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Chemical Structure| 1263774-59-9 Chemical Structure| 1263774-59-9

Structure of Delgocitinib
CAS No.: 1263774-59-9

Chemical Structure| 1263774-59-9

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Delgocitinib is a novel and specific JAK inhibitor with IC50s of 2.8, 2.6, 13 and 58 nM for JAK1, JAK2, JAK3 and Tyk2, respectively.

Synonyms: JTE-052

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Product Details of Delgocitinib

CAS No. :1263774-59-9
Formula : C16H18N6O
M.W : 310.35
SMILES Code : N#CCC(N1C[C@H](C)[C@]12CN(C3=C4C(NC=C4)=NC=N3)CC2)=O
Synonyms :
JTE-052
MDL No. :MFCD31630732

Safety of Delgocitinib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Delgocitinib

epigenetics
RTK
JAK-STAT

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
human T cells 8.9±3.6 nM (IC50) 3 days inhibited IL-2-induced proliferation of T cells Inflamm Res. 2015 Jan;64(1):41-51
normal human lung fibroblasts (NHLFs) >10,000 nM (IC50) 3 days no clear inhibitory effect Inflamm Res. 2015 Jan;64(1):41-51
human mast cells 133±18 nM (IC50) 5 days inhibited IL-4 and IgE-induced TNF-α production Inflamm Res. 2015 Jan;64(1):41-51
human monocytes 277±146 nM (IC50) 16 h inhibited GM-CSF-enhanced LPS-induced TNF-α production Inflamm Res. 2015 Jan;64(1):41-51
human B cells 49±6 nM (IC50) 3 days inhibited IL-21 and anti-CD40 antibody-induced B cell proliferation Inflamm Res. 2015 Jan;64(1):41-51

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Sclerodermatous GVHD mouse model Topical administration (eyelids or back skin) 0.5% Delgocitinib ointment or eye drops Twice daily for 21 consecutive days To evaluate the efficacy of topical Delgocitinib in alleviating skin and ocular symptoms in GVHD mice. Results showed that Delgocitinib significantly increased the meibomian gland area, attenuated corneal epithelial damage, and reduced inflammation and pathological fibrosis. Sci Rep. 2025 Jan 2;15(1):532
DBA/1J mice IL-2-induced IFN-γ production model Oral 0.24 mg/kg (ED50) Single dose Inhibited IL-2-induced IFN-γ production Inflamm Res. 2015 Jan;64(1):41-51

