2. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling
  3. JAK
  4. Tyk2-IN-5

Tyk2-IN-5 (compound 6) is a potent, selective and orally active tyrosine kinase 2 (Tyk2) inhibitor that acts on the JH2 structural domain. Tyk2-IN-5 shows a Ki value of 0.086 nM for Tyk2 JH2 and an IC50 value of 25 nM for IFNα. Tyk2-IN-5 efficiently inhibits the production of IFNγ in a pharmacodynamic rat model and is fully efficacious in a rat model of arthritis.

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Tyk2-IN-5 Chemical Structure

Tyk2-IN-5 Chemical Structure

CAS No. : 1797432-62-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 495 In-stock
Solution
10 mM * 1 mL in DMSO USD 495 In-stock
Solid
5 mg USD 450 In-stock
10 mg USD 750 In-stock
25 mg USD 1500 In-stock
50 mg USD 2250 In-stock
100 mg USD 3350 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Tyk2-IN-5 Related Antibodies

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JAK1 JAK2 JAK3 Tyk2 JAK

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Description

Tyk2-IN-5 (compound 6) is a potent, selective and orally active tyrosine kinase 2 (Tyk2) inhibitor that acts on the JH2 structural domain. Tyk2-IN-5 shows a Ki value of 0.086 nM for Tyk2 JH2 and an IC50 value of 25 nM for IFNα. Tyk2-IN-5 efficiently inhibits the production of IFNγ in a pharmacodynamic rat model and is fully efficacious in a rat model of arthritis[1].

IC50 & Target[1]

Tyk2 JH2

0.086 nM (Ki)

IFNα

25 nM (IC50)

In Vitro

Tyk2-IN-5 inhibits Jak1-3 with IC50 values of >2 μM and displays the Jak1-3 dependent cellular activities of >12.5 μM (IC50 values)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Tyk2-IN-5 Related Antibodies
In Vivo

Tyk2-IN-5 (5, 10 mg/kg; p.o.; twice daily for 20 days) shows highly efficacious in a rat adjuvant arthritis model[1].
Tyk2-IN-5 (1, 10 mg/kg; p.o.; single) inhibits IL-12/IL-18 induced IFNγ production in a dose-dependent manner[1].
Tyk2-IN-5 (10 mg/kg; p.o.; single) shows a high oral exposure and bioavailability (114%) in rat[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Lewis male rats (rat adjuvant arthritis model)[1].
Dosage: 5, 10 mg/kg
Administration: Oral administration; twice daily for 20 days
Result: Demonstrated full efficacy to prevent the rats′ paw from swelling.
Animal Model: Lewis male rats (IL-12/IL-18-induced)[1].
Dosage: 1, 10 mg/kg
Administration: Oral administration; single
Result: Inhibited IL-12/IL-18 induced IFNγ production by 45% and 77% at doses of 1 and 10 mg/kg, respectively.
Animal Model: Lewis male rats, mouse[1].
Dosage: 10 mg/kg
Administration: Oral administration; single
Result: 1.19 Pharmacokinetic Parameters of Tyk2-IN-5 in mouse and rat[1].
PO (10 mg/kg)
mouse rat
Cmax (μM) 15 9.4
AUC0-24 (μM•h) 19 57
CL (mL/min/kg) 16 7.8
F (%) 86 114
Molecular Weight

434.43

Formula

C21H19FN8O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C(NC2=NN3C(C(NC)=C2)=NC=C3C(N[C@H]4[C@@H](F)C4)=O)=CC=CN1C5=CC=CC=N5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 43.33 mg/mL (99.74 mM; Need ultrasonic; 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 2.3019 mL 11.5093 mL 23.0187 mL
5 mM 0.4604 mL 2.3019 mL 4.6037 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.17 mg/mL (5.00 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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% 
+
%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3019 mL 11.5093 mL 23.0187 mL 57.5467 mL
5 mM 0.4604 mL 2.3019 mL 4.6037 mL 11.5093 mL
10 mM 0.2302 mL 1.1509 mL 2.3019 mL 5.7547 mL
15 mM 0.1535 mL 0.7673 mL 1.5346 mL 3.8364 mL
20 mM 0.1151 mL 0.5755 mL 1.1509 mL 2.8773 mL
25 mM 0.0921 mL 0.4604 mL 0.9207 mL 2.3019 mL
30 mM 0.0767 mL 0.3836 mL 0.7673 mL 1.9182 mL
40 mM 0.0575 mL 0.2877 mL 0.5755 mL 1.4387 mL
50 mM 0.0460 mL 0.2302 mL 0.4604 mL 1.1509 mL
60 mM 0.0384 mL 0.1918 mL 0.3836 mL 0.9591 mL
80 mM 0.0288 mL 0.1439 mL 0.2877 mL 0.7193 mL
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Tyk2-IN-5 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-51797432-62-2JAKJanus kinasearthritisIFNαIFNγJak1Jak2Jak3IL-12IL-18Inhibitorinhibitorinhibit

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