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JAK INHIBITOR I

JAK INHIBITOR I Structure
JAK INHIBITOR I
  • CAS No.457081-03-7
  • Chemical Name:JAK INHIBITOR I
  • CBNumber:CB3670758
  • Molecular Formula:C18H16FN3O
  • Formula Weight:309.34
  • MOL File:Mol file
JAK INHIBITOR I Property
  • Melting point >178°C (dec.)
  • Boiling point 646.5±55.0 °C(Predicted)
  • Density 1.328
  • storage temp. -20C
  • solubility Soluble in DMSO (30 mg/ml)
  • form Off-white solid
  • pka 11.35±0.20(Predicted)
  • color Off-white
  • Stability Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
  • FDA UNII LDX3F0CCST
  • NCI Drug Dictionary JAK inhibitor
  • UNSPSC Code 12352200
  • NACRES NA.77
Hazard and Precautionary Statements (GHS)
  • Symbol(GHS)
  • Signal wordWarning
  • Hazard statements H302-H315-H319-H335
  • Precautionary statements P261-P305+P351+P338
JAK INHIBITOR I Price More Price(1)
  • Brand: Sigma-Aldrich(India)
  • Product number: 420097
  • Product name : InSolution JAK Inhibitor I - CAS 457081-03-7 - Calbiochem
  • Purity: The InSolution JAK Inhibitor I, also referenced under CAS 457081-03-7, controls the biological activity of JAK. This small molecule/inhibitor is prima
  • Packaging: 500μG
  • Price: ₹16670
  • Updated: 2022/06/14
  • Buy: Buy

JAK INHIBITOR I Chemical Properties,Usage,Production

  • Description Pyridone 6 (457081-03-7) is a potent, ATP-competitive pan-JAK inhibitor. Inhibits 1, 2 and 3 (IC50=1, 5 and 15 nM respectively) as well as JAK family member Tyk2 (IC50=1 nM).1 Also tested against 21 other kinases with inhibition ranging from 130 nm to >10 mM. Inhibits IL2 and IL4-dependent proliferation of CTLL cells.1 Induces intermediate mesoderm differentiation from embryonic stem cells in a cocktail with LY-294002, CCG-1423 and retinoic acid.2 Potently inhibits STAT1, STAT5 and STAT6 phosphorylation and ameliorates allergic skin inflammation in a mouse model.3 Suppresses asthmatic responses in a mouse allergic asthma model.4
  • Uses Pyridone 6 is a ATP-competitive JAK inhibitor in clinical development for the treatment of myeloproliferative neoplasms and B cell acute lymphoblastic leukemia.
  • Definition ChEBI: 2-tert-butyl-9-fluoro-1,6-dihydrobenzo[h]imidazo[4,5-f]isoquinolin-7-one is an organic heterotetracyclic compound that is 1,6-dihydrobenzo[h]imidazo[4,5-f]isoquinolin-7-one bearing additional tert-butyl and fluoro substituents at positions 2 and 9 respectively. It has a role as an EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor. It is an organic heterotetracyclic compound and an organofluorine compound.
  • in vivo

    Pyridone 6 (P6) delays the onset and reduced the magnitude of skin disease in an AD-like skin-disease model of NC/Nga mice. P6-nano strongly ameliorates atopic dermatitis (AD) in NC/Nga mice, exerting an effect comparable to that of betamethasone ointment, a commonly used drug, which also tested as a positive control. In contrast, empty polylactic acid with glycolic acid (PLGA)? nanoparticles (C-nano) seemed to have no effect[2].

