Branebrutinib

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.

Product Specifications

CAS Number

[1912445-55-6]

Product Name Alternative

BMS-986195

UNSPSC

12352005

Hazard Statement

H315, H319, H320

Target

Btk

Type

Reference compound

Related Pathways

Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/BMS-986195.html

Purity

99.78

Solubility

DMSO : ≥ 150 mg/mL

Smiles

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

Molecular Formula

C20H23FN4O2

Molecular Weight

370.42

Precautions

H315, H319, H320

References & Citations

[1]JR Burke, et al. BMS-986195 Is a Highly Selective and Rapidly Acting Covalent Inhibitor of Bruton’s Tyrosine Kinase with Robust Efficacy at Low Doses in Preclinical Models of RA and Lupus Nephritis. 2017 ACR/ARHP Annual Meeting, September 18, 2017.|[2]Watterson SH, et al. Discovery of Branebrutinib (BMS-986195) : A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK) . J Med Chem. 2019 Apr 11;62 (7) :3228-3250.