Upadacitinib

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Description: JAK1-selective inhibitor
Chemical Name: (3S,4R)-3-Ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)-1-pyrrolidinecarboxamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (3)
Pathways (1)

Biological Activity for Upadacitinib

Upadacitinib is a potent and selective JAK1 inhibitor (IC50 = 47 nM). In a cellular assay, Upadacitinib shows selectivity for JAK1 over JAK2, JAK3 and TYK2 (IC50 values are 0.014 μM, 0.593 μM, 1860 μM and 2715 μM). In vivo, Upadacitinib suppresses paw swelling and bone destruction in a rat model of arthritis.

Technical Data for Upadacitinib

M. Wt 380.37
Formula C17H19F3N6O
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1310726-60-3
PubChem ID 58557659
InChI Key WYQFJHHDOKWSHR-MNOVXSKESA-N
Smiles C(C)[C@H]1[C@@](C=2N3C4=C(N=CC3=NC2)NC=C4)(CN(C(NCC(F)(F)F)=O)C1)[H]

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 Upadacitinib

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 38.04 100
ethanol 19.02 50

Preparing Stock Solutions for Upadacitinib

The following data is based on the product molecular weight 380.37. 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 2.63 mL 13.15 mL 26.29 mL
5 mM 0.53 mL 2.63 mL 5.26 mL
10 mM 0.26 mL 1.31 mL 2.63 mL
50 mM 0.05 mL 0.26 mL 0.53 mL

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References for Upadacitinib

References are publications that support the biological activity of the product.

Parmentier et al (2018) In vitro and in vivo characterization of the JAK1 selectivity of upadacitinib (ABT-494). BMC Rheumatol. 2 23 PMID: 30886973


If you know of a relevant reference for Upadacitinib, please let us know.

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Keywords: Upadacitinib, Upadacitinib supplier, Potent, selective, JAK1, JAK2, JAK3, inhibitors, inhibits, janus, kinase, arthritis, in, vivo, JAK, 7783, Tocris Bioscience

Citations for Upadacitinib

Citations are publications that use Tocris products.

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

Reviews for Upadacitinib

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


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Pathways for Upadacitinib

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.