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Itacitinib (INCB39110)

Name: Itacitinib (INCB39110)
Brand: Selleck Chemicals
SKU: S7812
Rating: 5 (2 reviews)

Catalog No.S7812 Purity: 99.99%

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

Itacitinib (INCB39110) Chemical Structure

CAS: 1334298-90-6

Selleck's Itacitinib (INCB39110) has been cited by 2 publications

Purity & Quality Control

Batch: Purity: 99.99%

99.99

Itacitinib (INCB39110) Related Products

Related Targets	JAK1 JAK2 JAK3 Tyk2	Click to Expand
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Related Compound Libraries	Kinase Inhibitor Library FDA-approved Drug Library Natural Product Library Tyrosine Kinase Inhibitor Library JAK/STAT compound library	Click to Expand

Signaling Pathway

JAK Signaling Pathway

Choose Selective JAK Inhibitors

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 such as gemcitabine^[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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT05063110	Recruiting	Adults Patients Having Non Severe HLH	Assistance Publique - Hôpitaux de Paris\|Incyte Corporation	May 1 2022	Phase 2
NCT04239989	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

References

[4] Chen Y, et al. Evid Based Complement Alternat Med. 2022 May 6;2022:7942623.

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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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

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In vivo
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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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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.

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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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