Cat. No.: HY-111745

Tyk2-IN-5

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

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 K_i 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.

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

Purity: 99.35%
CAS No.: 1797432-62-2
Formula: C₂₁H₁₉FN₈O₂
Molecular Weight:434.43

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Tyk2-IN-5 Chemical Structure

CAS No.: 1797432-62-2

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

Tyk2 JH2

0.086 nM (Ki)

IFNα

25 nM (IC₅₀)

All JAK Isoforms :

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.

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

C_max (μM) 15 9.4

AUC_0-24 (μM•h) 19 57

CL (mL/min/kg) 16 7.8

F (%) 86 114

Chemical Information

CAS No. 1797432-62-2
Appearance Solid
Molecular Weight 434.43
Formula C₂₁H₁₉FN₈O₂
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

Publications (1)

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Journal Impact Factor

J Ethnopharmacol

"Shihu" promote T-cell immunity against breast cancer through bioactive constituent THMB enhancing JAK3-STAT1 signal. [Abstract]

2026 Oct 28:369:121888. PMID: 42202911

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3019 mL

11.5093 mL

23.0187 mL

5 mM

0.4604 mL

2.3019 mL

4.6037 mL

10 mM

0.2302 mL

1.1509 mL

2.3019 mL

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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Liu C, et al. Identification of Imidazo[1,2-b]pyridazine Derivatives as Potent, Selective, and Orally Active Tyk2 JH2 Inhibitors. ACS Med Chem Lett. 2019 Feb 21;10(3):383-388. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

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Product Name:
CAS No.:
Species:
Purity:
Quantity:

	PO (10 mg/kg)
	mouse	rat
C_max (μM)	15	9.4
AUC_0-24 (μM•h)	19	57
CL (mL/min/kg)	16	7.8
F (%)	86	114

Tyk2-IN-5

Bioactive Compound Library Max

Bioactive Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Pyroptosis Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Obesity Compound Library

Targeted Diversity Library

Anti-Liver Cancer Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Autoimmune Disease Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Tyk2-IN-5

All JAK Isoforms

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Tyk2-IN-5 Related Classifications

HY-111745 Related Classifications