PF 06551600 malonate

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Cat.No. 6506 - PF 06651600 malonate | C15H19N5O.C3H4O4 | CAS No. 2140301-97-7
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)
Datasheet
Citations
Reviews
Literature
Pathways

Biological Activity

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.

Technical Data

M. Wt 389.41
Formula C15H19N5O.C3H4O4
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 2140301-97-7
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 38.94 100
DMSO 38.94 100

Preparing Stock Solutions

The following data is based on the product molecular weight 389.41. Batch specific molecular weights may vary from batch to batch due to solvent 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

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Product Datasheets

Safety Datasheet

References

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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Literature in this Area

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Cancer

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Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

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Pathways for PF 06551600 malonate

JAK-STAT

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.