ChemicalBook > CAS DataBase List > Delgocitinib

Delgocitinib

Product Name
Delgocitinib
CAS No.
1263774-59-9
Chemical Name
Delgocitinib
Synonyms
JTE052;JTE-052;LEO124249;LEO 124249;Delgocitinib;Delgocitinib(JTE-052);Corectim(Delgocitinib);Delgocitinib (LEO124249;JTE052,Inhibitor,Janus kinase,inhibit,JAK,Delgocitinib,JTE 052;1,6-Diazaspiro[3.4]octane-1-propanenitrile, 3-methyl-β-oxo-6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-, (3S,4R)-
CBNumber
CB34667815
Molecular Formula
C16H18N6O
Formula Weight
310.35
MOL File
1263774-59-9.mol
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Delgocitinib Property

Density 
1.41±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO:58.0(Max Conc. mg/mL);186.89(Max Conc. mM)
pka
-0.65±0.40(Predicted)
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

ChemScene
Product number
CS-0031558
Product name
Delgocitinib
Purity
99.76%
Packaging
10mg
Price
$1100
Updated
2021/12/16
ChemScene
Product number
CS-0031558
Product name
Delgocitinib
Purity
99.76%
Packaging
25mg
Price
$2200
Updated
2021/12/16
ChemScene
Product number
CS-0031558
Product name
Delgocitinib
Purity
99.76%
Packaging
50mg
Price
$3500
Updated
2021/12/16
ChemScene
Product number
CS-0031558
Product name
Delgocitinib
Purity
99.76%
Packaging
100mg
Price
$5500
Updated
2021/12/16
ChemScene
Product number
CS-0031558
Product name
Delgocitinib
Purity
99.76%
Packaging
1mg
Price
$210
Updated
2021/12/16
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Delgocitinib Chemical Properties,Usage,Production

Characteristics

Class: non-receptor tyrosine kinase
Treatment: atopic dermatitis (topical ointment)
Protein binding = 22–29%

Definition

The lead compound to delgocitinib was tofacitinib, a potent pan-JAK inhibitor. To maintain the overall pan-JAK inhibition profile of tofacitinib, the pyrrolopyrimidine hinge binder, and the cyanoacetyl group were kept fixed. At the same time, the central aminopiperidine linker was replaced by a variety of spirocyclic scaffolds to maintain comparable binding patterns. This effort identified the three-dimensional diazaspiro[3.4]octane scaffold as the optimal linker, and further SAR studies led to delgocitinib, which demonstrates better selectivity against JAK3 compared to tofacitinib and its selectivity for the JAK family over LCK is also improved. Delgocitinib exhibits no significant inhibition of non-JAK kinases under 1 μM except ROCK2.

Definition

Delgocitinib is metabolically stable in both liver microsomes and hepatocytes across species (human, rat, dog, and monkey), and it is also not metabolized in human skin microsomes. It has favorable oral bioavailability in rats (78%) and dogs (124%). Following repeat topical application to the affected area twice daily with a maximum dose of 5 g per application, plasma levels of delgocitinib were detected in 12%, 16%, 14%, and 12% of the patients at week 4, 12, 28, and 52, respectively.

Definition

ChEBI: Delgocitinib is a pyrrolopyrimidine that is 7H-pyrrolo[2,3-d]pyrimidine substituted by a (3S,4R)-1-(cyanoacetyl)-3-methyl-1,6-diazaspiro[3.4]octan-6-yl group at position 4. It is a pan-Janus kinase (JAK) inhibitor and is approved for treatment of atopic dermatitis (AD) in Japan. It has a role as an EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor, an anti-inflammatory drug, an antipsoriatic and an antiseborrheic. It is a pyrrolopyrimidine, a tertiary amino compound, a nitrile, an azaspiro compound, a tertiary carboxamide and a N-acylazetidine.

Clinical Use

Delgocitinib is a pan-JAK inhibitor that inhibits all Janus Kinase (JAK) family members. Topical delgocitinib 0.5% ointment received its first approval in Japan in 2020 for treating adults with atopic dermatitis. The FDA has granted delgocitinib cream fast-track designation for chronic hand eczema.

Delgocitinib Preparation Products And Raw materials

Raw materials

Preparation Products

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1263774-59-9, DelgocitinibRelated Search:


  • Delgocitinib
  • JTE052
  • JTE-052
  • LEO 124249
  • LEO124249
  • 3-[(3S,4R)-3-methyl-6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)- 1,6-diazaspiro[3.4]octan-1-yl]-3-oxopropanenitrile
  • 1,6-Diazaspiro[3.4]octane-1-propanenitrile, 3-methyl-β-oxo-6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-, (3S,4R)-
  • Corectim(Delgocitinib)
  • Delgocitinib(JTE-052)
  • Delgocitinib (LEO124249
  • 3-[(3S,4R)-3-methyl-7-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1,7-diazaspiro[3.4]octan-1-yl]-3-oxopropanenitrile
  • JTE052,Inhibitor,Janus kinase,inhibit,JAK,Delgocitinib,JTE 052
  • 1263774-59-9
  • 263774-59-9