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Rilzabrutinib

Cat. No. M10605
Rilzabrutinib Structure
Synonym:

PRN1008

Size Price Availability Quantity
5mg USD 350  USD350 In stock
10mg USD 550  USD550 In stock
25mg USD 1100  USD1100 In stock
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Quality Control & Documentation
Biological Activity

Rilzabrutinib, also known as PRN1008, is a reversible covalent, selective and oral active inhibitor of Bruton’s Tyrosine Kinase (BTK) with IC50 of 1.3 nM. Cysteine targeting of BTK by Rilzabrutinib results in a slow off-rate demonstrated by retention of 79±2% of binding to BTK in PBMC 18 hours after washing away the compound in vitro. The covalent cysteine binding is completely reversible after denaturation of the target. Anti-IgM induces human B cell proliferation (10% serum) and B cell CD69 expression are inhibited by Rilzabrutinib with IC50 of 5±2.4 nM and 123±38 nM, respectively.

Chemical Information
Molecular Weight 665.76
Formula C36H40FN9O3
CAS Number 1575596-29-0
Solubility (25°C) DMSO ≥ 100 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Rundan Duan, et al. Front Cardiovasc Med. Effects of the Btk-Inhibitors Remibrutinib (LOU064) and Rilzabrutinib (PRN1008) With Varying Btk Selectivity Over Tec on Platelet Aggregation and in vitro Bleeding Time

[2] Aikaterini Patsatsi, et al. Front Med (Lausanne). Bruton Tyrosine Kinase Inhibition and Its Role as an Emerging Treatment in Pemphigus

[3] Datong Zhang, et al. Molecules. Recent Advances in BTK Inhibitors for the Treatment of Inflammatory and Autoimmune Diseases

[4] Claire L Langrish, et al. J Immunol. Preclinical Efficacy and Anti-Inflammatory Mechanisms of Action of the Bruton Tyrosine Kinase Inhibitor Rilzabrutinib for Immune-Mediated Disease

[5] Patrick F Smith, et al. Br J Clin Pharmacol. A phase I trial of PRN1008, a novel reversible covalent inhibitor of Bruton's tyrosine kinase, in healthy volunteers

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Keywords: Rilzabrutinib, PRN1008 supplier, BTK, inhibitors, activators


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