2. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling Immunology/Inflammation
  3. JAK STAT Interleukin Related IFNAR
  4. Deucravacitinib

Deucravacitinib  (Synonyms: BMS-986165)

製品番号: HY-117287 純度: 99.93%
COA 取扱説明書 Technical Support

Deucravacitinib (BMS-986165) is an orally active allosteric inhibitor of tyrosine kinase 2 (TYK2), with an IC50 of 0.2 nM and a Ki of 0.02 nM against the JH2 domain of TYK2, and it exhibits selectivity over other JAK subtypes and most of the kinome. Deucravacitinib blocks IL-23, IL-12, p-STAT1/3 and Type I IFN signaling, and inhibits Th17/Th1-mediated psoriasis inflammation. Deucravacitinib can be used in research related to moderate-to-severe plaque psoriasis, inflammatory bowel disease and systemic lupus erythematosus.

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CAS 番号 : 1609392-27-9

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 209 在庫あり
Solution
10 mM * 1 mL in DMSO USD 209 在庫あり
Solid
2 mg $95 お問い合わせ 2-4 weeks 2-4 weeks 2-4 weeks 2-4 weeks
5 mg $190 在庫あり
10 mg $350 在庫あり
25 mg $550 在庫あり
50 mg $850 在庫あり
100 mg $1200 在庫あり
200 mg $1560 在庫あり
500 mg $2400 お問い合わせ 2-4 weeks 2-4 weeks 2-4 weeks 2-4 weeks
1 g $3120 在庫あり
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カスタマーレビュー

Based on 33 publication(s) in Google Scholar

Other Forms of Deucravacitinib:

Deucravacitinib 関連抗体

Top Publications Citing Use of Products

顧客検証

WB
Cell Proliferation/Viability Assay
IHC
In Vivo Efficacy Study

    Deucravacitinib purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2023 Apr 14;29(8):1592-1604.  [Abstract]

    Deucravacitinib (5-80 μM; 0-72 h). The specific TYK2 inhibitor deucravacitinib (BMS-986165) decreases MPNST cell proliferation at lower doses.

    Deucravacitinib purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2023 Apr 14;29(8):1592-1604.  [Abstract]

    The combination of drugs inhibiting TYK2 and MEK block MPNST tumor growth in mice. Mice with JW23.3 MPNST xenograft tumors were treated daily with 30 mg/kg deucravacitinib (Deucra, BMS-986165), the combination of drugs, or vehicle control for 3 weeks or until tumors reached the maximum allowed volume.

    Deucravacitinib purchased from MedChemExpress. Usage Cited in: J Invest Dermatol. 2025 Apr 8:S0022-202X(25)00393-8.  [Abstract]

    BMS-986165 (10 mg/kg; Oral). Representative images of histopathology images taken from each experimental group.

    Deucravacitinib purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2022 Dec;18(12):1388-1398.  [Abstract]

    Western blots measuring effects of VVD-118313 (5a) and BMS-986165 (BMS) (2 µM, 2 h) on JAK1 phosphorylation (pJAK1).

    Deucravacitinib purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2021 Feb;28(2):748-763.  [Abstract]

    BMS-986165 (0.02-1 μM; 18 h).Cells are treated with the allosteric TYK2 inhibitor BMS-986165 (TYK2 Inh.). BMS-986165 dose-dependently inhibits upregulation of CASP5 in response to LPS in U937 macrophages.

    JAK アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    JAK1 JAK2 JAK3 Tyk2 JAK

    STAT アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    STAT3 STAT5 STAT6 STAT1

    Interleukin Related アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

    • 生物活性

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    Deucravacitinib (BMS-986165) is an orally active allosteric inhibitor of tyrosine kinase 2 (TYK2), with an IC50 of 0.2 nM and a Ki of 0.02 nM against the JH2 domain of TYK2, and it exhibits selectivity over other JAK subtypes and most of the kinome. Deucravacitinib blocks IL-23, IL-12, p-STAT1/3 and Type I IFN signaling, and inhibits Th17/Th1-mediated psoriasis inflammation. Deucravacitinib can be used in research related to moderate-to-severe plaque psoriasis, inflammatory bowel disease and systemic lupus erythematosus[1][2].

    Application

    1. This compound can be used as a tracer.
    2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.

    IC50 & Target[2]

    Tyk2

    0.2 nM (IC50)

    JAK1

    1 nM (IC50)

    IL-23

     

    IL-12

     

    STAT1

     

    STAT3

     

    体外実験

    Deucravacitinib potently inhibits TYK2-dependent IFNα-induced STAT5 phosphorylation in human CD3+ T cells, with an IC50 of 2 nM[2].
    Deucravacitinib potently inhibits TYK2-dependent IL-23-induced STAT3 phosphorylation in human CD161+ CD3+ T cells, with an IC50 of 9 nM[2].
    Deucravacitinib potently inhibits TYK2-dependent IFNα-induced STAT5 phosphorylation in human whole blood with an IC50 of 13 nM, while exhibiting high functional selectivity for signaling pathways dependent on JAK2, JAK1 and JAK3[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Deucravacitinib 関連抗体
    Parmacokinetics
    Species Dose Route Cmax AUC Bioavailability CL Vss T1/2 MRT
    Mice[2] 1 mg/kg i.v. / / / 13.2 mL/min/kg 2.9 L/kg 4.2 h 3.6 h
    Mice[2] 10 mg/kg p.o. 7.5 μM 36.4 μM·h 122 % / / / /
    Dog[2] 2 mg/kg i.v. / / / 6.8 mL/min/kg 2.3 L/kg 4.6 h 5.5 h
    Dog[2] 10 mg/kg p.o. 6.9 μM 73.6 μM·h 128 % / / / /
    Monkey[2] 2 mg/kg i.v. / / / 4.8 mL/min/kg 2 L/kg 5.3 h 7 h
    Monkey[2] 10 mg/kg p.o. 5.9 μM 75.7 μM·h 87 % / / / /
    体内実験

