Cat. No.: HY-16997

Itacitinib

(Synonyms: INCB039110)

23 Cited Publications

Customer Review

Based on 23 publication(s) in Google Scholar

Itacitinib (INCB039110) is an orally active selective inhibitor of JAK1 with an IC₅₀ value of 2 nM for human JAK1. Itacitinib inhibits IFN-γ-mediated phosphorylation of STAT1 and downstream pro-inflammatory signaling pathways. Itacitinib reduces the frequency and number of splenic neutrophils in mouse models, downregulates the levels of pro-inflammatory cytokines and chemokines, and inhibits pro-inflammatory gene expression pathways. Itacitinib improves survival rate and clinical scores in mouse models of hemophagocytic lymphohistiocytosis (HLH), and also suppresses metastasis in NSCLC models with high Rab1A expression. Itacitinib can be used for research on hemophagocytic lymphohistiocytosis and non-small cell lung cancer.

For research use only. We do not sell to patients.

Purity: 99.97%
CAS No.: 1334298-90-6
Formula: C₂₆H₂₃F₄N₉O
Molecular Weight:553.51

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Itacitinib Chemical Structure

CAS No.: 1334298-90-6

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (23)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]^[4]

JAK1

2 nM (IC₅₀)

STAT1

All JAK Isoforms :

All STAT Isoforms :

In Vitro

Itacitinib adipate (50-2500 nM; 1 h pretreatment) dose-dependently inhibits IFN-γ-induced STAT1 phosphorylation in bone marrow-derived macrophages, with significant suppression observed at 2500, 500, and 50 nM concentrations^[1].
Itacitinib (INCB039110) is a potent and selective JAK1 inhibitor with an IC₅₀ value of 2 nM for human JAK1. Its selectivity for JAK1 is more than 20 times that for JAK2, and its selectivity for JAK3 and TYK2 is more than 100 times^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Itacitinib adipate (120 mg/kg; p.o.; twice daily; for 5 or 6 consecutive days) significantly improves survival rate and clinical scores in mouse models of secondary HLH, while reducing tissue neutrophilia levels and the levels of multiple proinflammatory cytokines^[1].
Itacitinib adipate (120 mg/kg; p.o.; twice daily; for 30 consecutive days) is well tolerated in untreated wild-type mice and effectively inhibits IFN-γ-induced STAT1 phosphorylation in vivo^[1].
Itacitinib adipate (120 mg/kg; p.o.; twice daily; for 5 or 26 consecutive days) partially improves survival rate and clinical scores in a primary HLH mouse model, and exerts only mild effects on disease-related immune parameters and transcriptional profiles^[1].
Itacitinib adipate (25 mg/kg; intraperitoneal injection; administration schedule consists of 9 cycles, with 5 consecutive days of dosing followed by 2 days of withdrawal per cycle, lasting for 2 months) significantly inhibits the metastasis of non-small cell lung cancer with high Rab1A expression in the xenograft model derived from the A549-Rab1A-OE cell line, reduces bioluminescence flux and the number of metastatic organs; it also significantly reduces the number of metastatic organs in the non-small cell lung cancer xenograft model derived from the H358 cell line^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

C57BL/6J wildtype (sex- and age-matched, 8 to 12 weeks old; secondary HLH induced by intraperitoneal injection of CpG 1826 (HY-146245) and anti-IL-10 receptor antibody)^[1]
Dosage:

120 mg/kg
Administration:

p.o.; twice daily; 5 or 6 days
Result:

Markedly extended survival versus vehicle.
Lowered clinical scores with equivalent efficacy to ruxolitinib.
Exerted no beneficial effects on splenomegaly or thrombocytopenia, and aggravated anemia relative to vehicle.
Sharply lowered the proportion and count of splenic neutrophils (CD80+ neutrophils included).
Dropped serum CXCL10, IL-12(p70), IL-6, GM-CSF, MCP-1 and MIP1a concentrations significantly.

Animal Model:

C57BL/6J Prf1tm1Sdz/J (perforin-deficient, sex- and age-matched, 8 to 12 weeks old; primary HLH induced by intraperitoneal infection with LCMV)^[1]
Dosage:

120 mg/kg
Administration:

p.o.; twice daily; 5 or 26 days
Result:

Partially elevated survival relative to vehicle.
Reduced clinical disease scores relative to vehicle.
Alleviated splenomegaly at day 9 post-infection, with no impact on anemia or thrombocytopenia.
Failed to lower serum IFN-γ, TNF and sCD25 concentrations.
Did not alter total, CD44+ effector or gp33-specific splenic CD8 T cell populations, nor suppress IFN-γ secretion from these cells.
Repressed proinflammatory (IL-2 STAT5, IFN-α, IFN-γ response) and heme metabolism pathways in splenic CD8 T cells.
Suppressed proinflammatory IL-6 JAK STAT3, IFN-α and IFN-γ response pathways while boosting Myc-driven proliferation and oxidative phosphorylation metabolism in splenic monocytes; each cell subset only presented 3 distinct differentially expressed genes versus vehicle.

