ChemicalBook > CAS DataBase List > 2-Pyridinecarboxamide, N-[4-[[3-[(1-oxo-2-propen-1-yl)amino]benzoyl]amino]phenyl]-6-(1H-pyrazol-3-yl)-

2-Pyridinecarboxamide, N-[4-[[3-[(1-oxo-2-propen-1-yl)amino]benzoyl]amino]phenyl]-6-(1H-pyrazol-3-yl)-

Product Name
2-Pyridinecarboxamide, N-[4-[[3-[(1-oxo-2-propen-1-yl)amino]benzoyl]amino]phenyl]-6-(1H-pyrazol-3-yl)-
CAS No.
2227368-54-7
Chemical Name
2-Pyridinecarboxamide, N-[4-[[3-[(1-oxo-2-propen-1-yl)amino]benzoyl]amino]phenyl]-6-(1H-pyrazol-3-yl)-
Synonyms
JH-X-119-01;JH-X-119-01 ，S9780;JH-X-119-01, 10 mM in DMSO;N-(4-(3-Acrylamidobenzamido)phenyl)-6-(1H-pyrazol-3-yl)picolinamide;2-Pyridinecarboxamide, N-[4-[[3-[(1-oxo-2-propen-1-yl)amino]benzoyl]amino]phenyl]-6-(1H-pyrazol-3-yl)-;inhibit,MYD88,IRAK,IL-1R associated kinase,Waldenstr?m,Inhibitor,IRAK1,Interleukin-1 receptor associated kinase,JHX11901,Diffused Large B-cell Lymphoma,JH X 119 01,macroglobulinemia
CBNumber
CB18214965
Molecular Formula
C25H20N6O3
Formula Weight
452.46
MOL File
2227368-54-7.mol
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2-Pyridinecarboxamide, N-[4-[[3-[(1-oxo-2-propen-1-yl)amino]benzoyl]amino]phenyl]-6-(1H-pyrazol-3-yl)- Property

Boiling point:
654.0±55.0 °C(Predicted)
Density 
1.405±0.06 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO : 250 mg/mL (552.54 mM; Need ultrasonic)
pka
10.98±0.70(Predicted)
form 
Solid
color 
Light yellow to brown
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Hazard and Precautionary Statements (GHS)

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2-Pyridinecarboxamide, N-[4-[[3-[(1-oxo-2-propen-1-yl)amino]benzoyl]amino]phenyl]-6-(1H-pyrazol-3-yl)- Chemical Properties,Usage,Production

Uses

JH-X-119-01 is a potent and selective interleukin-1 receptor-associated kinases 1 (IRAK1) inhibitor. JH-X-119-01 ameliorates LPS-induced sepsis in mice[1]. JH-X-119-01 inhibits IRAK1 biochemically with an apparent IC50 of 9 nM while exhibiting no inhibition of IRAK4 at concentrations up to 10 μM[2].

in vivo

JH-X-119-01 improves survival and decreases immunopathies of LPS-challenged mice. JH-X-119-01 increases survival of mice at the dose of 5 mg/kg body weight. Survival is further improved when the dose is increased to 10 mg/kg[1].

Animal Model:C57BL/6 (20-22 g, male) mice[1]
Dosage:5 mg/kg and 10 mg/kg
Administration:Intraperitoneally injected; 5 days
Result:Protected mice from LPS (20 mg/kg)-induced sepsis. Survival at day 5 was 13.3% in control group where septic mice were treated by vehicle, while the values were 37.5% and 56.3% for 5 mg/kg and 10 mg/kg.

IC 50

IRAK-1: 9 nM (IC50)

References

[1] Bin Pan, et al. Selective inhibition of interleukin-1 receptor-associated kinase 1 ameliorates lipopolysaccharide-induced sepsis in mice. Int Immunopharmacol. 2020 Aug;85:106597. DOI:10.1016/j.intimp.2020.106597
[2] John M Hatcher, et al. Discovery of a Selective, Covalent IRAK1 Inhibitor with Antiproliferative Activity in MYD88 Mutated B-Cell Lymphoma. ACS Med Chem Lett. 2020 Oct 9;11(11):2238-2243. DOI:10.1021/acsmedchemlett.0c00378

2-Pyridinecarboxamide, N-[4-[[3-[(1-oxo-2-propen-1-yl)amino]benzoyl]amino]phenyl]-6-(1H-pyrazol-3-yl)- Preparation Products And Raw materials

Raw materials

Preparation Products

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2-Pyridinecarboxamide, N-[4-[[3-[(1-oxo-2-propen-1-yl)amino]benzoyl]amino]phenyl]-6-(1H-pyrazol-3-yl)- Suppliers

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ShangHai Caerulum Pharma Discovery Co., Ltd.
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2227368-54-7, 2-Pyridinecarboxamide, N-[4-[[3-[(1-oxo-2-propen-1-yl)amino]benzoyl]amino]phenyl]-6-(1H-pyrazol-3-yl)-Related Search:


  • 2-Pyridinecarboxamide, N-[4-[[3-[(1-oxo-2-propen-1-yl)amino]benzoyl]amino]phenyl]-6-(1H-pyrazol-3-yl)-
  • JH-X-119-01
  • N-(4-(3-Acrylamidobenzamido)phenyl)-6-(1H-pyrazol-3-yl)picolinamide
  • inhibit,MYD88,IRAK,IL-1R associated kinase,Waldenstr?m,Inhibitor,IRAK1,Interleukin-1 receptor associated kinase,JHX11901,Diffused Large B-cell Lymphoma,JH X 119 01,macroglobulinemia
  • JH-X-119-01, 10 mM in DMSO
  • JH-X-119-01 ，S9780
  • 2227368-54-7