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> Upadacitinib [1310726-60-3]

Upadacitinib [1310726-60-3]

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Katalog-Nummer HY-19569-100mg

Size : 100mg

Marke : MedChemExpress

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

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Upadacitinib Chemische Struktur

Upadacitinib Chemische Struktur

CAS. Nr. : 1310726-60-3

This product is a controlled substance and not for sale in your territory.

Based on 12 publication(s) in Google Scholar

Other Forms of Upadacitinib:

  • Upadacitinib-15N,d2 In-stock
  • Upadacitinib tartrate tetrahydrate Angebot einholen
  • Upadacitinib-d5 Angebot einholen

Alle JAK Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen
JAK1 JAK2 JAK3 Tyk2 JAK
Beschreibung

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

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

Upadacitinib Related Antibodies
In Vivo

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

MedChemExpress (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.
Klinische Studie
Molekulargewicht

380.37

Formel

C17H19F3N6O
CAS. Nr.

1310726-60-3
Appearance

Solid

Color

White to yellow

SMILES

O=C(N1C[C@@H](CC)[C@@H](C2=CN=C3C=NC(NC=C4)=C4N32)C1)NCC(F)(F)F
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Lösungsmittel & Löslichkeit
In Vitro: 

DMSO : 100 mg/mL (262.90 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molaritätsrechner

  • Verdünnungsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

    Solubility: ≥ 2.75 mg/mL (7.23 mM); Clear solution

  • Protocol 2

    Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.75 mg/mL (7.23 mM); Clear solution

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation

Purity: 99.98%

COA (255 KB) HNMR (282 KB) RP-HPLC (255 KB) LCMS (92 KB)

Handling Instructions (2659 KB)
Verweise

  • [1]. Nakayamada S, et al. Recent Progress in JAK Inhibitors for the Treatment of Rheumatoid Arthritis. BioDrugs. 2016 Oct;30(5):407-419.  [Content Brief]

    [2]. J. Voss, et al. THU0127 Pharmacodynamics of A Novel JAK1 Selective Inhibitor in Rat Arthritis and Anemia Models and in Healthy Human Subjects. doi 10.1136/annrheumdis-2014-eular.3823.

    [3]. Parmentier JM, et al. In vitro and in vivo characterization of the JAK1 selectivity of upadacitinib (ABT-494). BMC Rheumatol. 2018 Aug 28;2:23.  [Content Brief]

  • [1]. Nakayamada S, et al. Recent Progress in JAK Inhibitors for the Treatment of Rheumatoid Arthritis. BioDrugs. 2016 Oct;30(5):407-419.

    [2]. J. Voss, et al. THU0127 Pharmacodynamics of A Novel JAK1 Selective Inhibitor in Rat Arthritis and Anemia Models and in Healthy Human Subjects. doi 10.1136/annrheumdis-2014-eular.3823.

    [3]. Parmentier JM, et al. In vitro and in vivo characterization of the JAK1 selectivity of upadacitinib (ABT-494). BMC Rheumatol. 2018 Aug 28;2:23.

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6290 mL 13.1451 mL 26.2902 mL 65.7255 mL
5 mM 0.5258 mL 2.6290 mL 5.2580 mL 13.1451 mL
10 mM 0.2629 mL 1.3145 mL 2.6290 mL 6.5725 mL
15 mM 0.1753 mL 0.8763 mL 1.7527 mL 4.3817 mL
20 mM 0.1315 mL 0.6573 mL 1.3145 mL 3.2863 mL
25 mM 0.1052 mL 0.5258 mL 1.0516 mL 2.6290 mL
30 mM 0.0876 mL 0.4382 mL 0.8763 mL 2.1908 mL
40 mM 0.0657 mL 0.3286 mL 0.6573 mL 1.6431 mL
50 mM 0.0526 mL 0.2629 mL 0.5258 mL 1.3145 mL
60 mM 0.0438 mL 0.2191 mL 0.4382 mL 1.0954 mL
80 mM 0.0329 mL 0.1643 mL 0.3286 mL 0.8216 mL
100 mM 0.0263 mL 0.1315 mL 0.2629 mL 0.6573 mL
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Upadacitinib Related Classifications

  • Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling
  • JAK
Help & FAQs

Keywords:

Upadacitinib1310726-60-3ABT-494ABT494ABT 494JAKJanus kinaseJAK1orally activeautoimmuneInhibitorinhibitorinhibit

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