Itacitinib (INCB39110)

Catalog No.S7812

For research use only.

Itacitinib(INCB39110) is an orally bioavailable inhibitor of Janus-associated kinase 1 (JAK1) with potential antineoplastic activity.

Itacitinib (INCB39110) Chemical Structure

CAS No. 1334298-90-6

Purity & Quality Control

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Biological Activity

Description Itacitinib(INCB39110) is an orally bioavailable inhibitor of Janus-associated kinase 1 (JAK1) with potential antineoplastic activity.
Targets
JAK1 [1]
In vitro

INCB039110 is a potent and selective inhibitor of JAK1, with >20 and >200-fold selectivity over JAK2 and JAK3, respectively. The activity against JAK1, 2, 3, and TYK2 are 2, 63, >2000, and 795 nM, respectively[1].

In vivo INCB039110 blocks tumor growth in human pancreatic xenograft models in mice at clinically relevant doses, both as monotherapy and in combination with cytotoxic agents such as gemcitabine[2].

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 553.51
Formula

C26H23F4N9O

CAS No. 1334298-90-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CN(CCC1N2CC(C2)(CC#N)N3C=C(C=N3)C4=C5C=CNC5=NC=N4)C(=O)C6=C(C(=NC=C6)C(F)(F)F)F

In vivo Formulation Calculator (Clear solution)

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

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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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05063110 Recruiting Drug: Itacitinib Adults Patients Having Non Severe HLH Assistance Publique - Hôpitaux de Paris|Incyte Corporation May 1 2022 Phase 2
NCT04239989 Recruiting Drug: Itacitinib|Drug: Itacitinib Adipate Bronchiolitis Obliterans M.D. Anderson Cancer Center April 8 2021 Phase 1
NCT04220632 Terminated Drug: Itacitinib|Drug: Prednisone|Drug: Methylprednisolone GVHDAcute Innovent Biologics (Suzhou) Co. Ltd. June 18 2020 Phase 1|Phase 2
NCT03978637 Active not recruiting Drug: Itacitinib Bronchiolitis Obliterans Syndrome Incyte Corporation February 4 2020 Phase 1|Phase 2
NCT04070781 Recruiting Drug: Itacitinib|Drug: Tocilizumab Steroid Refractory GVHD|Graft Vs Host Disease Amer Assal|Incyte Corporation|Columbia University January 20 2020 Phase 1
NCT03721965 Terminated Drug: Itacitinib|Drug: Corticosteroids Acute Graft-versus-host Disease Incyte Corporation December 31 2019 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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