Decernotinib(VX-509) (Synonyms: Decernotinib, VRT-831509) |
| Catalog No.GC10770 |
Le decernotinib (VX-509) est un puissant inhibiteur de JAK3 actif par voie orale, avec un Kis de 2,5, 11, 13 et 11 nM pour JAK3, JAK1, JAK2 et TYK2, respectivement.
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Cas No.: 944842-54-0
Sample solution is provided at 25 µL, 10mM.
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Decernotinib(VX-509)is a novel, potent and selective inhibitor of JAK3 with Ki value of 2 nM [1].
The Janus kinase family consists of four members: JAK1, JAK2, JAK3, and TYK2. Janus kinase 3 (JAK3) is mainly expressed in lymphocytes, which are cells important to the immune response associated with many diseases, including rheumatoid arthritis (RA) [1].
Decernotinib(VX-509)is a novel, potent, selective and orally available JAK3 inhibitor for the treatment of autoimmune diseases. VX-509 inhibited JAK1, JAK2, JAK3, and TYK2 with Ki values of 11, 13, 2 and 11 nM, respectively. In HT-2 or TF-1 cells, VX-509 inhibited JAK3/1- or JAK2-mediated phosphorylation of STAT5 following stimulation with IL-2 or GMCSF with IC50 values of 99 and 2600 nM, respectively [1].
In the rat host versus graft (HvG) model, VX-509 at 50 mg/kg bid or 100 mg/kg qd significantly and dose-dependently inhibited popletial lymph node (PLN) hyperplasia by 66% and 94%, respectively, relative to cyclosporin A (CsA). VX-509 also significantly reduced CD25 expression. These results suggested that VX-509 showed significant dose-dependent immunosuppressive activity and effectively inhibited T-cell activation [1]. In the rat collagen-induced arthritis model, VX-509 dose-dependently reduced ankle swelling and paw weight, and improved paw histopathology scores. In oxazolone-induced delayed-type hypersensitivity mouse model, VX-509 reduced the T cell-mediated inflammatory response in skin [2].
References:
[1]. Farmer LJ, Ledeboer MW, Hoock T, et al. Discovery of VX-509 (Decernotinib): A Potent and Selective Janus Kinase 3 Inhibitor for the Treatment of Autoimmune Diseases. J Med Chem, 2015, 58(18): 7195-7216.
[2]. Mahajan S, Hogan JK, Shlyakhter D, et al. VX-509 (decernotinib) is a potent and selective janus kinase 3 inhibitor that attenuates inflammation in animal models of autoimmune disease. J Pharmacol Exp Ther, 2015, 353(2): 405-414.
| Cas No. | 944842-54-0 | SDF | |
| Synonymes | Decernotinib, VRT-831509 | ||
| Chemical Name | (R,Z)-2-((2-(1H-pyrrolo[2,3-b]pyridin-3-yl)pyrimidin-4-yl)amino)-2-methyl-N-(2,2,2-trifluoroethyl)butanimidic acid | ||
| Canonical SMILES | CC[C@](/C(O)=N/CC(F)(F)F)(NC1=NC(C2=CNC3=C2C=CC=N3)=NC=C1)C | ||
| Formula | C18H19F3N6O | M.Wt | 392.38 |
| Solubility | ≥ 16.95mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5485 mL | 12.7427 mL | 25.4855 mL |
| 5 mM | 0.5097 mL | 2.5485 mL | 5.0971 mL |
| 10 mM | 0.2549 mL | 1.2743 mL | 2.5485 mL |
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- Purity: >98.00%
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