Itacitinib (INCB39110)

製品コードS7812 バッチS781202

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₆H₂₃F₄N₉O
	分子量	553.51	CAS No.	1334298-90-6
Solubility (25°C)*	体外


* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

生物活性

製品説明	Itacitinib (INCB39110)は、潜在的な抗腫瘍活性を持つヤヌスキナーゼ1 (JAK1)の経口生物学的に利用可能な阻害剤です。
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.
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.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Monocyte-Derived Macrophages
	濃度	1 μM
	反応時間	1 h
	実験の流れ	Cells were treated with various concentrations of Itacitinib.
動物実験	動物モデル	Male Sprague-Dawley rats
	投薬量	30 mg/kg
	投与方法	s.c.

参考

https://pubmed.ncbi.nlm.nih.gov/27774824/
http://cancerres.aacrjournals.org/content/75/15_Supplement/779
https://pubmed.ncbi.nlm.nih.gov/32562787/

https://pubmed.ncbi.nlm.nih.gov/35571736/

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Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Keloids and inflammation: the crucial role of IL-33 in epidermal changes [ Front Immunol, 2025, 16:1514618]	PubMed: 40230853
The cGAS-STING pathway is a master regulator of OCT4 expression in persistent sarcoma cells and enhances cellular immunotherapy with NK and CIK lymphocytes [ Cancer Immunol Immunother, 2025, 74(10):312]	PubMed: 40986050
Targeting synergetic endothelial inflammation by inhibiting NFKB and JAK-STAT pathways [ iScience, 2025, 28(9):113307]	PubMed: 40894883
Suberosin attenuates rheumatoid arthritis by repolarizing macrophages and inhibiting synovitis via the JAK/STAT signaling pathway [ Arthritis Res Ther, 2025, 27(1):12]	PubMed: 39838477
AKT and EZH2 inhibitors kill TNBCs by hijacking mechanisms of involution [ Nature, 2024, 10.1038/s41586-024-08031-6]	PubMed: 39385030
Novel JAK Inhibitors to Reduce Graft-Versus-Host Disease after Allogeneic Hematopoietic Cell Transplantation in a Preclinical Mouse Model [ Molecules, 2024, 29(8)1801]	PubMed: 38675621
Comprehensive profiling of clinical JAK inhibitors in myeloproliferative neoplasms [ Am J Hematol, 2023, 98(7):1029-1042]	PubMed: 37203407
The rat Achilles and patellar tendons have similar increases in mechanical properties but become transcriptionally divergent during postnatal development [ J Physiol, 2023, 10.1113/JP284393]	PubMed: 37493407
Selective inhibitors of JAK1 targeting an isoform-restricted allosteric cysteine [ Nat Chem Biol, 2022, 10.1038/s41589-022-01098-0]	PubMed: 36097295
MEK inhibition activates STAT signaling to increase breast cancer immunogenicity via MHC-I expression [ Cancer Drug Resist, 2020, 3(3):603-612]	PubMed: 33062958

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。