Itacitinib (INCB39110)

Catalog No.S7812 Batch:S781201

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Technical Data

Formula

C26H23F4N9O
Molecular Weight 553.51 CAS No. 1334298-90-6
Solubility (25°C)* In vitro DMSO 100 mg/mL (180.66 mM)
Ethanol 100 mg/mL (180.66 mM)
Water Insoluble
* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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

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].
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].

Protocol (from reference)

Cell Assay:

[4]
  • Cell lines

    Monocyte-Derived Macrophages

  • Concentrations

    1 μM

  • Incubation Time

    1 h

  • Method

    Cells were treated with various concentrations of Itacitinib.
Animal Study:

[4]
  • Animal Models

    Male Sprague-Dawley rats

  • Dosages

    30 mg/kg

  • Administration

    s.c.

Selleck's Itacitinib (INCB39110) has been cited by 7 publications

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
Supplemental Material Monoclonal antibodies and flow cytometry [ , , ] PubMed: none

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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