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1609465-89-5

1609465-89-5 Structure

1609465-89-5 Structure
IdentificationBack Directory
[Name]

(R)-5-Amino-1-(1-cyanopiperidin-3-yl)-3-(4-[2,4-difluorophenoxy]phenyl)-1H-pyrazole-4-carboxamide
[CAS]

1609465-89-5
[Synonyms]

PF-06250112
PF06250112,PF 06250112
(R)-5-Amino-1-(1-cyanopiperidin-3-yl)-3-(4-[2,4-difluorophenoxy]phenyl)-1H-pyrazole-4-carboxamide
1H-Pyrazole-4-carboxamide, 5-amino-1-[(3S)-1-cyano-3-piperidinyl]-3-[4-(2,4-difluorophenoxy)phenyl]-
[Molecular Formula]

C22H20F2N6O2
[MDL Number]

MFCD28100804
[MOL File]

1609465-89-5.mol
[Molecular Weight]

438.43
Chemical PropertiesBack Directory
[Boiling point ]

643.6±55.0 °C(Predicted)
[density ]

1.46±0.1 g/cm3(Predicted)
[storage temp. ]

-20°C
[solubility ]

Soluble in DMSO
[form ]

powder
[pka]

14.99±0.50(Predicted)
[color ]

white to beige
Safety DataBack Directory
[Hazard Codes ]

Xi
[Risk Statements ]

36/37/38
[Safety Statements ]

26
Hazard InformationBack Directory
[Uses]

PF-06250112 is a potent, highly selective, orally bioavailable BTK inhibitor with an IC50 of 0.5 nM, shows inhibitory effect toward BMX nonreceptor tyrosine kinase and TEC with IC50s of 0.9 nM and 1.2 nM, respectively[1].
[Biological Activity]

PF-06250112 is a potent inhibitor of Brutonμs tyrosine kinase (BTK). PF-06250112 blocks both B-cell receptor and FcR-mediated signalingand prevents FcR-dependentAntibody-mediated proteinuria in a mouse glomerulonephritis model.
[References]

[1] Rankin AL, et al. Selective inhibition of BTK prevents murine lupus and antibody-mediated glomerulonephritis. J Immunol. 2013 Nov 1;191(9):4540-50. DOI:10.4049/jimmunol.1301553
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