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Purity: ≥98%
Decernotinib (VX509; VRT831509; adelatinib) is a novel, potent, selective, and orally bioavailable inhibitor of JAK3 (Janus associated kinase) with potential anti-inflammatory activities. It inhibits JAK3, JAK1, JAK2, and TYK2 with Ki values of 2.5, 11, 13 and 11 nM, respectively. It has >4-fold selectivity for JAK3 over JAK1, JAK2, and TYK2. Decernotinib is being developed by Vertex for the treatment of inflammatory diseases such as rheumatoid arthritis-RA. In immune-mediated diseases, JAK3 is an essential component of the immune signaling cascade. This cascade ultimately contributes to abnormal immune response that results in chronic inflammation and, in the case of rheumatoid arthritis (RA).
| ln Vitro |
Strong JAK3 inhibitor decernotinib (VX-509) has Ki values of 2.5, 11, 13, and 11 nM for JAK3, JAK1, JAK2, and TYK2, in that order. With a mean IC50 of 170 ± 101 nM, decernotinib potently inhibits T cell proliferation. It also inhibits T cell proliferation driven by IL-2 (IC50, 140, and 400 nM). In reaction to CD40L and IL-4, VX-509 is also cytotoxic (IC50, 50 nM) against B cells [1].
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| ln Vivo |
In rats injected with collagen, decernotinib (VX-509, 10, 25, or 50 mg/kg, po) substantially and dose-dependently reduced the increases in ankle diameter and paw weight. In rats, decernotinib effectively lowers bone resorption and cartilage degradation. Decernotinib (10, 25, or 50 mg/kg, po, bid) reduces delayed-type hypersensitivity-related ear edema in a mouse model [1].
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| References |
[1]. Mahajan S, et al. VX-509 is a potent and selective Janus kinase 3 (JAK3) inhibitor that attenuates inflammation in animal models of autoimmune disease. J Pharmacol Exp Ther. 2015 Mar 11. pii: jpet.114.221176
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| Molecular Formula |
C18H19F3N6O
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| Molecular Weight |
392.38
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| CAS # |
944842-54-0
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| Related CAS # |
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| SMILES |
CC[C@](NC1=NC(C2=CNC3=NC=CC=C32)=NC=C1)(C)C(NCC(F)(F)F)=O.
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| Chemical Name |
(R)-2-((2-(1H-pyrrolo[2,3-b]pyridin-3-yl)pyrimidin-4-yl)amino)-2-methyl-N-(2,2,2-trifluoroethyl)butanamide
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| Synonyms |
PubChem CID 59422203; VX-509; VRT831509 ; VRT-831509; VX509; VX 509 ; VRT 831509 ; Decernotinib; Adelatinib
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.37 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.37 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.37 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01830985 | Completed | Drug: VX-509 | Rheumatoid Arthritis | Vertex Pharmaceuticals Incorporated | April 2013 | Phase 2 Phase 3 |
| NCT01886209 | Completed | Drug: Prednisone Drug: VX-509 |
Drug Interactions | Vertex Pharmaceuticals Incorporated | June 2013 | Phase 1 |
| NCT01754935 | Completed | Drug: VX-509 Drug: VX-509 matching placebo |
Rheumatoid Arthritis | Vertex Pharmaceuticals Incorporated | January 2013 | Phase 2 |
| NCT01590459 | Completed | Drug: VX-509 Drug: VX-509 matching placebo |
Rheumatoid Arthritis | Vertex Pharmaceuticals Incorporated | April 2012 | Phase 2 |
Effect of VX-509 on progression of established disease in rat CIA model.J Pharmacol Exp Ther.2015 May;353(2):405-14. |
(A) Representative histopathology photomicrographs of a control (collagen + vehicle) rat ankle and VX-509 b.i.d. treatment groups, with approximate mean score for group showing synovium (S), cartilage (large arrow), and bone (small arrow).J Pharmacol Exp Ther.2015 May;353(2):405-14. |
Effect of VX-509 on the oxazolone-induced mouse DTH model.J Pharmacol Exp Ther.2015 May;353(2):405-14. |
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