Upadacitinib [1310726-60-3]

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Cat# NB-64-41747-1mL

Size : 1mLx10mM(inDMSO)

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Upadacitinib (Synonyms: ABT-494)

Catalog No. T7503 Copy Product Info
Purity: 99.94%
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Upadacitinib (ABT-494) (ABT-494) is a selective Janus kinase (JAK) 1 inhibitor, which is being studied for the treatment of several autoimmune disorders in the IC50 of 43 nM.

Upadacitinib

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Synonyms ABT-494

Upadacitinib (ABT-494) (ABT-494) is a selective Janus kinase (JAK) 1 inhibitor, which is being studied for the treatment of several autoimmune disorders in the IC50 of 43 nM.

Upadacitinib
Cas No. 1310726-60-3
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Purity:99.94%
Color:White
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Product Introduction

Bioactivity
Description
Upadacitinib (ABT-494) (ABT-494) is a selective Janus kinase (JAK) 1 inhibitor, which is being studied for the treatment of several autoimmune disorders in the IC50 of 43 nM.
Targets&IC50
JAK3:2.3 μM, JAK2:200 nM, JAK1:43 nM, Tyk2:4.7 μM
In vitro
Upadacitinib is 74-fold more selective for JAK-1 than for JAK-2, which is involved in erythropoiesis. And Upadacitinib is 58-fold more selective for JAK-1 than for JAK-3, which is involved in immunosurveillance. The enhanced selectivity of Upadacitinib for JAK-1 over JAK-2 and JAK-3 may offer an improved benefit-risk profile in patients with RA range.
In vivo
Upadacitinib, a second JAK inhibitor, has been developed by AbbVie.Upadacitinib finished multiple-dose Phase I studies in 2013. Upadacitinib show to be safe and well-tolerated up to multiple doses of 24 mg twice daily using the immediate release formulation in phase I trials. Upadacitinib exposure is dose proportional to the evaluated multiple dose.
SynonymsABT-494
Chemical Properties
Molecular Weight380.37
FormulaC17H19F3N6O
Cas No.1310726-60-3
SmilesCC[C@@H]1CN(C[C@@H]1c1cnc2cnc3[nH]ccc3n12)C(=O)NCC(F)(F)F
Relative Density.1.56 g/cm3 (Predicted)
Storage & Solubility Information
StorageStore at low temperature | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 55 mg/mL (144.6 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.63 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.6290 mL13.1451 mL26.2902 mL131.4510 mL
5 mM0.5258 mL2.6290 mL5.2580 mL26.2902 mL
10 mM0.2629 mL1.3145 mL2.6290 mL13.1451 mL
20 mM0.1315 mL0.6573 mL1.3145 mL6.5725 mL
50 mM0.0526 mL0.2629 mL0.5258 mL2.6290 mL
100 mM0.0263 mL0.1315 mL0.2629 mL1.3145 mL
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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