Fadeucravacitinib
Based on 1 Customer Validation
Fadeucravacitinib (Tyk2-IN-8) is an orally active selective TYK2 inhibitor with an IC50 of 5.7 nM against the JH2 pseudokinase domain. Fadeucravacitinib specifically binds to the TYK2 JH2 domain to exert allosteric inhibition, reduces JH1 kinase activity, and thereby blocks the TYK2/STAT pathway and pro-inflammatory signaling cascades. Fadeucravacitinib can be used in research related to inflammatory bowel disease.
For research use only. We do not sell to patients.
- Purity: 98.04%
- CAS No.: 2704587-24-4
- Formula: C20H19D3N8O3
- Molecular Weight:425.46
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NK92 cells
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Concentration:0.31 μM-2.5 mM (serial 4-fold dilutions, incubated with NK92 cells and IL-12 for 24 hours)
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Incubation Time:24 h
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Result:Inhibited IL-12-induced IFN-γ secretion in NK92 cells.
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Animal Model:CB17-Scid mice (female, 8-10 weeks old, 18-20 g) were subjected to a single intraperitoneal injection of 100 μg FGK4.5 anti-CD40 monoclonal antibody (dissolved in PBS) to induce intestinal inflammation (colitis model)[1]
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Dosage:1.5 mg/kg, 5 mg/kg, 15 mg/kg
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Administration:p.o.; twice daily; administered from Day 0 to Day 7, a total of 8 days of treatment.
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Result:Effectively protected the mice with induced colitis, significantly alleviating and preventing the severe body weight loss caused by the disease.
Significantly prevented inflammation-induced spleen enlargement in the mice.
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. 2704587-24-4
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Unlabeled Cas 2417137-50-7
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Appearance Solid
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Molecular Weight 425.46
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Formula C20H19D3N8O3
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Color Off-white to gray
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SMILES
[2H]C([2H])([2H])OC1=C(C2=NN(C)C=N2)C=CC=C1NC3=C(N=NC(NC(C4CC4)=O)=C3)C(NC)=O
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Synonyms
Tyk2-IN-8
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (235.04 mM; ultrasonic and warming and heat to 80°C; 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (289 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[2]. Zhou Y, et al. Novel Small Molecule Tyrosine Kinase 2 Pseudokinase Ligands Block Cytokine-Induced TYK2-Mediated Signaling Pathways. Frontiers in immunology. 2022;13:884399. [Content Brief]
[3]. Modak S, et al. B7H3-Directed Intraperitoneal Radioimmunotherapy With Radioiodinated Omburtamab for Desmoplastic Small Round Cell Tumor and Other Peritoneal Tumors: Results of a Phase I Study. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2020 Dec 20;38(36):4283-4291. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| 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 | |
| 80 mM | 0.0294 mL | 0.1469 mL | 0.2938 mL | 0.7345 mL | |
| 100 mM | 0.0235 mL | 0.1175 mL | 0.2350 mL | 0.5876 mL |
Fadeucravacitinib Related Classifications
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