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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
$187
Updated
2024/03/01
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
$245
Updated
2024/03/01
Sigma-Aldrich
Product number
420097
Product name
InSolutionJAKInhibitorI-CAS457081-03-7-Calbiochem
Purity
TheInSolutionJAKInhibitorI,alsoreferencedunderCAS457081-03-7,controls
Packaging
500μg
Price
$159
Updated
2024/03/01
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.

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

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JAK INHIBITOR I Suppliers

Canada 1 China 87 India 1 United Kingdom 2 United States 23 Global 114
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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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