Deucravacitinib
Based on 34 publication(s) in Google Scholar
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.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.93%
- CAS No.: 1609392-27-9
- 화학식: C20H19D3N8O3
- 분자량:425.46
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보관:Powder -20°C, 3 years ; In solvent -80°C, 1 year , -20°C, 6 months
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Deucravacitinib
More- Ann Rheum Dis. 2025 Sep 25:S0003-4967(25)04383-3. [Abstract]
- Nat Commun. 2025 Jul 29;16(1):6972. [Abstract]
- Cell Death Differ. 2021 Feb;28(2):748-763. [Abstract]
- Nat Chem Biol. 2022 Dec;18(12):1388-1398. [Abstract]
- Cell Rep Med. 2025 Feb 6:101970. [Abstract]
- Clin Cancer Res. 2023 Apr 14;29(8):1592-1604. [Abstract]
- Mol Syst Biol. 2024 Jan;20(1):28-55. [Abstract]
- J Invest Dermatol. 2025 May 27:S0022-202X(25)00531-7. [Abstract]
- J Invest Dermatol. 2025 Apr 8:S0022-202X(25)00393-8. [Abstract]
- Int J Mol Sci. 2023 May 25;24(11):9243. [Abstract]
- Int J Mol Sci. 2022 May 1;23(9):5040. [Abstract]
- Arthritis Res Ther. 2021 Apr 19;23(1):120. [Abstract]
- Inflamm Bowel Dis. 2021 Oct 18;27(10):1674-1683. [Abstract]
- iScience. 2024 Dec 10;28(1):111563. [Abstract]
- iScience. 2021 May 3;24(6):102498. [Abstract]
- J Biotechnol. 2025 Mar:399:9-18. [Abstract]
- J Biol Chem. 2022 May;298(5):101938. [Abstract]
- Med Microbiol Immunol. 2025 Nov 14;214(1):50. [Abstract]
- PLoS One. 2024 Nov 1;19(11):e0308647. [Abstract]
- Anticancer Drugs. 2025 Apr 1;36(4):280-289. [Abstract]
- Iran J Immunol. 2024 Sep 25;21(3). [Abstract]
- bioRxiv. 2026 May 29.
- Res Sq. 2026 Jan 6.
- bioRxiv. 2025 Oct 15.
- bioRxiv. 2025 Aug 16.
- Patent. US20250235450A1.
- medRxiv. 2025 Mar 01.
- Immune Sys. 2024;0:1–13
- bioRxiv. 2024 Jun 6:2024.06.04.595773. [Abstract]
- bioRxiv. 2024 May 9:2024.03.20.585925. [Abstract]
- bioRxiv. 2023 Jul 1.
- Patent. US20230147873A1.
- Patent. US20220339151A1.
- Patent. US20200345731A1.
Customer Validation & Images
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Cell Proliferation/Viability Assay
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In Vivo Efficacy Study
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IHC
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WB
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WB
Biological Activity
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Tyk2 0.2 nM (IC50) |
JAK1 1 nM (IC50) |
IL-23 |
IL-12 |
STAT1 |
STAT3 |
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.
| 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 % | / | / | / | / |
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.
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Animal Model:C57BL/6 (PK studies; IL-23-driven acanthosis psoriasis model)[2]
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Dosage:7.5 mg/kg; 15 mg/kg; 30 mg/kg
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Administration:p.o.; twice daily; 9 days
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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.
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Animal Model:NZB/W (spontaneous lupus-prone nephritis model; treated for three months)[2]
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Dosage:30 mg/kg
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Administration:p.o.; once daily; three months
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
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.
Chemical Information
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CAS No. 1609392-27-9
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Unlabeled Cas 2417137-50-7
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Appearance Solid
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분자량 425.46
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화학식 C20H19D3N8O3
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Color Off-white to light yellow
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SMILES
O=C(C1=NN=C(NC(C2CC2)=O)C=C1NC3=CC=CC(C4=NN(C)C=N4)=C3OC)NC([2H])([2H])[2H]
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Synonyms
BMS-986165
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 1 year -20°C 6 months
Publications (34)
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Journal Impact Factor
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Most Recent
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Ann Rheum Dis
Augmentation of immunothrombosis as a key mechanism underlying JAK inhibition associated hypercoagulability in rheumatoid arthritis. [Abstract]2025 Sep 25:S0003-4967(25)04383-3. PMID: 41006174 -
Nat Commun
Autocrine interferon poisoning mediates ADAR1-dependent synthetic lethality in BRCA1/2-mutant cancers. [Abstract]2025 Jul 29;16(1):6972. PMID: 40730818 -
Cell Death Differ
2021 Feb;28(2):748-763. PMID: 32929218
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.
