Home JAK/STAT JAK inhibitor Solcitinib For research use only.

Solcitinib

Synonyms: GLPG0778, GSK2586184

Solcitinib (GLPG0778, GSK2586184) is an inhibitor of JAK1 with an IC50 of 8-9 nM, and shows 11-, 55- and 23-fold selectivity over JAK2, JAK3 and TYK2, respectively.

Solcitinib Chemical Structure

Solcitinib Chemical Structure

CAS No. 1206163-45-2

Purity & Quality Control

Solcitinib Related Products

Signaling Pathway

JAK Signaling Pathways

JAK Signaling Pathway

Biological Activity

Description Solcitinib (GLPG0778, GSK2586184) is an inhibitor of JAK1 with an IC50 of 8-9 nM, and shows 11-, 55- and 23-fold selectivity over JAK2, JAK3 and TYK2, respectively.
Targets
JAK2 [1] JAK3 [1] TYK2 [1] JAK1 [1]
8-9 nM
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02000453 Terminated
Colitis Ulcerative
GlaxoSmithKline|Prof Geert D''Haens AMC Amsterdam
 December 20 2013 Phase 1
NCT01336244 Completed
Healthy
Galapagos NV
 April 2011 Phase 1

Chemical Information & Solubility

Molecular Weight 389.45 Formula

C22H23N5O2
CAS No. 1206163-45-2 SDF --
Smiles CC1(CN(C1)C(=O)C2=CC=C(C=C2)C3=CC=CC4=NC(=NN43)NC(=O)C5CC5)C
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 39 mg/mL ( (100.14 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 3 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

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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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