PF 06551600 malonate

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Description: Potent and selective JAK3 inhibitor
Chemical Name: 1-[(2S,5R)-2-Methyl-5-(7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-1-piperidinyl]-2-propen-1-one malate
Purity: ≥98% (HPLC)
Reviews (1)
Pathways (1)

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.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Compound Libraries for PF 06551600 malonate

PF 06651600 malonate is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.

Technical Data for PF 06551600 malonate

M. Wt 389.41
Formula C15H19N5O.C3H4O4
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 2140301-97-7
PubChem ID 124203830
Smiles C[C@H]1CC[C@@H](NC2=C3C=CNC3=NC=N2)CN1C(C=C)=O.OC(CC(O)=O)=O

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
water 38.94 100
DMSO 38.94 100

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.

Select a batch to recalculate based on the batch molecular weight:
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

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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

If you know of a relevant reference for PF 06551600 malonate, please let us know.

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Citations for PF 06551600 malonate

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Reviews for PF 06551600 malonate

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Works well for JAK inhibitor..
By Scott Scarneo on 08/07/2019
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: THP-1 Cells

To test the effects of this inhibitor on TNF production in stimulated THP-1 cells.

review image

Pathways for PF 06551600 malonate

JAK-STAT Signaling Pathway

JAK-STAT Signaling Pathway

The JAK-STAT signaling pathway has several roles, including the control of cell proliferation and hematopoiesis. It is the main signal transduction cascade from cytokine receptors.