Itacitinib (INCB39110)

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

Itacitinib (INCB39110) Chemical Structure

Itacitinib (INCB39110) Chemical Structure

CAS No. 1334298-90-6

Purity & Quality Control

Itacitinib (INCB39110) Related Products

Signaling Pathway

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
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].

Cell Research Cell lines Monocyte-Derived Macrophages
Concentrations 1 μM
Incubation Time 1 h
Method

Cells were treated with various concentrations of Itacitinib.

In Vivo
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[2].

Animal Research Animal Models Male Sprague-Dawley rats
Dosages 30 mg/kg
Administration s.c.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05063110 Recruiting
Adults Patients Having Non Severe HLH
Assistance Publique - Hôpitaux de Paris|Incyte Corporation
May 1 2022 Phase 2
NCT04239989 Active not recruiting
Bronchiolitis Obliterans
M.D. Anderson Cancer Center
April 8 2021 Phase 1
NCT04220632 Terminated
GVHDAcute
Innovent Biologics (Suzhou) Co. Ltd.
June 18 2020 Phase 1|Phase 2
NCT03978637 Terminated
Bronchiolitis Obliterans Syndrome
Incyte Corporation
February 4 2020 Phase 1|Phase 2
NCT04070781 Terminated
Steroid Refractory GVHD|Graft Vs Host Disease
Columbia University|Incyte Corporation
January 20 2020 Phase 1
NCT03721965 Terminated
Acute Graft-versus-host Disease
Incyte Corporation
December 31 2019 Phase 1|Phase 2

Chemical Information & Solubility

Molecular Weight 553.51 Formula

C26H23F4N9O

CAS No. 1334298-90-6 SDF --
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
Storage (From the date of receipt)

In vitro
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In vivo
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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.

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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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