Animal Model:

C57BL/6J wildtype (sex- and age-matched, 8 to 12 weeks old)^[1]
Dosage:

120 mg/kg
Administration:

p.o.; twice daily; 30 days
Result:

Showed no significant untoward effects on clinical score, body weight, bone marrow cellularity, or peripheral blood cell counts compared to vehicle-treated controls.
Significantly decreased the percentage of pSTAT1+ F4/80+ peritoneal macrophages and the fold-change mean fluorescence intensity of pSTAT1 compared to vehicle-treated mice after IFN-γ stimulation.

Animal Model:

BALB/c nude (male, 6-8 weeks old, inoculated via tail vein with luciferase-expressing A549-Rab1A-OE cells)
^[2]
Dosage:

25 mg/kg
Administration:

i.p.; 9 cycles of 5 consecutive days on medication followed by 2 consecutive days off; over 2 months
Result:

Reduced total bioluminescence flux from a median of ~7.0 lg[p/s] in controls to ~6.0 lg[p/s].
Decreased the number of metastatic organs from a median of ~6 organs in controls to ~2 organs.

Animal Model:

BALB/c nude (male, 6-8 weeks old, inoculated via tail vein with H358 cells)^[2]
Dosage:

25 mg/kg
Administration:

i.p.; 9 cycles of 5 consecutive days on medication followed by 2 consecutive days off; over 2 months
Result:

Decreased the number of metastatic organs from a median of ~6 organs in controls to ~2 organs.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1334298-90-6
Appearance Solid
Molecular Weight 553.51
Formula C₂₆H₂₃F₄N₉O
Color White to light yellow
SMILES

N#CCC1(N2N=CC(C3=C4C(NC=C4)=NC=N3)=C2)CN(C5CCN(C(C6=C(F)C(C(F)(F)F)=NC=C6)=O)CC5)C1
Synonyms

INCB039110
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (23)

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Nature

Microbial metabolite drives ageing-related clonal haematopoiesis via ALPK1. [Abstract]

2025 Jun;642(8066):201-211. PMID: 40269158
Circulation

Sustained but Decoyed Activation of the JAK1-STAT Pathway by Aberrant Protein Aggregation Exacerbates Proteotoxicity. [Abstract]

2024 Oct 15;150(16):1302-1305. PMID: 39401278
Nat Commun

A loss-of-function human ADAR variant activates innate immune response and promotes bowel inflammation. [Abstract]

2025 Sep 29;16(1):8560. PMID: 41022715
Oncogene

RBM12 drives PD-L1-mediated immune evasion in hepatocellular carcinoma by increasing JAK1 mRNA translation. [Abstract]

2024 Oct;43(41):3062-3077. PMID: 39187545
Leukemia

Stem cell persistence in CML is mediated by extrinsically activated JAK1-STAT3 signaling. [Abstract]

2019 Aug;33(8):1964-1977. PMID: 30842608
J Med Chem

Functional and Structural Characterization of Clinical-Stage Janus Kinase 2 Inhibitors Identifies Determinants for Drug Selectivity. [Abstract]

2024 Jun 27;67(12):10012-10024. PMID: 38843875
JCI Insight

Selective inhibition of JAK3 signaling is sufficient to reverse alopecia areata. [Abstract]

2021 Apr 8;6(7):e142205. PMID: 33830087
J Autoimmun

Autophagy promotes aortic adventitial fibrosis via the IL-6/Jak1 signaling pathway in Takayasu's arteritis. [Abstract]

2019 May:99:39-47. PMID: 30765261
Mol Syst Biol

Illuminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics. [Abstract]

2024 Jan;20(1):28-55. PMID: 38177929
CNS Neurosci Ther

Network Pharmacology-Based and Experimental Validation Elucidate the Target Mechanism of Vinorine in Ameliorating Secondary Brain Injury After Intracerebral Hemorrhage. [Abstract]

2025 Sep;31(9):e70609. PMID: 40994248
Biochem Pharmacol

Dual inhibition of EGR1/STAT3 transcriptional hubs suppresses macrophage-driven liver fibrosis: A multi-omics-guided drug repurposing strategy. [Abstract]

