457081-03-7
Synonym(s):
2-(1,1-Dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, P6, Pyridone 6, DBI, JAK1 Inhibitor I, JAK2 Inhibitor I, JAK3 Inhibitor X;2-(1,1-Dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, Pyridone 6, P6, DBI, JAK1 Inhibitor I, JAK2 Inhibitor I, JAK3 Inhibitor X;InSolution JAK Inhibitor I - CAS 457081-03-7 - Calbiochem;JAK Inhibitor I - CAS 457081-03-7 - Calbiochem
| Pack Size | Price | Stock | Quantity |
| 500μG | RMB1623.33 | In Stock |
|
| 1MG | RMB2046.81 | In Stock |
|
| others | Enquire |
PRODUCT Properties
| 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. |
| InChI | 1S/C18H16FN3O/c1-18(2,3)17-21-14-10-5-4-9(19)8-12(10)13-11(15(14)22-17)6-7-20-16(13)23/h4-8H,1-3H3,(H,20,23)(H,21,22) |
| InChIKey | VNDWQCSOSCCWIP-UHFFFAOYSA-N |
| SMILES | Fc1cc2c(c3[nH]c(nc3c4c2c(ncc4)O)C(C)(C)C)cc1 |
Description and Uses
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
Pyridone 6 is a ATP-competitive JAK inhibitor in clinical development for the treatment of myeloproliferative neoplasms and B cell acute lymphoblastic leukemia.
Safety
| Symbol(GHS) |  GHS07 |
| Signal word | Warning |
| Hazard statements | H302-H315-H319-H335 |
| Precautionary statements | P261-P305+P351+P338 |
| WGK Germany | WGK 2 |
| Storage Class | 10 - Combustible liquids |
