Rilzabrutinib

Rilzabrutinib (PRN1008) is a reversible covalent, selective and oral active inhibitor of Bruton’s Tyrosine Kinase (BTK), with an IC50 of 1.3 nM.

Product Specifications

CAS Number

[1575596-29-0]

Product Name Alternative

PRN1008

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; Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/PRN1008.html

Purity

98.97

Solubility

DMSO : ≥ 130 mg/mL

Smiles

NC1=C2C(C3=C(C=C(OC4=CC=CC=C4)C=C3)F)=NN([C@H]5CN(CCC5)C(/C(C#N)=C/C(C)(N6CCN(C7COC7)CC6)C)=O)C2=NC=N1

Molecular Formula

C36H40FN9O3

Molecular Weight

665.76

Precautions

H315, H319, H320

References & Citations

[1]Smith PF, et al. A phase I trial of PRN1008, a novel reversible covalent inhibitor of Bruton's tyrosine kinase, in healthy volunteers. Br J Clin Pharmacol. 2017 Nov;83 (11) :2367-2376.|[2]Hill RJ, Bradshaw JM, Bisconte A, Tam D, Owens TD, Brameld KA, Smith PF, Funk JO, Goldstein DM, Nunn PA. Preclinical Characterization of PRN1008, a Novel Reversible Covalent Inhibitor of BTK that Shows Efficacy in a RAT Model of Collagen-Induced Arthritis. Annals of the Rheumatic Diseases 2015; 74 (Suppl 2) : 216.