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Deucravacitinib (BMS-986165) is a highly selective, orally bioavailable, allosteric TYK2 inhibitor for the treatment of autoimmune diseases. It blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain, inhibiting IL-12/23 and type I IFN pathways. It selectively binds to the TYK2 pseudokinase (JH2) domain with an IC50 of 1.0 nM.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $54 | In Stock | In Stock | |
| 5 mg | $147 | In Stock | In Stock | |
| 10 mg | $275 | In Stock | In Stock | |
| 25 mg | $432 | In Stock | In Stock | |
| 50 mg | $638 | In Stock | In Stock | |
| 100 mg | $908 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $161 | In Stock | In Stock |
| Description | Deucravacitinib (BMS-986165) is a highly selective, orally bioavailable, allosteric TYK2 inhibitor for the treatment of autoimmune diseases. It blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain, inhibiting IL-12/23 and type I IFN pathways. It selectively binds to the TYK2 pseudokinase (JH2) domain with an IC50 of 1.0 nM. |
| Targets&IC50 | Tyk2 JH2:0.2 nM, IL-12:2–19 nM, IL-23:2–19 nM, IFN-α:2–19 nM, JAK1 JH2:1 nM |
| In vitro | METHODS: The mean daily percent inhibition of TYK2 was simulated by Deucravacitinib (BMS-986165) (6 mg/12 mg once daily) at clinically relevant concentrations.
RESULTS Deucravacitinib (BMS-986165) had minimal effects on IL-2-induced STAT5 phosphorylation (JAK 1/3) and TPO-induced STAT3 phosphorylation (JAK 2/2). [3] |
| In vivo | METHODS: When mirdametinib was used in combination with Deucravacitinib (BMS-986165) (40 μM) in JW23.3 cells, cell growth was observed.
RESULTS Both drugs synergistically inhibited cell proliferation and increased cell apoptosis compared to either drug alone. [4] |
| Synonyms | BMS-986165 |
| Molecular Weight | 425.46 |
| Formula | C20H19D3N8O3 |
| Cas No. | 1609392-27-9 |
| Smiles | [2H]C([2H])([2H])NC(=O)c1nnc(NC(=O)C2CC2)cc1Nc1cccc(-c2ncn(C)n2)c1OC |
| Relative Density. | no data available |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 84.2 mg/mL (197.9 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (7.76 mM), Sonication is recommeded. 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
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