1. Epigenetics
    Stem Cell/Wnt
    JAK/STAT Signaling
  2. JAK
  3. Upadacitinib tartrate tetrahydrate

Upadacitinib tartrate tetrahydrate (Synonyms: ABT-494 tartrate tetrahydrate)

Cat. No.: HY-19569A
Handling Instructions

Upadacitinib (ABT-494) tartrate tetrahydrate is a potent, orally active and selective Janus kinase 1 (JAK1) inhibitor (IC50=43 nM). Upadacitinib tartrate tetrahydrate displays approximately 74 fold selective for JAK1 over JAK2 (200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib tartrate tetrahydrate can be used for several autoimmune disorders research.

For research use only. We do not sell to patients.

Upadacitinib tartrate tetrahydrate Chemical Structure

Upadacitinib tartrate tetrahydrate Chemical Structure

CAS No. : 1607431-21-9

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Description

Upadacitinib (ABT-494) tartrate tetrahydrate is a potent, orally active and selective Janus kinase 1 (JAK1) inhibitor (IC50=43 nM). Upadacitinib tartrate tetrahydrate displays approximately 74 fold selective for JAK1 over JAK2 (200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib tartrate tetrahydrate can be used for several autoimmune disorders research[1][2].

IC50 & Target[1]

JAK1

0.043 μM (IC50)

JAK2

0.2 μM (IC50)

JAK3

2.3 μM (IC50)

Tyk2

4.7 μM (IC50)

In Vitro

In biochemical assays, Upadacitinib tartrate tetrahydrate is 74-fold more selective for JAK-1 than for JAK-2 (which is involved in erythropoiesis) and 58-fold more selective for JAK-1 than for JAK-3 (which is involved in immunosurveillance)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Upadacitinib (0.1-10 mg/kg; oral gavage; twice a day for 10 days) tartrate tetrahydrate demonstrates efficacy in rat arthritis models[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female Lewis rats (Rat adjuvant-induced arthritis model)[3]
Dosage: 0.1, 0.3, 1, 3, 10 mg/kg
Administration: Oral gavage; twice a day for 10 days
Result: Inhibited disease pathology in rat adjuvant induced arthritis.
Molecular Weight

602.52

Formula

C17H19F3N6O.C4H6O6.4H2O

CAS No.
SMILES

O=C(NCC(F)(F)F)N1C[[email protected]]([[email protected]](C1)C2=CN=C3C=NC4=C(N32)C=CN4)CC.O=C([[email protected]@H]([[email protected]](C(O)=O)O)O)O.[4.H2O]

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Product Name:
Upadacitinib tartrate tetrahydrate
Cat. No.:
HY-19569A
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