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PRN1008 Inhibitor

For Research Use Only. Not for use in diagnostic procedures. Catalog #: MBS5753723

PRN1008 is a reversible covalent, selective and oral active inhibitor of Bruton's Tyrosine Kinase (BTK)(IC50 of 1.3nM). More details

Product Documentation
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Sample Manual Insert View PDF
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Testing Data View PDF
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Certificate of Analysis (COA) View PDF
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QC Report View PDF
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Material Safety Data Sheet View PDF
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Technical Datasheet View PDF
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Protocol View PDF

Product Overview

Online Datasheet in PDF
Product Name
PRN1008, Inhibitor
Full Product Name
PRN1008
Product Gene Name
Form/Format
Solid. Powder
Purity/Purification
99.76%
Preparation and Storage
Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent
Molecular Weight
665.76
Solubility
DMSO: 130mg/mL (195.27mM)
(<1mg/ml refers to the product slightly soluble or insoluble)
Formula
C36H40FN9O3
SMILES
CC(C)(\C=C(/C#N)C(=O)N1CCC[C@H](C1)n1nc(-c2ccc(Oc3ccccc3)cc2F)c2c(N)ncnc12)N1CCN(CC1)C1COC1
CAS Number
1575596-29-0
Target & IC50
BTK: ic50 1.3nM
BMX: ic50 1.0nM
ITK: ic50 440nM
TEC: ic50 0.8nM
RLK: ic50 1.2nM
BLK: ic50 6.3nM
EGFR: ic50 520nM
ERBB2: ic50 3900nM
ERBB4: ic50 11.3nM

Product Categories/Family for PRN1008, inhibitor

Structure of PRN1008, inhibitor

PRN1008 Inhibitor – Cat# MBS5753723

Product References and Citations for PRN1008, inhibitor

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.
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.
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.
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.

Other Notes

Small volumes of PRN1008, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

Searchable Terms for PRN1008 purchase

MBS5753723 is an inhibitor targeting PRN1008.
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