Decernotinib
Decernotinib Basic information
- Product Name:
- Decernotinib
- Synonyms:
-
- Decernotinib
- Decernotinib(VX-509)
- (R)-2-((2-(1H-Pyrrolo[2,3-b]pyridin-3-yl)pyrimidin-4-yl)amino)-2-methyl-N-(2,2,2-trifluoroethyl)butanamide
- (2R)-2-Methyl-2-[[2-(1H-pyrrolo[2,3-b]pyridin-3-yl)-4-pyrimidinyl]amino]-N-(2,2,2-trifluoroethyl)butanamide
- VRT 831509
- VX 509
- Butanamide, 2-methyl-2-[[2-(1H-pyrrolo[2,3-b]pyridin-3-yl)-4-pyrimidinyl]amino]-N-(2,2,2-trifluoroethyl)-, (2R)-
- adelatinib
- CAS:
- 944842-54-0
- MF:
- C18H19F3N6O
- MW:
- 392.38
- Product Categories:
-
- Inhibitors
- Mol File:
- 944842-54-0.mol
Decernotinib Chemical Properties
- Density
- 1.363±0.06 g/cm3(Predicted)
- storage temp.
- 4°C, protect from light, stored under nitrogen
- solubility
- insoluble in H2O; ≥16.95 mg/mL in DMSO; ≥2.92 mg/mL in EtOH with ultrasonic
- form
- solid
- pka
- 12.36±0.40(Predicted)
- color
- White to off-white
Decernotinib Usage And Synthesis
Uses
Decernotinib is a potent and selective Janus kinase 3 inhibitor for treatment of autoimmune diseases.
Biological Activity
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.
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