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| ln Vitro |
ITK-IN-6 (compound C-161) (24 hours) inhibited the transcriptional activity downstream of ITK in the Jurkat-NFAT-Luc stable cell line with an inhibition rate of 62.27% [1]. ITK-IN-6 (0.07-5 μM, 12 hours) showed good safety for CD4+ T cells at effective doses and could attenuate the differentiation of Th2 and Th17 cells in vitro [1]. ITK-IN-6 (0.15-2.5 μM, 12 hours) blocked key factors for T cell activation and inhibited the expression of activation markers on the surface of T cells in Jurkat cells [1]. ITK-IN-6 (0.625-2.5 μM, 12 hours) specifically inhibited ITK in Jurkat T cells, blocked the cellular and molecular activation potential of proximal T cell receptor signals, and significantly inhibited the expression of CD69 [1]. ITK-IN-6 (0.15–2.5 μM) inhibited IL-2 transcription and protein expression in a dose-dependent manner, with an IC50 of 494 nM in Jurkat cells [1]. Treatment of Jurkat cells with ITK-IN-6 (0.625–2.5 μM, 30 min) significantly reduced anti-CD3-induced intracellular Ca2+ flux [1].
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| ln Vivo |
ITK-IN-6 (compound C-161) (10 mg/kg, intraperitoneal injection, once daily for 7 to 11 days) significantly reduced airway inflammation in C57BL/6J mice induced by house dust mite (HDM) by inhibiting Th2/Th17 differentiation and cytokine production, and had good safety [1].
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| Cell Assay |
Western Blot Analysis [1]
Cell Types: Jurkat T cells Tested Concentrations: 0.625 μM, 1.25 μM, 2.5 μM Incubation Duration: 12 hours Experimental Results: C-161 inhibited the phosphorylation of p-PLCγ1, p-IκBα, p-NF-κB and p-ERK in a dose-dependent manner, while the phosphorylation of upstream ZAP70 remained unchanged. |
| Animal Protocol |
Animal/Disease Models:C57BL/6J mouse model of asthma induced by house dust mite (6-8 weeks old, 18-20 g) [1]
Doses: 10 mg/kg Route of Administration: Intraperitoneal injection (ip) once daily 7 to 11 days after house dust mite sensitization, 1 hour before house dust mite challenge. Experimental Results: Reduced the total number of inflammatory cells, eosinophils (EOS), neutrophils (NEU) and B cells in bronchoalveolar lavage fluid (BALF), alleviated inflammatory infiltration and mucus secretion in lung tissue, and reduced serum total IgE and house dust mite-specific IgE levels. Decreased CD3⁺ T cell infiltration in lung tissue, reduced proportion and number of CD4⁺ T cells in lung tissue, and downregulated mRNA and protein levels of Th2/Th17-related cytokines (IL-4/IL-5/IL-13/IL-17A) in lung tissue. No weight loss or death was caused in mice, nor were any abnormalities observed in organ parameters, serum biochemical parameters, or histopathological findings. |
| References |
| Molecular Formula |
C20H16CL2N2O4S
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|---|---|
| Molecular Weight |
451.32
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| CAS # |
2616666-32-9
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| Appearance |
Off-white to gray solid
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| SMILES |
OC1=C(NS(=O)(C)=O)C=C(NC(C2=CC=C(C3=C(Cl)C(Cl)=CC=C3)C=C2)=O)C=C1
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~221.57 mM; with sonication)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.54 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you canAdd 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD saline (4°C, store for one week): Dissolve 2 g of SBE-β-CD powder in 10 mL of saline until completely dissolved and clear. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.54 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you canAdd 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2157 mL | 11.0786 mL | 22.1572 mL | |
| 5 mM | 0.4431 mL | 2.2157 mL | 4.4314 mL | |
| 10 mM | 0.2216 mL | 1.1079 mL | 2.2157 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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