TYK2-IN-12
Based on 1 Customer Validation
TYK2-IN-12 (compound 30) is an orally active, potent and selective TYK2 (tyrosine kinase 2) inhibitor, with a Ki of 0.51 nM. TYK2-IN-12 inhibits IL-12 induced IFNγ, with IC50 values of 2.7 and 7.0 μM in human and mouse whole blood, respectively. TYK2-IN-12 can be used for psoriasis research.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 98.81%
- CAS No.: 2244061-66-1
- Formule: C24H20F2N4O2
- Masse moléculaire:434.44
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Stockage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Epigenetics Compound Library
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Immunology/Inflammation Compound Library
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JAK/STAT Compound Library
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Kinase Inhibitor Library
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Activité biologique
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Tyk2 0.51 nM (Ki) |
JAK3 6.63 nM (Ki) |
JAK2 21.93 nM (Ki) |
JAK1 45.9 nM (Ki) |
TYK2-IN-12 (compound 30) shows 90, 43, and 13-fold selectivity over JAK1, JAK2, and JAK3, respectively[1].
TYK2-IN-12 exhibits excellent selectivity over hERG (IC50 > 30 μM) and over a panel of 10 cytochrome P450 enzymes (IC50s > 30 μM against CYP450s 3A4, 3D6, 2C9, 2C8, 1A2, 2A6, 2B6, 2C19, 2E1, and 3A5)[1].
TYK2-IN-12 shows cell-based potency and selectivity in human PBMC by blockade of IL-12 induced phospho-STAT4, GM-CSF induced phospho-STAT5, and IL-2 induced phospho-STAT5, with IC50 values of 0.10 μM, 4.1 μM and 0.25 μM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
TYK2-IN-12 (3 mg/kg (IV), 10 mg/kg (PO), once) shows moderate clearance and volumes of distribution, and exhibits moderate to good oral absorption[1].
Pharmacokinetic Parameters of TYK2-IN-12 in male C57Bl/6 mice and smale Sprague-Dawley rats[1].
| Species | Mouse | Rat |
| PPB Fumax (h) | 0.061 | 0.10 |
| CL (mL/min/kg) | 28 | 27 |
| t1/2 (h) | 1.8 | 1.6 |
| Vd (L/kg) | 1.2 | 1.9 |
| F (%) | >90 | 32 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice (IL-23 induced inflammation model)[1]
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Dosage:0, 10, 30, and 100 mg/kg
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Administration:PO, daily for 10 days
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Result:Dose-dependently reduced immune responses, with up to 74 % inhibition of ear swelling and 96 % inhibition of tissue levels of IL-17A at 100 mg/kg, highlighting the crucial role of TYK2 in IL-23 induced IL-17 and tissue inflammation. Exhibited improved skin histology and a dose-dependent reduction of spleen weight.
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Animal Model:Male C57Bl/6 mice, male SD rats[1]
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Dosage:3 mg/kg (IV), 10 mg/kg (PO)
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Administration:IV or PO, once (Pharmacokinetic Analysis)
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Result:Showed moderate clearance and volumes of distribution of 1.2 L/Kg and 1.9 L/Kg, respectively in mouse and rat IV PK, and exhibited moderate to good oral absorption, with oral bioavailabilities of 32-100%.
Chemical Information
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CAS No. 2244061-66-1
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Appearance Solid
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Masse moléculaire 434.44
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Formule C24H20F2N4O2
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Color Off-white to light yellow
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SMILES
FC1=CC=CC(F)=C1C2=NC(CN3)=C(C(NC4=CC=C(C(N5CCCC5)=O)C=C4)=C2)C3=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvant et solubilité
DMSO : 7.14 mg/mL (16.43 mM; ultrasonic and warming and heat to 60°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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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)
Pureté et documentation
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Fiche technique (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
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 (sealed storage, away from moisture). 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 | 2.3018 mL | 11.5091 mL | 23.0181 mL | 57.5453 mL |
| 5 mM | 0.4604 mL | 2.3018 mL | 4.6036 mL | 11.5091 mL | |
| 10 mM | 0.2302 mL | 1.1509 mL | 2.3018 mL | 5.7545 mL | |
| 15 mM | 0.1535 mL | 0.7673 mL | 1.5345 mL | 3.8364 mL |
TYK2-IN-12 Related Classifications
HY-150720 Related Classifications
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