Home Protein Tyrosine Kinase BTK inhibitor Branebrutinib (BMS-986195) For research use only.

Branebrutinib (BMS-986195)

Branebrutinib (BMS-986195) is a potent inhibitor of BTK with IC50 values of 0.1 nM, 0.9 nM, 1.5 nM, 5 nM for BTK, TEC, BMX, TXK, respectively.

Branebrutinib (BMS-986195) Chemical Structure

Branebrutinib (BMS-986195) Chemical Structure

CAS No. 1912445-55-6

Purity & Quality Control

Batch: S883201 DMSO]74 mg/mL]false]Ethanol]38 mg/mL]false]Water]Insoluble]false Purity: 99.87%
99.87

Branebrutinib (BMS-986195) Related Products

Signaling Pathway

BTK Signaling Pathways

BTK Signaling Pathway

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, 5 nM for BTK, TEC, BMX, 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 vitro

In human whole blood assays, BMS-986195 potently inhibited BCR-stimulated expression of CD69 on B cells with an IC50 of 11 nM. BMS-986195 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 vivo

In multi-species pharmacokinetic studies, the absolute oral bioavailability of BMS-986195 is 100% in mice, 74% in rats, 46% in cynomolgus monkeys, and 81% in dogs. The total body plasma clearance of BMS-986195 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].
Animal Research Animal Models NZB/W lupus-prone mouse model
Dosages 0.2, 0.5, and 1.5 mg/kg
Administration by oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04515628 Completed
Healthy Participants
Bristol-Myers Squibb
 August 2 2020 Phase 1
NCT03245515 Completed
Rheumatoid Arthritis
Bristol-Myers Squibb
 August 15 2017 Phase 1
NCT02705989 Completed
Rheumatoid Arthritis
Bristol-Myers Squibb
 August 18 2016 Phase 1

Chemical Information & Solubility

Molecular Weight 370.42 Formula

C20H23FN4O2
CAS No. 1912445-55-6 SDF --
Smiles CC#CC(=O)NC1CCCN(C1)C2=C(C=C(C3=C2C(=C(N3)C)C)C(=O)N)F
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 74 mg/mL ( (199.77 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 38 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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