2025 Oct:240:117120. PMID: 40623460
Biochem Pharmacol

Combined anti-fibrotic and anti-inflammatory properties of JAK-inhibitors on macrophages in vitro and in vivo: Perspectives for scleroderma-associated interstitial lung disease. [Abstract]

2020 Aug:178:114103. PMID: 32562787
EMBO Rep

Tau accumulation triggers STAT1-dependent memory deficits by suppressing NMDA receptor expression. [Abstract]

2019 Jun;20(6):e47202. PMID: 31085626
Cell Rep Methods

RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]

2023 Oct 23;3(10):100599. PMID: 37797618
Int Immunopharmacol

APLNR inhibited nasopharyngeal carcinoma growth and immune escape by downregulating PD-L1. [Abstract]

2024 Aug 20:137:112523. PMID: 38909500
J Immunol

IL-10 Negatively Controls the Primary T Cell Response of Tilapia by Triggering the JAK1/STAT3/SOCS3 Axis That Suppresses NF-κB and MAPK/ERK Signaling. [Abstract]

2023 Feb 1;210(3):229-244. PMID: 36548476
J Leukoc Biol

HIV-1-induced type I IFNs promote viral latency in macrophages. [Abstract]

2022 Nov;112(5):1343-1356. PMID: 35588262
Technol Cancer Res Treat

Combining Radiation and anti-PD-L1 Enhances the Antitumor Activity in Colorectal Cancer via IFN-γ-Dependent Activation of STAT1. [Abstract]

2025 Jan-Dec:24:15330338251406931. PMID: 41406067
Fundam Clin Pharmacol

Inhibition of organic cation transporter 3 activity by tyrosine kinase inhibitors. [Abstract]

2021 Oct;35(5):919-929. PMID: 33523504
Eur J Drug Metab Pharmacokinet

Differential Inhibition of Equilibrative Nucleoside Transporter 1 (ENT1) Activity by Tyrosine Kinase Inhibitors. [Abstract]

2021 Sep;46(5):625-635. PMID: 34275128
SSRN

2026 May 21.
bioRxiv

2026 Mar 7.
bioRxiv

2025 February 21.

Solvent & Solubility

In Vitro:

DMSO : ≥ 30 mg/mL (54.20 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8067 mL

9.0333 mL

18.0665 mL

5 mM

0.3613 mL

1.8067 mL

3.6133 mL

10 mM

0.1807 mL

0.9033 mL

1.8067 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.52 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.52 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.52 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (289 KB)
SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Keenan C, et al. Differential effects of itacitinib, fedratinib, and ruxolitinib in mouse models of hemophagocytic lymphohistiocytosis. Blood. 2024 Jun 06;143(23):2386-2400. [Content Brief]

[2]. Huang T, et al. Rab1A promotes IL-4R/JAK1/STAT6-dependent metastasis and determines JAK1 inhibitor sensitivity in non-small cell lung cancer. Cancer Letters, 2021, 523: 182-194.

[3]. Carmona-Rocha E, et al. New and Emerging Oral/Topical Small-Molecule Treatments for Psoriasis. Pharmaceutics. 2024 Feb 06;16(2):239. [Content Brief]

[4]. Lescoat A, et al. Combined anti-fibrotic and anti-inflammatory properties of JAK-inhibitors on macrophages in vitro and in vivo: Perspectives for scleroderma-associated interstitial lung disease. Biochem Pharmacol. 2020 Aug;178:114103. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8067 mL	9.0333 mL	18.0665 mL	45.1663 mL
	5 mM	0.3613 mL	1.8067 mL	3.6133 mL	9.0333 mL
	10 mM	0.1807 mL	0.9033 mL	1.8067 mL	4.5166 mL
	15 mM	0.1204 mL	0.6022 mL	1.2044 mL	3.0111 mL
	20 mM	0.0903 mL	0.4517 mL	0.9033 mL	2.2583 mL
	25 mM	0.0723 mL	0.3613 mL	0.7227 mL	1.8067 mL
	30 mM	0.0602 mL	0.3011 mL	0.6022 mL	1.5055 mL
	40 mM	0.0452 mL	0.2258 mL	0.4517 mL	1.1292 mL
	50 mM	0.0361 mL	0.1807 mL	0.3613 mL	0.9033 mL

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Itacitinib

Bioactive Compound Library Max

Bioactive Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Obesity Compound Library

Transcription Factor-Targeted Library

Targeted Diversity Library

Anti-Liver Cancer Compound Library

Rare Diseases Drug Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Autoimmune Disease Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Itacitinib

All JAK Isoforms

All STAT Isoforms

Biological Activity

Chemical Information

Publications (23)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Itacitinib Related Classifications

HY-16997 Related Classifications