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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 3
Available Sizes
Frequently Asked Questions
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