  • IC 50 JAK2: 1 nM (IC50); Tyk2: 1 nM (IC50); JAK3: 5 nM (IC50); Murine JAK1: 15 nM (IC50); CDK2: 3.3 μM (IC50); cAMP-dependent kinase: 7.1 μM (IC50); Csk: 2.1 μM (IC50); Hck: 7.7 μM (IC50); Fyn T: 0.5 μM (IC50); p38: 11 μM (IC50); MAPK: 1.78 μM (IC50); Mek: 0.16 μM (IC50); IκB Kinase 2: 0.3 μM (IC50); KDR: 1.4 μM (IC50); Flt-1: 1.52 μM (IC50); Flt-4: 0.69 μM (IC50); FGFR: 1.48 μM (IC50); FGFR2: 0.94 μM (IC50); Tek: 24 μM (IC50); PDGFR: 1.49 μM (IC50); PKC(α): 1.2 μM (IC50)
  • storage Store at -20°C
  • References Thompson et al. (2002) Photochemical preparation of a pyridine containing tetracycle: a JAK protein kinase inhibitor Med. Chem. Lett. 12 1219 Mae et al. (2010) Combination of small molecules enhances differentiation of mouse embryonic stem cells into intermediate mesoderm through BMP7-positive cells; Biochem. Biophys. Res. Commun. 393 877 Nakagawa et al. (2011) Pyridone 6, a pan-JAK inhibitor, ameliorates allergic skin inflammation of NC/Nga mice via suppression of Th2 and enhancement of Th17; Immunol. 187 4611 Moriwaki et al. (2011) IL-13 suppresses double-stranded RNA-induced IFN-l production in lung cells; Biochem. Biophys. Res. Commun. 404 922
JAK INHIBITOR I Preparation Products And Raw materials
Raw materials
Preparation Products
JAK INHIBITOR I Suppliers
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JAK INHIBITOR I Spectrum
457081-03-7, JAK INHIBITOR IRelated Search:
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  • 457091-03-7
  • 吡啶酮6,10 MM DMSO 溶液
  • 2-(叔丁基)-9-氟-1,6-二氢-7H-苯并[H]咪唑并[4,5-F]异喹啉-7-酮
  • 5级
  • 泛JAK抑制剂(PYRIDONE 6)
  • 2-(1,1-二甲基乙基)-9-氟-1,6-二氢-7H-苯并[H]咪唑并[4,5-F]异喹啉-7-酮
  • 吡啶酮6
  • 457081-03-7
  • Pyridone 6, 10 mM in DMSO
  • 2-(tert-butyl)-9-fluoro-1H-benzo[h]imidazo[4,5-f]isoquinolin-7(6H)-one
  • 4-tert-butyl-15-fluoro-3,5,10-triazatetracyclo[11.4.0.02,?.0?,12]heptadeca-1(13),2(6),4,7(12),8,14,16-heptaen-11-one
  • Pyridone 6
  • 7H-Benz[h]imidazo[4,5-f]isoquinolin-7-one, 2-(1,1-dimethylethyl)-9-fluoro-1,6-dihydro-
  • 9-Fluoro-2-(2-methyl-2-propanyl)-1,6-dihydro-7H-benzo[h]imid...
  • 2-(tert-butyl)-9-fluoro-1,6-dihydro-7H-benzo[h]imidazo[4,5-f]isoquinolin-7-one
  • InSolution JAK Inhibitor I
  • JAK Inhibitor I(Merck 5, Pyridone 6)
  • Janus-Associated Kinase Inhibitor I
  • InSolution(TM) JAK Inhibitor I
  • CS-665
  • MERCK 5;MERCK5
  • JAK Inhibitor I(Merck 5)
  • JAK Inhibitor I - CAS 457081-03-7 - Calbiochem
  • Pyridone 6（JAK INHIBITOR I）
  • Pyridone 6(CMP 6)
  • CMP 6 2-(1,1-Dimethylethyl)-9-fluoro-1,6-dihydro-7H-benz[h]imidazo[4,5-f]isoquinolin-7-one
  • JAK Inhibitor
  • Merck-5 ,JAK INHIBITOR I
  • JAK INHIBITOR I
  • 2-(1,1-DIMETHYLETHYL)-9-FLUORO-3,6-DIHYDRO-7H-BENZ[H]-IMIDAZ[4,5-F] ISOQUINOLIN-7-ONE
  • Pyridone 6, >=98%
  • 2-(1,1-Dimethylethyl)-9-fluoro-1,6-dihydro-7H-benz[h]imidazo[4,5-f]isoquinolin-7-one
  • CMP 6
  • 2-(tert-butyl)-9-fluoro-3H-benzo[h]iMidazo[4,5-f]isoquinolin-7(6H)-one
  • MERk-5
  • Merck-5

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