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;MERk-5;CS-665;Merck-5;JAK Inhibitor;MERCK 5;MERCK5;JAK INHIBITOR I;Pyridone 6, >=98%
- CBNumber:
- CB3670758
- Molecular Formula:
- C18H16FN3O
- Molecular Weight:
- 309.34
- MDL Number:
- MFCD17019334
- MOL File:
- Mol file
| 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 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H302-H315-H319-H335 |
| Precautionary statements | P261-P305+P351+P338 |
JAK INHIBITOR I price More Price(39)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | 420099 | JAK Inhibitor I - CAS 457081-03-7 - Calbiochem 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). | 457081-03-7 | 500μg | $187 | 2024-03-01 | Buy |
| Sigma-Aldrich | 420099 | JAK Inhibitor I - CAS 457081-03-7 - Calbiochem 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). |
457081-03-7 | 1mg | $245 | 2024-03-01 | Buy |
| Sigma-Aldrich | 420097 | InSolutionJAKInhibitorI-CAS457081-03-7-Calbiochem TheInSolutionJAKInhibitorI,alsoreferencedunderCAS457081-03-7,controls | 457081-03-7 | 500μg | $159 | 2024-03-01 | Buy |
| Cayman Chemical | 15146 | JAK Inhibitor I ≥98% | 457081-03-7 | 1mg | $29 | 2024-03-01 | Buy |
| Cayman Chemical | 15146 | JAK Inhibitor I ≥98% | 457081-03-7 | 500μg | $70 | 2023-06-20 | Buy |
JAK INHIBITOR I Chemical Properties,Uses,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
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Capot Chemical Co.,Ltd. | +86-（0）57185586718 +86-13336195806 | sales@capot.com | China | 29791 | 60 |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32957 | 60 |
| Alchem Pharmtech,Inc. | 8485655694 | sales@alchempharmtech.com | United States | 63687 | 58 |
| career henan chemical co | +86-0371-86658258 +8613203830695 | factory@coreychem.com | China | 29811 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32165 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10473 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
| Hefei TNJ Chemical Industry Co.,Ltd. | +86-0551-65418684 +8618949823763 | sales@tnjchem.com | China | 25356 | 58 |
| TargetMol Chemicals Inc. | support@targetmol.com | United States | 38632 | 58 | |
| ShenZhen Trendseen Biological Technology Co.,Ltd. | 13417589054 | trendseenbio@gmail.com | China | 11681 | 58 |
View Lastest Price from JAK INHIBITOR I manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2024-11-19 | Pyridone 6
457081-03-7
|
US $75.00-165.00 / mg | 98.74% | 10g | TargetMol Chemicals Inc. | ||
 |
2019-12-31 | Pyridone 6
457081-03-7
|
US $1.00 / KG | 1KG | Min98% HPLC | g/kg/ton | Career Henan Chemical Co |
-
- Pyridone 6
457081-03-7
- US $75.00-165.00 / mg
- 98.74%
- TargetMol Chemicals Inc.
-
- Pyridone 6
457081-03-7
- US $1.00 / KG
- Min98% HPLC
- Career Henan Chemical Co