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Rilzabrutinib

Catalog No. T12542   CAS 1575596-29-0
Synonyms: PRN-1008, inhibit, PRN1008, Rilzabrutinib, PRN 1008, Inhibitor, Btk, Bruton tyrosine kinase

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

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Rilzabrutinib, CAS 1575596-29-0
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Purity: 98%
Biological Description
Chemical Properties
Storage & Solubility Information
Description PRN1008 is a reversible covalent, selective and oral active inhibitor of Bruton’s Tyrosine Kinase (BTK)(IC50 of 1.3 nM).
Targets&IC50 TEC:0.8 nM, Bmx:1.0 nM, Itk:440 nM, ErbB2:3900 nM, BTK:1.3 nM, ErbB4:11.3 nM, BLK:6.3 nM, EGFR:520 nM, RLK:1.2 nM
Synonyms PRN-1008, inhibit, PRN1008, Rilzabrutinib, PRN 1008, Inhibitor, Btk, Bruton tyrosine kinase
Molecular Weight 665.76
Formula C36H40FN9O3
CAS No. 1575596-29-0

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 130 mg/mL (195.27 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
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.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Compound Library Inhibitor Library Covalent Inhibitor Library Drug Repurposing Compound Library Anti-Breast Cancer Compound Library Kinase Inhibitor Library Angiogenesis related Compound Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Bioactive Compound Library

Related Products

Related compounds with same targets
(±)-Zanubrutinib BTK inhibitor 1 (Compound 27) SB-633825 PCI-33380 Naluzotan G-744 CHMFL-BTK-01 Spebrutinib besylate

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An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
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An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
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The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.