PF-956980

Names

[ Name ]:
PF-956980

[Synonym ]:
((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)(pyrrolidin-1-yl)methanone
Methanone, [(3R,4R)-4-methyl-3-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-1-piperidinyl]-1-pyrrolidinyl-
{(3R,4R)-4-Methyl-3-[methyl(1H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]-1-piperidinyl}(1-pyrrolidinyl)methanone

Biological Activity

[Description]:

PF-00956980 is a reversible pan-JAK inhibitor with IC50 values of 2.2, 23.1 and 59.9 μM for JAK1, JAK2 and JAK3, respectively. PF-00956980 can be used in the research of lung and skin inflammatory diseases[1].

[Related Catalog]:

Signaling Pathways >> JAK/STAT Signaling >> JAK

Signaling Pathways >> Epigenetics >> JAK

Signaling Pathways >> Stem Cell/Wnt >> JAK

Research Areas >> Inflammation/Immunology

[Target]

JAK1:2.2 μM (IC50)

JAK2:23.1 μM (IC50)

JAK3:59.9 μM (IC50)

[In Vivo]

The pharmacokinetic parameters of PF-00956980(compound 2) in rat or dog Spesies Dose (mg/kg) Cl (mL/min/Kg) Clunbound (mL/min/Kg) Vss (L/Kg) Terminal T1/2 (h) Oral Bioavailability Rat i.v. 0.5 48 >48,000 0.8 2.1 - Rat p.o. 1 - - - - <5% Dog i.v. 0.1 18 >18,000 1.0 2.0 -

[References]

[1]. Peter Jones, 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.

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Molecular Formula ]:
C₁₈H₂₆N₆O

[ Molecular Weight ]:
342.439

[ Exact Mass ]:
342.216797

[ LogP ]:
2.35

[ Index of Refraction ]:
1.658

[ Storage condition ]:
Store at -20°C

Related Compounds

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