Home / Pharmacology / Enzymes / Kinases / JAK / JAK Inhibitors / PF 06551600 malonate

PF 06551600 malonate

Cat. No. 6506 1 Review Submit a Review Datasheet / COA / SDS
Pricing Availability   Qty
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 (1)
Pathways (1)
Biological Activity Technical Data Solubility Calculators Datasheets References

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
InChI Key QMPMPSGDPRHZCG-VZXYPILPSA-N
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
Solubility
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

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

Product Datasheets for PF 06551600 malonate

Certificate of Analysis / Product Datasheet
Safety Datasheet

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.

View Related Products by Target

View Related Products by Product Action

View all JAK Inhibitors

Keywords: PF 06651600 malonate, PF 06651600 malonate supplier, PF06651600, malonate, JAK3, kinase, inhibitors, inhibits, potent, selective, anti-inflammatory, JAK, 6506, Tocris Bioscience

Citations for PF 06551600 malonate

Citations are publications that use Tocris products.

Currently there are no citations for PF 06551600 malonate. Do you know of a great paper that uses PF 06551600 malonate from Tocris? Please let us know.

Reviews for PF 06551600 malonate

Average Rating: 5 (Based on 1 Review.)

5 Star
100%
4 Star
0%
3 Star
0%
2 Star
0%
1 Star
0%

Have you used PF 06551600 malonate?

Submit a review and receive an Amazon gift card.

$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image

$25/€18/£15/$25CAN/¥75 Yuan/¥2500 Yen for a review with an image

$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image

Submit a Review

Filter by:


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.