[CAS NO. 1310726-60-3] Upadacitinib (ABT-494)

Name: Upadacitinib (ABT-494)
Brand: Arctom Scientific
SKU: SLK-S8162

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PRODUCTS SPECIFICATIONS [1310726-60-3]

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Catalog

SLK-S8162

Brand

Selleck

CAS

1310726-60-3

DESCRIPTION [1310726-60-3]

Overview

MDL	MFCD30502663
Molecular Weight	380.37
Molecular Formula	C17H19F3N6O
SMILES	C(C)[C@H]1[C@@](C=2N3C4=C(N=CC3=NC2)NC=C4)(CN(C(NCC(F)(F)F)=O)C1)[H]

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.6290 mL	13.1451 mL	26.2902 mL
5 mM	0.5258 mL	2.6290 mL	5.2580 mL
10 mM	0.2629 mL	1.3145 mL	2.6290 mL
50 mM	0.0526 mL	0.2629 mL	0.5258 mL

Description

Upadacitinib (ABT-494) is a selective inhibitor which demonstrates activity against JAK1 (0.045 μM) and JAK2 (0.109 μM), with > 40 fold selectivity over JAK3 (2.1 μM) and 100 fold selectivity over TYK2 (4.7 μM) as compared to JAK1.

Targets

JAK1 ^[1] (Cell-free assay)	JAK2 ^[1] (Cell-free assay)
45 nM	109 nM

In vitro

Upadacitinib is most potent on JAK1compared to other family members (JAK1 > JAK2 > JAK3 > TYK2). Upadacitinib demonstrates selectivity across a broad panel of 70+ kinases, with only Rock1 and Rock2 demonstrating IC50 values below 1 μM. Consistent with the Ba/F3 cellular data, upadacitinib potently inhibits the JAK1 dependent cytokines IL-6, OSM, IL-2, and IFNγ, as measured by inhibition of STAT phosphorylation.

References

[1] Julie M. Parmentier, et al. BMC Rheumatology. 2018, 23.
[2] Tamara Pérez-Jeldres, et al. Front Pharmacol. 2019, 10: 212.

Synonyms

1-Pyrrolidinecarboxamide, 3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)-, (3S,4R)-

(3S,4R)-3-Ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)-1-pyrrolidinecarboxamide

rel-(-)-(3S,4R)-3-Ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide

Upadacitinib

ABT 494

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