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PRN1008 BTK inhibitor

Cat.No.S9944

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

Chemical Structure

Molecular Weight: 665.76

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S994401 DMSO]100 mg/mL]false]Ethanol]100 mg/mL]false]Water]Insoluble]false Purity: 99.05%
99.05

Chemical Information, Storage & Stability

Molecular Weight 665.76 Formula

C36H40FN9O3

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1575596-29-0,1575591-66-0 -- Storage of Stock Solutions

Synonyms Rilzabrutinib Smiles CC(C)(/C=C(C#N)/C(=O)N1CCC(CC1)[N]2N=C(C3=C(F)C=C(OC4=CC=CC=C4)C=C3)C5=C2N=CN=C5N)N6CCN(CC6)C7COC7

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (150.2 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
BTK [1]
1.3 nM
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05104892 Completed
Asthma
Sanofi
 December 12 2021 Phase 2
NCT05107115 Completed
Chronic Spontaneous Urticaria
Sanofi
 November 24 2021 Phase 2
NCT04748926 Completed
Healthy Volunteers
Principia Biopharma a Sanofi Company|Sanofi
 April 7 2021 Phase 1
NCT04562766 Recruiting
Immune Thrombocytopenia
Principia Biopharma a Sanofi Company|Sanofi
 December 14 2020 Phase 3
NCT04520451 Active not recruiting
Immunoglobulin G4 Related Disease
Principia Biopharma a Sanofi Company|Massachusetts General Hospital|Sanofi
 August 22 2020 Phase 2

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