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.
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- Purity: 98.04%
- CAS No.: 2704587-24-4
- 화학식: C20H19D3N8O3
- 분자량:425.46
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보관: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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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
[1]|
Tyk2 JH2 5.7 nM (IC50) |
IL-12 |
In Vitro
Fadeucravacitinib (0.31 μM-2.5 mM; 24 h) inhibits IL-12-induced IFN-γ secretion in NK92 cells[1].
Fadeucravacitinib (Compound 3) (61 nM - 1 mM; pre-incubated with JAK2 kinase for 15 minutes and with substrate for 30 minutes) inhibits the enzymatic activity of the recombinant human JAK2 kinase domain (JH1), with an IC50 of 3.0 μM[1].
Fadeucravacitinib exhibits extremely low inhibitory activity against the recombinant human TYK2 kinase domain (JH1) at concentrations ranging from 61 nM to 1 mM, with a pre-incubation time of 15 minutes with TYK2 kinase and a 40-minute incubation with the substrate; its IC50 is greater than 10 μM[1].
Fadeucravacitinib (61 nM - 1 mM; 30 min) potently binds to the recombinant human TYK2 pseudokinase domain (JH2), with an IC50 value of 5.7 nM[1].
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.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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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.
신청
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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분자량 425.46
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
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)
순도&문서
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Data Sheet (290 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 |
|---|---|---|---|---|---|
| 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
HY-144031S Related Classifications
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