| Identification | Back Directory | [Name]
(2-(6-(2-ETHYL-5-FLUORO-4-HYDROXYPHENYL)-1H-INDAZOL-3-YL)-3,4,6,7-TETRAHYDRO-5H-IMIDAZO[4,5-C]PYRIDIN-5-YL)(5-(PIPERIDIN-1-YL)PYRAZIN-2-YL)METHANONE | [CAS]
1421502-62-6 | [Synonyms]
PF 6263276
PF06263276,PF 06263276
PF-06263276 (PF 6263276)
PF-06263276 >=98% (HPLC)
(2-(6-(2-ETHYL-5-FLUORO-4-HYDROXYPHENYL)-1H-INDAZOL-3-YL)-3,4,6,7-TETRAHYDRO-5H-IMIDAZO[4,5-C]PYRIDIN-5-YL)(5-(PIPERIDIN-1-YL)PYRAZIN-2-YL)METHANONE
Methanone, [2-[6-(2-ethyl-5-fluoro-4-hydroxyphenyl)-1H-indazol-3-yl]-3,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl][5-(1-piperidinyl)-2-pyrazinyl]- | [Molecular Formula]
C31H31FN8O2 | [MDL Number]
MFCD30718580 | [MOL File]
1421502-62-6.mol | [Molecular Weight]
566.63 |
| Chemical Properties | Back Directory | [Boiling point ]
921.1±65.0 °C(Predicted) | [density ]
1.394±0.06 g/cm3(Predicted) | [storage temp. ]
room temp | [solubility ]
Soluble in DMSO | [form ]
powder | [pka]
8.54±0.25(Predicted) | [color ]
white to beige | [InChIKey]
XDJGNPSZQSWJCV-UHFFFAOYSA-N | [SMILES]
FC1=C(O)C=C(CC)C(C2=CC(NN=C3C4=NC5=C(CCN(C(C6=CN=C(N7CCCCC7)C=N6)=O)C5)N4)=C3C=C2)=C1 |
| Hazard Information | Back Directory | [Uses]
PF-06263276 (PF 6263276) is a potent and selective pan-JAK inhibitor, with IC50s of 2.2 nM, 23.1 nM, 59.9 nM and 29.7 nM for JAK1, JAK2, JAK3 and TYK2, respectively. PF-06263276 inhibits pSTAT3 and TYK2 pathway. PF-06263276 has a protective effect against ear skin inflammation[1]. | [Biological Activity]
PF-06263276 is an inhibitor of the Janus kinase (JAK) enzymes 123 and tyrosine kinase 2 (TYK2). PF-06263276 has been investigated for the treatment of psoriasis. | [in vivo]
PF-06263276 (0.3-100 μg/animal; i.t.) can dose-dependently inhibit the increase of lung pSTAT3 in the pharmacodynamic model of IL-6-induced lung pSTAT3 response in mice, with an ED50 of approximately 3 μg/animal[1].
PF-06263276 (4% solution; topical administration; multiple times; 11 days) can significantly reduce ear swelling by 48% in the IL-23-induced mouse ear skin inflammation model and inhibit the JAK2/TYK2 pathway[1].
| [IC 50]
JAK1: 2.2 nM (IC50); JAK2: 23.1 nM (IC50); JAK3: 59.9 nM (IC50); Tyk2: 29.7 nM (IC50) | [storage]
Store at -20°C | [References]
[1] Jones P, et al. Design and Synthesis of a Pan-Janus Kinase Inhibitor Clinical Candidate (PF-06263276) Suitable for Inhaled and Topical Delivery for the Treatment of Inflammatory Diseases of the Lungs and Skin. J Med Chem. 2017 Jan 26;60(2):767-786. DOI:10.1021/acs.jmedchem.6b01634 |
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| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
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