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Synonyms: ITK kinase-IN-1

| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 1 mg | $329 | - | In Stock | |
| 5 mg | $787 | - | In Stock | |
| 10 mg | $1,260 | - | In Stock |
| Description | Modzatinib (ITKkinase-IN-1) (compound I) is an inhibitor targeting ITK kinase with an IC50 of 8 nM in Jurkat cells, useful for researching inflammatory diseases. Modzatinib (ITKkinase-IN-1) (compound I) inhibits JAK3 in hPBMC cells with an IC50 of 23 nM (based on IL-2/pSTAT5 levels) and shows no inhibitory effect on JAK2. Modzatinib (ITKkinase-IN-1) (compound I) is therefore applied in immunological signaling research to study T-cell receptor–associated kinase pathways, JAK/STAT signaling selectivity, and cytokine response modulation in primary immune cell systems. |
| Targets & IC50 | JAK3:23 nM, ITK:8 nM |
| In vitro | Methods:Whole blood was treated with modzatinib at concentrations of 0.01–1000 ng/mL for 2–18 hours, and its effects on related signaling pathways and gene expression were detected. Results:Modzatinib inhibited aCD3/CD28-induced mRNA expression of IL2 and IFNγ, as well as IL15-mediated activation of pSTAT5 [1]. |
| In vivo | Methods:Rat adjuvant-induced arthritis (AIA) model and mouse T cell transfer colitis model were established. Modzatinib was administered continuously via different routes, and changes in inflammation-related indicators were observed. Results: 1.In rat AIA model, intragastric administration of Modzatinib at 5–15 mg/kg twice daily for 14 consecutive days alleviated ankle swelling in a dose-dependent manner. 2.In mouse T cell transfer colitis model, dietary administration of the compound at 100–300 ppm once daily for 35 consecutive days ameliorated inflammatory lesions in colon and ileum dose-dependently [1]. |
| Synonyms | ITK kinase-IN-1 |
| Molecular Weight | 361.39 |
| Formula | C18H21F2N5O |
| Cas No. | 2411407-25-3 |
| Smiles | N(C1=C2C(=CNC2=NC=N1)[C@@H]3C(F)(F)C3)[C@H]4CN(C(C=C)=O)[C@@H](C)CC4 |
| Storage | Keep away from moisture,Keep away from direct sunlight,Store at low temperature,Store under nitrogen Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||
| Solubility Information | DMSO: 4.5 mg/mL (12.45 mM), Sonication is recommended. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | |||||||||||||||||||||
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 µL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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