Home Transmembrane Transporters CFTR chemical Icenticaftor (QBW251)

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Icenticaftor (QBW251) CFTR chemical

Cat.No.S9972

Icenticaftor (QBW251, NVP-QBW251) is an oral potentiator of the cystic fibrosis transmembrane conductance regulator (CFTR) channel with EC50 of 79 nM and 497 nM for F508del CFTR and G551D CFTR in Fisher Rat Thyroid (FRT) cells.

Icenticaftor (QBW251) CFTR chemical Chemical Structure

Chemical Structure

Molecular Weight: 361.24

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

Quality Control

Batch: S997201 DMSO]72 mg/mL]false]Ethanol]72 mg/mL]false]Water]Insoluble]false Purity: 99.89%
99.89

Chemical Information, Storage & Stability

Molecular Weight 361.24 Formula

C12H13F6N3O3

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1334546-77-8 -- Storage of Stock Solutions

Solubility

In vitro
Batch:

DMSO : 72 mg/mL (199.31 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 72 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
F508del CFTR [1]
79 nM(EC50)
G551D CFTR [1]
497 nM(EC50)
References

Clinical Trial Information

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

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04396366 Terminated
Bronchiectasis
Novartis Pharmaceuticals|Innovative Medicines Initiative|Novartis
 February 2 2021 Phase 2
NCT04587622 Completed
Hepatic Failure
Novartis Pharmaceuticals|Novartis
 October 30 2020 Phase 1
NCT04268823 Terminated
Chronic Obstructive Pulmonary Disease
Novartis Pharmaceuticals|Novartis
 September 10 2020 Phase 2
NCT02449018 Completed
Chronic Obstructive Pulmonary Disease COPD
Novartis Pharmaceuticals|Novartis
 April 30 2015 Phase 2
NCT02190604 Terminated
Cystic Fibrosis
Novartis Pharmaceuticals|Novartis
 July 31 2012 Phase 1|Phase 2

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