (C481S) with an IC50 of 2.6 μM, indicating a significant loss in potency upon exchanging the targeted thiol nucleophile with an alcohol, suggesting Cys481 is important in the manner in which Elsubrutinib inhibits BTK. Elsubrutinib irreversibly inhibits BTK enzyme activity and blocks BTK-dependent cellular activation. Elsubrutinib inhibits histamine release from IgE-stimulated basophils and IL-6 release from IgG-stimulated monocytes, which utilize Fce and Fcc receptors respectively. Elsubrutinib inhibits IgM-mediated B cell proliferation, which is dependent on signaling through the BCR. Elsubrutinib also inhibits TNF-release from CpG-DNA stimulated PBMCs, which signals through TLR9, although it does not inhibit the function of TLRs that do not use ITAM motifs, namely, TNF release from PBMCs stimulated either through TLR4 (with LPS) or through TLR7/8 (with R848). Elsubrutinib has significant impacts on IgM-mediated B cell proliferation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Elsubrutinib (0.1~10 mg/kg; p.o.) results in dose-dependent inhibition of paw swelling throughout the course of disease and significantly prevents the onset of proteinuria and prolongs survival at the 10 mg/kg QD and BID doses, while lower doses does not significantly inhibit these endpoints[1].
Elsubrutinib demonstrates exposure-dependent inhibition of increases in paw volume. Elsubrutinib significantly inhibits bone volume loss in a dose dependent manner consistent with the observed anti-inflammatory effects[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female C57/BL6 mice[1]
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Dosage:10 mg/kg
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Administration:P.o.
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Result:Inhibited antibody responses to NP-Ficoll and NP-KLH, but not to NP-LPS or Prevnar-13.
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Animal Model:Lewis rats[1]
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Dosage:0.1~10 mg/kg
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Administration:P.o.
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Result:Resulted in dose-dependent inhibition of paw swelling throughout the course of disease.
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Animal Model:NZBWF1 mice[1]
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Dosage:0.1~10 mg/kg
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Administration:P.o.
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Result:Significantly prevented the onset of proteinuria and prolonged survival at the 10 mg/kg QD and BID doses, while lower doses did not significantly inhibit these endpoints.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1643570-24-4
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Appearance Solid
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Peso molecular 297.35
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Fòrmula C17H19N3O2
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Color White to off-white
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SMILES
O=C(C1=CC=C([C@H]2CN(C(C=C)=O)CCC2)C3=C1NC=C3)N
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Synonyms
ABBV-105
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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ACS Pharmacol Transl Sci
Comprehensive Characterization of Bruton's Tyrosine Kinase Inhibitor Specificity, Potency, and Biological Effects: Insights into Covalent and Noncovalent Mechanistic Signatures. [Abstract]2025 Mar 12;8(4):917-931. PMID: 40242575 -
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (336.30 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)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (16.82 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
In Vivo Dissolution Calculator
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.
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 | 3.3630 mL | 16.8152 mL | 33.6304 mL | 84.0760 mL |
| 5 mM | 0.6726 mL | 3.3630 mL | 6.7261 mL | 16.8152 mL | |
| 10 mM | 0.3363 mL | 1.6815 mL | 3.3630 mL | 8.4076 mL | |
| 15 mM | 0.2242 mL | 1.1210 mL | 2.2420 mL | 5.6051 mL | |
| 20 mM | 0.1682 mL | 0.8408 mL | 1.6815 mL | 4.2038 mL | |
| 25 mM | 0.1345 mL | 0.6726 mL | 1.3452 mL | 3.3630 mL | |
| 30 mM | 0.1121 mL | 0.5605 mL | 1.1210 mL | 2.8025 mL | |
| 40 mM | 0.0841 mL | 0.4204 mL | 0.8408 mL | 2.1019 mL | |
| 50 mM | 0.0673 mL | 0.3363 mL | 0.6726 mL | 1.6815 mL | |
| 60 mM | 0.0561 mL | 0.2803 mL | 0.5605 mL | 1.4013 mL | |
| 80 mM | 0.0420 mL | 0.2102 mL | 0.4204 mL | 1.0510 mL | |
| 100 mM | 0.0336 mL | 0.1682 mL | 0.3363 mL | 0.8408 mL |
Elsubrutinib Related Classifications
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