Itacitinib

• Description:

  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[1][2].

• Product Name Alternative:

  INCB039110

• UNSPSC:

  12352005

• Hazard Statement:

  H301, H311, H331

• Target:

  JAK

• Type:

  Reference compound

• Related Pathways:

  Epigenetics; JAK/STAT Signaling; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

• Applications:

  Cancer-Kinase/protease

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/Itacitinib.html

• Purity:

  99.97

• Solubility:

  DMSO : ≥ 30 mg/mL

• 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

• Molecular Formula:

  C26H23F4N9O

• Molecular Weight:

  553.51

• Precautions:

  H301, H311, H331

• References & Citations:

  [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.|[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.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  Phase 3

• Isoform:

  JAK1

• CAS Number:

  1334298-90-6