Fenebrutinib

Fenebrutinib (GDC-0853) is a potent, selective, orally available, and noncovalent bruton's tyrosine kinase (Btk) inhibitor with Kis of 0.91 nM, 1.6, 1.3, 12.6, and 3.4 nM for WT Btk, and the C481S, C481R, T474I, T474M mutants. Fenebrutinib has the potential for rheumatoid arthritis and systemic lupus erythematosus research[1].

Product Specifications

CAS Number

[1434048-34-6]

Product Name Alternative

GDC-0853

UNSPSC

12352005

Hazard Statement

H315, H317, H318, H334, H335, H341, H361, H370, H413

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/GDC-0853.html

Purity

99.89

Solubility

DMSO : 20 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C1C(NC(C=C2)=NC=C2N3CCN(C4COC4)C[C@@H]3C)=CC(C5=CC=NC(N6C(C7=CC(CC(C)(C)C8)=C8N7CC6)=O)=C5CO)=CN1C

Molecular Formula

C37H44N8O4

Molecular Weight

664.80

Precautions

H315, H317, H318, H334, H335, H341, H361, H370, H413

References & Citations

[1]Erickson RI , et al. Bruton's Tyrosine Kinase Small Molecule Inhibitors Induce a Distinct Pancreatic Toxicity in Rats. J Pharmacol Exp Ther. 2017 Jan;360 (1) :226-238.|[2]Crawford JJ, et al. Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development. J Med Chem. 2018 Mar 22;61 (6) :2227-2245.