Upadacitinib (ABT-494) - Moligand™, 10mM in DMSO , Inhibitor of Janus kinase 1;Inhibitor of Janus kinase 2;Inhibitor of Janus kinase 3;Inhibitor of tyrosine kinase 2, CAS No.1310726-60-3, Inhibitor of Janus kinase 1;Inhibitor of Janus kinase 2;Inhibitor of Janus kinase 3;Inhibitor of tyrosine kinase 2

CAS: 1310726-60-3 Cat. No.: U408740 Peso molecular: 380.37 PubChem CID: 58557659

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

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

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

Upadacitinib (ABT-494) is a selectiveJAK1inhibitor 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.
In vitro

Upadacitinib is most potent on JAK1compared to other family members (JAK1\u2009>\u2009JAK2\u2009>\u2009JAK3\u2009>\u2009TYK2). 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.

In vivo

Upadacitinib inhibits disease pathology in rat adjuvant induced arthritis. It is a non-sensitive substrate for cytochrome P450, approximately 20% is eliminated, unchanged, in urine.
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Sinónimos

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

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

Upadacitinib (ABT-494) is a selective JAK1 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.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Grado

Moligand™

Tipo de acción

INHIBITOR

Mecanismo de acción

Inhibitor of Janus kinase 1;Inhibitor of Janus kinase 2;Inhibitor of Janus kinase 3;Inhibitor of tyrosine kinase 2

Propiedades del producto

• ALogP: 2.7

Nombres e identificadores

• Isómeros SMILES: CC[C@@H]1CN(C[C@@H]1C2=CN=C3N2C4=C(NC=C4)N=C3)C(=O)NCC(F)(F)F
• CAS alternativo: 1310726-60-3
• PubChem CID: 58557659
• Términos de entrada MeSH: (3S,4R)-3-ethyl-4-(3H-imidazo(1,2-a)pyrrolo(2,3-e)pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)-1-pyrrolidinecarboxamide;ABT-494;Rinvoq;upadacitinib
• Peso molecular: 380.37

Objetivos asociados (humanos)

TYK2 Tclin Non-receptor tyrosine-protein kinase TYK2 (1 Activities)

Discover Target: TYK2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

JAK3 Tclin Tyrosine-protein kinase JAK3 (1 Activities)

Discover Target: JAK3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

JAK1 Tclin Tyrosine-protein kinase JAK1 (5 Activities)

Discover Target: JAK1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

JAK2 Tclin Tyrosine-protein kinase JAK2 (2 Activities)

Discover Target: JAK2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propiedades químicas y físicas

• Solubilidad: Solubility (25°C) In vitro DMSO: 46 mg/mL (201.54 mM); Ethanol: 46 mg/mL (201.54 mM); Water: Insoluble