Itacitinib
Based on 23 publication(s) in Google Scholar
Itacitinib (INCB039110) is an orally active and selective inhibitor of JAK1 with an IC50 of 2 nM for human JAK1. Itacitinib shows >20-fold selectivity for JAK1 over JAK2 and >100-fold over JAK3 and TYK2; Itacitinib is used in the research of myelofibrosis.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.97%
- CAS 番号: 1334298-90-6
- 分子式: C26H23F4N9O
- 分子量:553.51
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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Epigenetics Compound Library
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MedChemExpress（MCE）の使用を引用している文献 Itacitinib
More- Nature. 2025 Jun;642(8066):201-211. [Abstract]
- Circulation. 2024 Oct 15;150(16):1302-1305. [Abstract]
- Nat Commun. 2025 Sep 29;16(1):8560. [Abstract]
- Leukemia. 2019 Aug;33(8):1964-1977. [Abstract]
- Mol Syst Biol. 2024 Jan;20(1):28-55. [Abstract]
- Oncogene. 2024 Oct;43(41):3062-3077. [Abstract]
- J Autoimmun. 2019 May:99:39-47. [Abstract]
- J Med Chem. 2024 Jun 27;67(12):10012-10024. [Abstract]
- EMBO Rep. 2019 Jun;20(6):e47202. [Abstract]
- JCI Insight. 2021 Apr 8;6(7):e142205. [Abstract]
- Biochem Pharmacol. 2025 Oct:240:117120. [Abstract]
- Biochem Pharmacol. 2020 Aug;178:114103. [Abstract]
- CNS Neurosci Ther. 2025 Sep;31(9):e70609. [Abstract]
- Int Immunopharmacol. 2024 Jun 21:137:112523. [Abstract]
- Cell Rep Methods. 2023 Oct 23;3(10):100599. [Abstract]
- J Immunol. 2023 Feb 1;210(3):229-244. [Abstract]
- J Leukoc Biol. 2022 Nov;112(5):1343-1356. [Abstract]
- Technol Cancer Res Treat. 2025 Jan-Dec:24:15330338251406931. [Abstract]
- Fundam Clin Pharmacol. 2021 Oct;35(5):919-929. [Abstract]
- Eur J Drug Metab Pharmacokinet. 2021 Sep;46(5):625-635. [Abstract]
- SSRN. 2026 May 21.
- bioRxiv. 2026 Mar 7.
- bioRxiv. 2025 February 21.
生物活性
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JAK1 |
Itacitinib (INCB039110) is a potent and selective inhibitor of JAK1, with >20-fold selectivity for JAK1 over JAK2 and >100-fold over JAK3 and TYK2. Itacitinib is used in the research of myelofibrosis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1334298-90-6
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性状 Solid
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分子量 553.51
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分子式 C26H23F4N9O
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Color White to light yellow
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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
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別名
INCB039110
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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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Journal Impact Factor
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Most Recent
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Nature
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 -
Leukemia
Stem cell persistence in CML is mediated by extrinsically activated JAK1-STAT3 signaling. [Abstract]2019 Aug;33(8):1964-1977. PMID: 30842608 -
Mol Syst Biol
Illuminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics. [Abstract]2024 Jan;20(1):28-55. PMID: 38177929 -
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 -
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 -
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 -
EMBO Rep
Tau accumulation triggers STAT1-dependent memory deficits by suppressing NMDA receptor expression. [Abstract]2019 Jun;20(6):e47202. PMID: 31085626 -
JCI Insight
2021 Apr 8;6(7):e142205. PMID: 33830087 -
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 -
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 -
Int Immunopharmacol
APLNR inhibited nasopharyngeal carcinoma growth and immune escape by downregulating PD-L1. [Abstract]2024 Jun 21:137:112523. PMID: 38909500 -
Cell Rep Methods
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]2023 Oct 23;3(10):100599. PMID: 37797618 -
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
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
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 -
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溶剤 & 溶解度
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.
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (278 KB)
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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)
- Portuguese - PT (480 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Mascarenhas JO, et al. Primary analysis of a phase II open-label trial of INCB039110, a selective JAK1 inhibitor, in patients with myelofibrosis. Haematologica. 2017 Feb;102(2):327-335. [Content Brief]
[2]. Alain Lescoat, 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 Jun 17;114103. [Content Brief]
Complete Stock Solution Preparation Table
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.
| 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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