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Nat Chem Biol
2022 Dec;18(12):1388-1398. PMID: 36097295
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).
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Cell Rep Med
2025 Feb 6:101970. PMID: 39938523 -
Clin Cancer Res
MEK Inhibition Synergizes with TYK2 Inhibitors in NF1-Associated Malignant Peripheral Nerve Sheath Tumors. [Abstract]2023 Apr 14;29(8):1592-1604. PMID: 36799629
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.
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Mol Syst Biol
Illuminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics. [Abstract]2024 Jan;20(1):28-55. PMID: 38177929 -
J Invest Dermatol
Pharmacological Characterization of Zasocitinib (TAK-279): An Oral, Highly Selective, and Potent Allosteric TYK2 Inhibitor. [Abstract]2025 May 27:S0022-202X(25)00531-7. PMID: 40441292 -
J Invest Dermatol
2025 Apr 8:S0022-202X(25)00393-8. PMID: 40210114
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.
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Int J Mol Sci
JAK Signaling Is Critically Important in Cytokine-Induced Viral Susceptibility of Keratinocytes. [Abstract]2023 May 25;24(11):9243. PMID: 37298195 -
Int J Mol Sci
In Vitro Assays to Identify Metabolism-Disrupting Chemicals with Diabetogenic Activity in a Human Pancreatic β-Cell Model. [Abstract]2022 May 1;23(9):5040. PMID: 35563431 -
Arthritis Res Ther
Mitochondrial protein CMPK2 regulates IFN alpha-enhanced foam cell formation, potentially contributing to premature atherosclerosis in SLE. [Abstract]2021 Apr 19;23(1):120. PMID: 33874983 -
Inflamm Bowel Dis
2021 Oct 18;27(10):1674-1683. PMID: 33295611 -
iScience
2024 Dec 10;28(1):111563. PMID: 39868044 -
iScience
Mitochondrial CMPK2 mediates immunomodulatory and antiviral activities through IFN-dependent and IFN-independent pathways. [Abstract]2021 May 3;24(6):102498. PMID: 34142025 -
J Biotechnol
2025 Mar:399:9-18. PMID: 39824361 -
J Biol Chem
Mitogen-activated protein kinase phosphatase-1 controls PD-L1 expression by regulating type I interferon during systemic Escherichia coli infection. [Abstract]2022 May;298(5):101938. PMID: 35429501 -
Med Microbiol Immunol
Furamidine enhances IL-23-mediated autophagic response through IL-23R-TYK2-STAT3-dependent regulation of intracellular Ca²⁺ level to facilitate mycobacterial clearance in human macrophages. [Abstract]2025 Nov 14;214(1):50. PMID: 41236630 -
PLoS One
A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]2024 Nov 1;19(11):e0308647. PMID: 39485774 -
Anticancer Drugs
Dual inhibition of TYK2 and PD-L1 boosts immune response in triple negative breast cancer. [Abstract]2025 Apr 1;36(4):280-289. PMID: 39774369 -
Iran J Immunol
2024 Sep 25;21(3). PMID: 39319693 -
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bioRxiv
2024 Jun 6:2024.06.04.595773. PMID: 38895380 -
bioRxiv
Pharmacological inhibition of tyrosine protein-kinase 2 reduces islet inflammation and delays type 1 diabetes onset in mice. [Abstract]2024 May 9:2024.03.20.585925. PMID: 38766166 -
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용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
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Data Sheet (282 KB)
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SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Portuguese - PT (419 KB)
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Handling Instructions (2659 KB)
References
[1]. Armstrong AW, et al. Deucravacitinib versus placebo and apremilast in moderate to severe plaque psoriasis: Efficacy and safety results from the 52-week, randomized, double-blinded, placebo-controlled phase 3 POETYK PSO-1 trial. J Am Acad Dermatol. 2023;88(1):29-39. [Content Brief]
[2]. Wrobleski ST, et al. Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165. J Med Chem. 2019;62(20):8973-8995. [Content Brief]
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 |
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| 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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