2. Protein Tyrosine Kinase/RTK
  3. Btk
  4. Elsubrutinib

Elsubrutinib  (Synonyms: ABBV-105)

Cat. No.: HY-109143 Purity: ≥98.0%
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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.

For research use only. We do not sell to patients.

Elsubrutinib Chemical Structure

Elsubrutinib Chemical Structure

CAS No. : 1643570-24-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 671 In-stock
Solution
10 mM * 1 mL in DMSO USD 671 In-stock
Solid
1 mg USD 244 In-stock
5 mg USD 610 In-stock
10 mg USD 980 In-stock
25 mg USD 1950 In-stock
50 mg USD 3120 In-stock
100 mg USD 5000 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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Elsubrutinib Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

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[1].

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.

Elsubrutinib Related Antibodies
In Vivo

Elsubrutinib (10 mg/kg; p.o.) inhibits antibody responses to NP-Ficoll and NP-KLH, but not to NP-LPS or Prevnar-13[1].
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.

Animal Model: Female C57/BL6 mice[1]
Dosage: 10 mg/kg
Administration: P.o.
Result: Inhibited antibody responses to NP-Ficoll and NP-KLH, but not to NP-LPS or Prevnar-13.
Animal Model: Lewis rats[1]
Dosage: 0.1~10 mg/kg
Administration: P.o.
Result: Resulted in dose-dependent inhibition of paw swelling throughout the course of disease.
Animal Model: NZBWF1 mice[1]
Dosage: 0.1~10 mg/kg
Administration: P.o.
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.
Clinical Trial
Molecular Weight

297.35

Formula

C17H19N3O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC=C([C@H]2CN(C(C=C)=O)CCC2)C3=C1NC=C3)N
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3630 mL 16.8152 mL 33.6304 mL
5 mM 0.6726 mL 3.3630 mL 6.7261 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.

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

Mass
=
Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

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: ≥ 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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

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 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
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Elsubrutinib 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:

Elsubrutinib1643570-24-4ABBV-105ABBV105ABBV 105BtkBruton tyrosine kinaseorallyactivepotentselectiveirreversibleBruton'styrosinekinaseinflammatoryInhibitorinhibitorinhibit

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