    Deucravacitinib (7.5-30 mg/kg; p.o.; twice daily; for 9 consecutive days) exhibits dose-dependent efficacy in a mouse IL-23-driven psoriasis model[2].
    Deucravacitinib (50 mg/kg; p.o.; twice daily) almost completely inhibits body weight loss and significantly reduces histological damage in a mouse model of anti-CD40-induced colitis[2].
    Deucravacitinib (30 mg/kg; p.o.; once daily; for 3 consecutive months) is well tolerated in a mouse lupus model and exerts significant efficacy in preventing nephritis[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: C57BL/6 (PK studies; IL-23-driven acanthosis psoriasis model)[2]
    Dosage: 7.5 mg/kg; 15 mg/kg; 30 mg/kg
    Administration: p.o.; twice daily; 9 days
    Result: Reduced ear thickness increase relative to vehicle, inhibited epidermal hyperplasia and inflammatory cellular infiltration, and dose-dependently reduced relative gene expression of IL-17a, IL-21, IL-23a, IL-23R, IL-12 (p35), and IL-12 (p40) in skin biopsies at 7.5 mg/kg twice daily.
    Maintained drug levels at or above mouse whole blood IC50 (100 nM) for 19 hours at 7.5 mg/kg twice daily.
    Achieved ear thickness inhibition equivalent to the anti-IL-23 adnectin positive control, reduced epidermal hyperplasia and inflammatory cellular infiltration, showed greater reduction of cytokine gene expression than the 7.5 mg/kg dose, and maintained drug levels at or above mouse whole blood IC50 for 21 hours at 15 mg/kg twice daily.
    Provided greater ear thickness protection than the anti-IL-23 adnectin, more effectively inhibited epidermal hyperplasia and inflammatory cellular infiltration than the positive control, showed the greatest reduction of cytokine gene expression across all doses, and maintained drug levels at or above mouse whole blood IC50 for 24 hours at 30 mg/kg twice daily.
    Animal Model: NZB/W (spontaneous lupus-prone nephritis model; treated for three months)[2]
    Dosage: 30 mg/kg
    Administration: p.o.; once daily; three months
    Result: Was well-tolerated, highly efficacious in protecting against nephritis, inhibited type I IFN-dependent gene expression in whole blood and kidneys, and was at least as effective as a blocking anti-IFNαR antibody control; efficacy correlated with coverage of the whole blood IC50 over dosing intervals.
    臨床実験
    分子量

    425.46

    分子式

    C20H19D3N8O3
    CAS 番号
    Unlabeled CAS
    Appearance

    Solid

    Color

    Off-white to light yellow

    SMILES

    O=C(C1=NN=C(NC(C2CC2)=O)C=C1NC3=CC=CC(C4=NN(C)C=N4)=C3OC)NC([2H])([2H])[2H]
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 33.33 mg/mL (78.34 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.3504 mL 11.7520 mL 23.5040 mL
    5 mM 0.4701 mL 2.3504 mL 4.7008 mL
    10 mM 0.2350 mL 1.1752 mL 2.3504 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

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    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

    C1

    ×
    体積 （開始）

    V1

    =
    濃度 （終了）

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    V2

    体内:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: 3.83 mg/mL (9.00 mM); Suspended solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.88 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    % 
    +
    %
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション

    純度: 99.93%

    COA (253 KB) HNMR (286 KB) RP-HPLC (246 KB)

    取扱説明書 (2659 KB)
    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.3504 mL 11.7520 mL 23.5040 mL 58.7599 mL
    5 mM 0.4701 mL 2.3504 mL 4.7008 mL 11.7520 mL
    10 mM 0.2350 mL 1.1752 mL 2.3504 mL 5.8760 mL
    15 mM 0.1567 mL 0.7835 mL 1.5669 mL 3.9173 mL
    20 mM 0.1175 mL 0.5876 mL 1.1752 mL 2.9380 mL
    25 mM 0.0940 mL 0.4701 mL 0.9402 mL 2.3504 mL
    30 mM 0.0783 mL 0.3917 mL 0.7835 mL 1.9587 mL
    40 mM 0.0588 mL 0.2938 mL 0.5876 mL 1.4690 mL
    50 mM 0.0470 mL 0.2350 mL 0.4701 mL 1.1752 mL
    60 mM 0.0392 mL 0.1959 mL 0.3917 mL 0.9793 mL
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    Deucravacitinib Related Classifications

    • Molarity Calculator

    • Dilution Calculator

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    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    質量   濃度   体積   分子量 *
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    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Deucravacitinib1609392-27-9BMS-986165BMS986165BMS 986165JAKSTATInterleukin RelatedIFNARJanus kinaseILInterferon-α/β receptorInterferon-alpha/beta receptortyrosine kinase 2JAK isoformssystemic lupus erythematosushuman CD161+ CD3+ T-cellsTYK2 JH2 domainplaque psoriasisTF-1 cellspsoriatic arthritishuman CD3+ T-cellsinflammatory bowel diseaseInhibitorinhibitorinhibit

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    製品名:
    Deucravacitinib
    製品番号:
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