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT03683719 Chronic Hand Eczema Phase 2 Not yet recruiting March 2020 -
NCT03725722 Atopic Dermatitis Phase 2 Not yet recruiting December 2019 -
NCT05486117 Chronic Hand Eczema PHASE1 COMPLETED 2022-11-22 LEO Investigational Site, Hamb... More >>urg, 20095, Germany Less <<
NCT04949841 Chronic Hand Eczema PHASE3 COMPLETED 2023-09-18 LEO Investigational Site, Brus... More >>sel, 1000, Belgium|LEO Investigational Site, Gent, 9000, Belgium|LEO Investigational Site, Kortrijk, 8500, Belgium|LEO Investigational Site, Leuven, 3000, Belgium|LEO Investigational Site, Loverval, 6280, Belgium|LEO Investigational Site, Maldegem, 9990, Belgium|LEO Investigational Site, Calgary, Alberta, T2J 7E1, Canada|LEO Investigational Site, Calgary, Alberta, T3E 0B2, Canada|LEO Investigational Site, Edmonton, Alberta, T5J 3S9, Canada|LEO Investigational Site, Edmonton, Alberta, T6G 1C3, Canada|LEO Investigational Site, Surrey, British Columbia, V3R 6A7, Canada|LEO Investigational Site, Vancouver, British Columbia, V6 4E1, Canada|LEO Investigational Site, Fredericton, New Bruswick, E3B 1G9, Canada|LEO Investigational Site, Ajax, Ontario, L1S 7K8, Canada|LEO Investigational Site, Cobourg, Ontario, K9A 4J9, Canada|LEO Investigational Site, Etobicoke, Ontario, M8X 1Y9, Canada|LEO Investigational Site, Hamilton, Ontario, L8S 1G5, Canada|LEO Investigational Site, Kingston, Ontario, K7L 2V7, Canada|LEO Investigational Site, London, Ontario, N6A 3H7, Canada|LEO Investigational Site, Markham, Ontario, L3P 1X3, Canada|LEO Investigational Site, Toronto, Ontario, M2M 4J5, Canada|LEO Investigational Site, Toronto, Ontario, M3H 5Y8, Canada|LEO Investigational Site, Waterloo, Ontario, N2J 1C4, Canada|LEO Investigational Site, Windsor, Ontario, N8W 1E6, Canada|LEO Investigational Site, Montreal, Quebec, H2X 2V1, Canada|LEO Investigational Site, Aarhus N, 8200, Denmark|LEO investigational Site, Copenhagen, 2400, Denmark|LEO Pharma Investigational Site, Hellerup, 2900, Denmark|LEO Investigational Site, Bordeaux, 33000, France|LEO Investigational Site, Dijon, 21000, France|LEO Investigational Site, Le Mans, 72037, France|LEO Investigational Site, Lille, 5900, France|LEO Investigational Site, Martigues, 13500, France|LEO Pharma Investigational Site, Nantes, 44093, France|LEO Investigational Site, Nice, 06000, France|LEO Investigational Site, Nice, 06202, France|LEO Investigational Site, Paris, 75014, France|LEO Investigational Site, Reims, 51100, France|LEO Investigational Site, Toulouse, 31000, France|LEO Investigational Site, Aachen, 52074, Germany|LEO Investigational Site, Bad Bentheim, 48455, Germany|LEO Investigational Site, Berlin, 10115, Germany|LEO Investigational Site, Dresden, 01307, Germany|LEO Investigational Site, Frankfurt am Main, 60590, Germany|LEO Investigational Site, Friedrichshafen, 88045, Germany|LEO Investigational Site, Gera, 07548, Germany|LEO Investigational Site, G?ttingen, 37073, Germany|LEO Investigational Site, Hamburg, 22391, Germany|LEO Investigational Site, Hannover, 30159, Germany|LEO Investigational Site, Hassfurt, 97437, Germany|LEO Investigational Site, Jena, 07743, Germany|LEO Investigational Site, Luebeck, 23538, Germany|LEO Investigational Site, Mahlow, 15831, Germany|LEO Investigational Site, Mainz-Bretzenheim, 55128, Germany|LEO Pharma Investigational Site, Memmingen, 87700, Germany|LEO Investigational Site, München, 80802, Germany|Leo Investigational Site, Münster, 48149, Germany|LEO Investigational Site, Osnabrück, 49074, Germany|LEO Investigational Site, Stuttgart, 70178, Germany|LEO Investigational Site, Brescia, 25123, Italy|LEO Investigational Site, L'Aquila, 67100, Italy|LEO Investigational Site, Rome, 00168, Italy|LEO Investigational Site, Vicenza, 36100, Italy|LEO Investigational Site, Amsterdam, 1105 AZ, Netherlands|LEO Investigational Site, Bergen Op Zoom, 4614 VT, Netherlands|LEO Investigational Site, Groningen, 9713 GZ, Netherlands|LEO Investigational Site, Hoofddorp, 2134 TM, Netherlands|LEO Investigational Site, Utrecht, 3584 CX, Netherlands|LEO Investigitional Site, Bia?ystok, 15-375, Poland|LEO Investigational Site, Bia?ystok, 15-794, Poland|LEO Investigational Site, Gdansk, 80-546, Poland|LEO Investigational Site, Kraków, 30-033, Poland|LEO Investigational Site, Kraków, 31-011, Poland|LEO Investigational Site, Lublin, 20-081, Poland|LEO Investigational Site, Lublin, 20-406, Poland|LEO Investigational Site, Osielsko, 86-031, Poland|LEO Pharma Investigational Site, Rzeszów, 35-055, Poland|LEO Investigational Site, Warsaw, 02-953, Poland|LEO Investigational Site, Warsaw, 02-962, Poland|LEO Investigational Site, Warszawa, 02-507, Poland|LEO Investigational Site, Warszawa, 02-625, Poland|LEO Investigational Site, Wroc?aw, 50-566, Poland|LEO Investigational Site, Wroc?aw, 51-318, Poland|LEO Investigational Site, ?ód?, 90-436, Poland|LEO Investigational Site, Alicante, 03010, Spain|LEO Investigational Site, Badalona, 08915, Spain|LEO Investigitional Site, Barcelona, 08041, Spain|LEO Investigational Site, Bilbao, 48013, Spain|LEO Investigational Site, Madrid, 28031, Spain|LEO Investigational Site, Mieres, 33611, Spain|LEO Investigational Site, Sevilla, 41009, Spain|LEO Investigational Sites, Redhill, Surrey, RH1 5RH, United Kingdom|LEO Investigational Site, London, SE1 7EH, United Kingdom|LEO Investigational Site, Middlesborough, TS4 3BW, United Kingdom|LEO Investigational Site, Salford, M6 8HD, United Kingdom Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.22mL

0.64mL

0.32mL

16.11mL

3.22mL

1.61mL

32.22mL

6.44mL

3.22mL

 

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