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1262832-74-5

1262832-74-5 Structure

1262832-74-5 Structure
IdentificationBack Directory
[Name]

PF 956980
[CAS]

1262832-74-5
[Synonyms]

PF 956980
[(3R,4R)-4-methyl-3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]-pyrrolidin-1-ylmethanone
Methanone, [(3R,4R)-4-methyl-3-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-1-piperidinyl]-1-pyrrolidinyl-
[Molecular Formula]

C18H26N6O
[MOL File]

1262832-74-5.mol
[Molecular Weight]

342.44
Chemical PropertiesBack Directory
[solubility ]

DMSO (Slightly), Methanol (Slightly)
[form ]

Solid
[color ]

White to Pale Yellow
[Stability:]

Hygroscopic
Hazard InformationBack Directory
[Uses]

PF-956980 is a FGF1 receptor antagonist; PDGF receptor modulator; Flt3 tyrosine kinase modulator; and VEGF antagonist. PF-956980 is used as immunosuppressive agent.
[Definition]

ChEBI: PF-956980 is a pyrrolopyrimidine that is 7H-pyrrolo[2,3-d]pyrimidine substituted at position 4 by a methyl[(3R,4R)-4-methyl-1-(pyrrolidin-1-ylcarbonyl)piperidin-3-yl]nitrilo group. It is a potent JAK3-selective chemical probe. It has a role as an EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor. It is a pyrrolopyrimidine, a tertiary amino compound, a N-acylpiperidine and a N-acylpyrrolidine.
[in vivo]

The pharmacokinetic parameters of PF-00956980(compound 2) in rat or dog

SpesiesDose (mg/kg)Cl (mL/min/Kg)Clunbound (mL/min/Kg)Vss (L/Kg)Terminal T1/2 (h)Oral Bioavailability
Rat i.v.0.548>48,0000.82.1-
Rat p.o.1----<5%
Dog i.v.0.118>18,0001.02.0-
[IC 50]

JAK1: 2.2 μM (IC50); JAK2: 23.1 μM (IC50); JAK3: 59.9 μM (IC50)
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