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Poseltinib BTK inhibitor

Cat.No.E2843

Poseltinib (HM71224, LY3337641) shows a highly selective inhibition for Bruton’s tyrosine kinase (BTK) with IC50 of 1.95 nM, in which the selectivity toward other BMX, TEC and TXK are 0.3, 2.3 and 2.4 fold, respectively. 
Poseltinib BTK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 470.52

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

Quality Control

Batch: E284301 DMSO]94 mg/mL]false]Ethanol]23 mg/mL]false]Water]Insoluble]false Purity: 99.31%
99.31

Chemical Information, Storage & Stability

Molecular Weight 470.52 Formula

C26H26N6O3

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1353552-97-2 -- Storage of Stock Solutions

Synonyms HM71224, LY3337641 Smiles CN1CCN(CC1)C2=CC=C(NC3=NC(=C4OC=CC4=N3)OC5=CC(=CC=C5)NC(=O)C=C)C=C2

Solubility

In vitro
Batch:

DMSO : 94 mg/mL (199.77 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 23 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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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]
(in kinase assays)
1.95 nM
References

Clinical Trial Information

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

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05335018 Recruiting
Relapsed/Refractory Diffuse Large B Cell Lymphoma
Seoul National University Hospital
 May 30 2022 Phase 2
NCT03083561 Completed
Healthy
Eli Lilly and Company
 March 15 2017 Phase 1
NCT02914379 Completed
Healthy
Eli Lilly and Company
 September 2016 Phase 1
NCT02628028 Terminated
Rheumatoid Arthritis
Eli Lilly and Company
 August 22 2016 Phase 2

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