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Deucravacitinib

Deucravacitinib
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.
Catalog No. T14687Cas No. 1609392-27-9
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Deucravacitinib

Catalog No. T14687Cas No. 1609392-27-9

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.
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Pack SizePriceAvailabilityQuantity
1 mg$64In Stock
5 mg$155In Stock
10 mg$289In Stock
25 mg$455In Stock
50 mg$672In Stock
100 mg$956In Stock
200 mg$1,290In Stock
500 mg$1,920In Stock
1 mL x 10 mM (in DMSO)$169In Stock
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Product Introduction

Bioactivity
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]
AliasBMS-986165
Chemical Properties
Molecular Weight425.46
FormulaC20H19D3N8O3
Cas No.1609392-27-9
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM2.3504 mL11.7520 mL23.5040 mL117.5199 mL
5 mM0.4701 mL2.3504 mL4.7008 mL23.5040 mL
10 mM0.2350 mL1.1752 mL2.3504 mL11.7520 mL
20 mM0.1175 mL0.5876 mL1.1752 mL5.8760 mL
50 mM0.0470 mL0.2350 mL0.4701 mL2.3504 mL
100 mM0.0235 mL0.1175 mL0.2350 mL1.1752 mL

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