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PF 06551600 malonate
Biological Activity for PF 06551600 malonate
PF 06551600 malonate is a potent and selective JAK3 inhibitor (IC50 = 33.1 μM). Exhibits no significant activity against a panel of other kinases including JAK1, JAK2 and TYK2. Inhibits phosphorylation of STAT5, induced by IL-2, IL-4, IL-7 and IL-15. Suppresses Th1 and Th17 T-cell differentiation and function in vitro. Reduces paw swelling in a rat model of arthritis and reduces disease severity in a rat EAE model.
Sold for research purposes under agreement from Pfizer Inc.
Compound Libraries for PF 06551600 malonate
Technical Data for PF 06551600 malonate
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for PF 06551600 malonate
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for PF 06551600 malonate
The following data is based on the product molecular weight 389.41. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.57 mL||12.84 mL||25.68 mL|
|5 mM||0.51 mL||2.57 mL||5.14 mL|
|10 mM||0.26 mL||1.28 mL||2.57 mL|
|50 mM||0.05 mL||0.26 mL||0.51 mL|
Product Datasheets for PF 06551600 malonate
References for PF 06551600 malonate
References are publications that support the biological activity of the product.
Thorarensen et al (2017) Design of a Janus Kinase 3 (JAK3) specific inhibitor 1-((2S,5R)-5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) allowing for the interrogation of JAK3 signaling in humans. J.Med.Chem. 60 1971 PMID: 28139931
Telliez et al (2016) Discovery of a JAK3-selective inhibitor: functional differentiation of JAK3-selective inhibition over pan-JAK or JAK1-selective inhibition. ACS Chem.Biol. 11 3442 PMID: 27791347
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Citations for PF 06551600 malonate
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Reviews for PF 06551600 malonate
Average Rating: 5 (Based on 1 Review.)
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Literature in this Area
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