Home Angiogenesis BTK inhibitor PRN1008 For research use only.

PRN1008

Synonyms: Rilzabrutinib

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 Chemical Structure

PRN1008 Chemical Structure

CAS: 1575596-29-0

Purity & Quality Control

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

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Signaling Pathway

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BTK Signaling Pathway

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Biological Activity

Description PRN1008 (Rilzabrutinib) is a reversible covalent, selective and oral active inhibitor of Bruton’s Tyrosine Kinase (BTK), with an IC50 of 1.3 nM.
Targets
BTK [1]
1.3 nM
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05104892 Active not recruiting
Asthma
Sanofi
 December 12 2021 Phase 2
NCT05107115 Active not recruiting
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
NCT03762265 Terminated
Pemphigus
Principia Biopharma a Sanofi Company|Sanofi
 January 8 2019 Phase 3

Chemical Information & Solubility

Molecular Weight 665.76 Formula

C36H40FN9O3
CAS No. 1575596-29-0 SDF --
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
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (150.2 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

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.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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