Branebrutinib (BMS-986195)

Catalog No.S8832 Batch:S883201

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Technical Data

Formula

C20H23FN4O2
Molecular Weight 370.42 CAS No. 1912445-55-6
Solubility (25°C)* In vitro DMSO 74 mg/mL (199.77 mM)
Ethanol 38 mg/mL (102.58 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 3.7mg/ml (9.99mM) Taking the 1 mL working solution as an example, add 50 μL of 74 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 0.37mg/ml (1.00mM) Taking the 1 mL working solution as an example, add 50 μL of 7.4 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Branebrutinib (BMS-986195) is a potent inhibitor of BTK, with IC50 values of 0.1 nM, 0.9 nM, 1.5 nM, and 5 nM for BTK, TEC, BMX, and TXK, respectively.
Targets
BTK [1]
(Cell-free assay)		 TEC [1]
(Cell-free assay)		 BMX [1]
(Cell-free assay)		 TXK [1]
(Cell-free assay)
0.1 nM 0.9 nM 1.5 nM 5 nM
In vitro

In human whole blood assays, Branebrutinib (BMS-986195) potently inhibited BCR-stimulated expression of CD69 on B cells with an IC50 of 11 nM. It is highly selective, providing >5,000-fold selectivity for BTK over 240 kinases with only the 4 related Tec family kinases demonstrating less than 5000-fold selectivity (9 - 1,000-fold)[1].
In vivo

In multi-species pharmacokinetic studies, the absolute oral bioavailability of Branebrutinib (BMS-986195) is 100% in mice, 74% in rats, 46% in cynomolgus monkeys, and 81% in dogs. The total body plasma clearance of this compound is low in all species. The steadystate volume of distribution observed is greater than the plasma volume but less than the total body water, indicative of extravascular distribution, in spite of the high protein binding (free fraction: 0.2-1.2%). Brain penetration is very low in mice, rats, and dogs (<5% of plasma concentration). Both the plasma T1/2 (i.v.) and Tmax (p.o.) values were short across species (0.46-4.3 h and 0.58-1.0 h, respectively）[1].

Protocol (from reference)

Animal Study:

[1]
  • Animal Models

    NZB/W lupus-prone mouse model

  • Dosages

    0.2, 0.5, and 1.5 mg/kg

  • Administration

    by oral gavage

References

  • https://www.ncbi.nlm.nih.gov/pubmed/?term=30893553

Selleck's Branebrutinib (BMS-986195) Has Been Cited by 4 Publications

Branebrutinib (BMS-986195), a Bruton's Tyrosine Kinase Inhibitor, Resensitizes P-Glycoprotein-Overexpressing Multidrug-Resistant Cancer Cells to Chemotherapeutic Agents [ Front Cell Dev Biol, 2021, 9:699571] PubMed: 34350184
Assessment of the effects of Syk and BTK inhibitors on GPVI-mediated platelet signaling and function [ Am J Physiol Cell Physiol, 2021, 320(5):C902-C915] PubMed: 33689480
Effects of Inhibitors against Syk-BTK-PI3K Signaling on Platelet Function [ ScholarsArchive@OSU, 2020, 51] PubMed: N/A
Effects of Inhibitors against Syk-BTK-PI3K Signaling on Platelet Function [ ScholarsArchive@OSU, 2020, None] PubMed: None

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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