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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 | Availability | Quantity |
---|---|---|---|
1 mg | $64 | In Stock | |
5 mg | $155 | In Stock | |
10 mg | $289 | In Stock | |
25 mg | $455 | In Stock | |
50 mg | $672 | In Stock | |
100 mg | $956 | In Stock | |
200 mg | $1,290 | In Stock | |
500 mg | $1,920 | In Stock | |
1 mL x 10 mM (in DMSO) | $169 | 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 JH1:0.2 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] |
Alias | 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. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 50 mg/mL (117.52 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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