ChemicalBook > CAS DataBase List > JAK INHIBITOR I

JAK INHIBITOR I

Product Name: JAK INHIBITOR I
CAS No.: 457081-03-7
Chemical Name: JAK INHIBITOR I
Synonyms: Pyridone 6;7H-Benz[h]imidazo[4,5-f]isoquinolin-7-one, 2-(1,1-dimethylethyl)-9-fluoro-1,6-dihydro-;CMP 6;CS-665;MERk-5;Merck-5;JAK Inhibitor;MERCK 5;MERCK5;JAK INHIBITOR I;Pyridone 6, >=98%
CBNumber: CB3670758
Molecular Formula: C18H16FN3O
Formula Weight: 309.34
MOL File: Mol file

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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.

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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

Sigma-Aldrich

Product number: 420099
Product name: JAK Inhibitor I - CAS 457081-03-7 - Calbiochem
Purity: JAK Inhibitor I, CAS 457081-03-7, is a potent, reversible, cell-permeable, and ATP-competitive inhibitor of JAK 1 (IC?? = 15 nM), JAK2 (IC?? = 1 nM), JAK3 (Ki = 5 nM) and Tyk2 (IC?? = 1 nM).
Packaging: 500μg
Price: $192
Updated: 2025/07/31

Sigma-Aldrich

Product number: 420099
Product name: JAK Inhibitor I - CAS 457081-03-7 - Calbiochem<br />JAK Inhibitor I, CAS 457081-03-7, is a potent, reversible, cell-permeable, and ATP-competitive inhibitor of JAK 1 (IC = 15 nM), JAK2 (IC = 1 nM), JAK3 (Ki = 5 nM) and Tyk2 (IC = 1 nM).
Packaging: 1mg
Price: $252
Updated: 2025/07/31

Sigma-Aldrich

Product number: 420097
Product name: InSolutionJAKInhibitorI-CAS457081-03-7-Calbiochem
Purity: TheInSolutionJAKInhibitorI,alsoreferencedunderCAS457081-03-7,controls
Packaging: 500μg
Price: $171
Updated: 2025/07/31

Cayman Chemical

Product number: 15146
Product name: JAK Inhibitor I
Purity: ≥98%
Packaging: 1mg
Price: $29
Updated: 2024/03/01

Cayman Chemical

Product number: 15146
Product name: JAK Inhibitor I
Purity: ≥98%
Packaging: 500μg
Price: $70
Updated: 2023/06/20

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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

[1] JAMES E. THOMPSON. Photochemical preparation of a pyridone containing tetracycle: A jak protein kinase inhibitor[J]. Bioorganic & Medicinal Chemistry Letters, 2002, 12 8: Pages 1219-1223. DOI:10.1016/s0960-894x(02)00106-3
[2] SHIN-ICHI MAE . Combination of small molecules enhances differentiation of mouse embryonic stem cells into intermediate mesoderm through BMP7-positive cells[J]. Biochemical and biophysical research communications, 2010, 393 4: Pages 877-882. DOI:10.1016/j.bbrc.2010.02.111
[3] RYUSUKE NAKAGAWA. Pyridone 6, a pan-JAK inhibitor, ameliorates allergic skin inflammation of NC/Nga mice via suppression of Th2 and enhancement of Th17.[J]. ACS Applied Electronic Materials, 2011: 4611-4620. DOI:10.4049/jimmunol.1100649
[4] ATSUSHI MORIWAKI . IL-13 suppresses double-stranded RNA-induced IFN-λ production in lung cells[J]. Biochemical and biophysical research communications, 2011, 404 4: Pages 922-927. DOI:10.1016/j.bbrc.2010.12.082

JAK INHIBITOR I Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from JAK INHIBITOR I manufacturers

Career Henan Chemical Co

Product: Pyridone 6 457081-03-7
Price: US $1.00/KG
Min. Order: 1KG
Purity: Min98% HPLC
Supply Ability: g/kg/ton
Release date: 2019-12-30

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JAK Inhibitor I - CAS 457081-03-7 - Calbiochem

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JAK Inhibitor I - CAS 457081-03-7 - Calbiochem[420099]

457081-03-7

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Inhibitors