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

Branebrutinib  (Synonyms: BMS-986195)

Cat. No.: HY-112161 Purity: 99.82%
SDS COA Handling Instructions

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Branebrutinib (BMS-986195) is a highly potent, selective covalent, irreversible inhibitor of Bruton’s tyrosine kinase (BTK), with an IC50 of 0.1 nM. Branebrutinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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Branebrutinib Chemical Structure

Branebrutinib Chemical Structure

CAS No. : 1912445-55-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO USD 149 In-stock
Solid
5 mg USD 135 In-stock
10 mg USD 215 In-stock
25 mg USD 430 In-stock
50 mg USD 690 In-stock
100 mg USD 1100 In-stock
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Based on 1 publication(s) in Google Scholar

Branebrutinib Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Branebrutinib

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Branebrutinib (BMS-986195) is a highly potent, selective covalent, irreversible inhibitor of Bruton’s tyrosine kinase (BTK), with an IC50 of 0.1 nM[1][2]. Branebrutinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC50 & Target

IC50: 0.1 nM (BTK)[1].
Cellular Effect
Cell Line Type Value Description References
Ramos IC50
7.2 nM
Compound: 5a; BMS-986195
Inhibition of BTK in human Ramos B cells assessed as reduction in BCR-stimulated calcium flux after 1 hr in dark condition measured for 180 sec
Inhibition of BTK in human Ramos B cells assessed as reduction in BCR-stimulated calcium flux after 1 hr in dark condition measured for 180 sec
[PMID: 30893553]
In Vitro

BMS-986195 is a potent and highly selective inhibitor of BTK, which acts by covalently modifying an active-site cysteine residue. BMS-986195 is more than 5000-fold selective for BTK over all kinases outside of the Tec family, and selectivity ranges from 9- to 1010-fold within the Tec family. BMS-986195 inactivates BTK in human whole blood with a rapid rate of inactivation (3.5×10-4nM-1•min-1) and potently inhibits antigen-dependent interleukin-6 production, CD86 expression and proliferation in B cells (IC50<1 nM) without effect on antigen-independent measures in the same cells. A similar potency is measured against FcγR-dependent TNF-α production in human cells[1].

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

Branebrutinib Related Antibodies
In Vivo

In mice, BMS-986195 demonstrates robust efficacy in murine models of RA including CIA and CAIA, protecting against clinically evident disease, histologic joint damage and bone mineral density loss. In both mice and monkeys, maximal efficacy is observed at doses ≤0.5 mg/kg PO QD, which achieves ≥95% inactivation of BTK in vivo. At similar doses, BMS-986195 is also highly protective against nephritis in the NZB/W mouse model of lupus. To investigate the dynamics of BTK inactivation and resynthesis of BTK, cynomolgus monkeys are given single or multiple doses of BMS-986195. 100% peak inactivation of BTK is obtained with a single administration of BMS-986195 at 0.5 mg/kg PO[1].

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

370.42

Formula

C20H23FN4O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC(F)=C(N2C[C@@H](NC(C#CC)=O)CCC2)C3=C1NC(C)=C3C)N
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 150 mg/mL (404.95 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6996 mL 13.4982 mL 26.9964 mL
5 mM 0.5399 mL 2.6996 mL 5.3993 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
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: ≥ 3.75 mg/mL (10.12 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (37.5 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: ≥ 3.75 mg/mL (10.12 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (37.5 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:

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

Purity: 99.82%

SDS (252 KB)

COA (254 KB) LCMS (263 KB)

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6996 mL 13.4982 mL 26.9964 mL 67.4910 mL
5 mM 0.5399 mL 2.6996 mL 5.3993 mL 13.4982 mL
10 mM 0.2700 mL 1.3498 mL 2.6996 mL 6.7491 mL
15 mM 0.1800 mL 0.8999 mL 1.7998 mL 4.4994 mL
20 mM 0.1350 mL 0.6749 mL 1.3498 mL 3.3745 mL
25 mM 0.1080 mL 0.5399 mL 1.0799 mL 2.6996 mL
30 mM 0.0900 mL 0.4499 mL 0.8999 mL 2.2497 mL
40 mM 0.0675 mL 0.3375 mL 0.6749 mL 1.6873 mL
50 mM 0.0540 mL 0.2700 mL 0.5399 mL 1.3498 mL
60 mM 0.0450 mL 0.2250 mL 0.4499 mL 1.1248 mL
80 mM 0.0337 mL 0.1687 mL 0.3375 mL 0.8436 mL
100 mM 0.0270 mL 0.1350 mL 0.2700 mL 0.6749 mL
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Branebrutinib 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:

Branebrutinib1912445-55-6BMS-986195BMS986195BMS 986195BtkBruton tyrosine kinaseInhibitorinhibitorinhibit

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