2. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling Immunology/Inflammation
  3. JAK IFNAR
  4. TYK2-IN-12

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.

For research use only. We do not sell to patients.

TYK2-IN-12 Chemical Structure

TYK2-IN-12 Chemical Structure

CAS No. : 2244061-66-1

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Based on 1 publication(s) in Google Scholar

TYK2-IN-12 Related Antibodies

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Description

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[1].

IC50 & Target

Tyk2

0.51 nM (Ki)

JAK3

6.63 nM (Ki)

JAK2

21.93 nM (Ki)

JAK1

45.9 nM (Ki)

In Vitro

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 Related Antibodies
In Vivo

TYK2-IN-12 (compound 30) (0-100 mg/kg, PO, daily for 10 days) dose-dependently reduces immune responses[1].
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.

Animal Model: C57BL/6 mice (IL-23 induced inflammation model)[1]
Dosage: 0, 10, 30, and 100 mg/kg
Administration: PO, daily for 10 days
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.
Animal Model: Male C57Bl/6 mice, male SD rats[1]
Dosage: 3 mg/kg (IV), 10 mg/kg (PO)
Administration: IV or PO, once (Pharmacokinetic Analysis)
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%.
Molecular Weight

434.44

Formula

C24H20F2N4O2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

FC1=CC=CC(F)=C1C2=NC(CN3)=C(C(NC4=CC=C(C(N5CCCC5)=O)C=C4)=C2)C3=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3018 mL 11.5091 mL 23.0181 mL
5 mM 0.4604 mL 2.3018 mL 4.6036 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, 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.

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Purity & Documentation
References

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
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TYK2-IN-12 Related Classifications

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:

TYK2-IN-122244061-66-1JAKIFNARJanus kinaseInterferon-α/β receptorInterferon-alpha/beta receptorPsoriasisPyrrolidino-pyridinePyrrolidino-pyrimidineFEPPBMCIL12pSTAT4Inhibitorinhibitorinhibit

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