| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
IC50: 14.6 nM (ZAP-70)[1]
RDN2150 TFA targets ZAP-70 (zeta-chain-associated protein kinase 70), a tyrosine kinase that plays a critical role in T cell receptor (TCR) signaling. ZAP-70 is essential for T cell activation and function. By covalently binding to the C346 residue of ZAP-70 with an IC50 of 14.6 nM, RDN2150 TFA irreversibly inhibits ZAP-70 kinase activity, thereby suppressing TCR signaling and T cell activation. |
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| ln Vitro |
RDN2150 TFA shows potent in vitro activity as a ZAP-70 inhibitor with an IC50 of 14.6 nM. The compound covalently binds to the C346 residue of ZAP-70, resulting in irreversible inhibition. RDN2150 TFA inhibits the expression of CD25 and CD69, which are activation markers on T cells, and inhibits CD4+ T cell activation.
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| ln Vivo |
In vivo activity of RDN2150 TFA has been suggested for research applications in psoriasis. By inhibiting ZAP-70 and suppressing T cell activation, the compound has the potential to modulate immune responses in autoimmune and inflammatory diseases. However, detailed in vivo efficacy data have not been extensively reported in the available literature.
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| Enzyme Assay |
Non-cell-based kinase assays for RDN2150 TFA typically involve measuring the inhibition of recombinant ZAP-70 kinase activity using a radioactive or fluorescence-based assay. A standard protocol includes incubating purified ZAP-70 kinase with a peptide substrate and ATP in kinase buffer. RDN2150 TFA is added at various concentrations (0.001–100 nM), and the phosphorylation of the substrate is measured. IC50 values are calculated from dose-response curves.
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| Cell Assay |
Cellular assays for RDN2150 TFA typically involve primary human CD4+ T cells or T cell lines. A representative protocol includes isolating CD4+ T cells from peripheral blood, activating them with anti-CD3/anti-CD28 antibodies, treating with RDN2150 TFA at various concentrations (0.01–1000 nM) for 24–72 hours, and measuring activation markers CD25 and CD69 by flow cytometry. Inhibition of T cell proliferation is assessed by CFSE dilution or BrdU incorporation.
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| Animal Protocol |
In vivo animal studies with RDN2150 TFA have not been extensively reported in the available literature. If conducted, a typical protocol would involve mouse models of psoriasis (e.g., imiquimod-induced or IL-23-induced models), with administration of the compound via oral gavage or intraperitoneal injection, followed by assessment of skin inflammation, cytokine levels, and histopathological analysis.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of RDN2150 TFA have not been extensively reported in the available literature. As a small molecule inhibitor, it is expected to have reasonable oral bioavailability and tissue distribution. The compound is typically stored as a powder at -20°C. Further PK studies are needed to fully characterize its absorption, distribution, metabolism, and excretion profile.
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| Toxicity/Toxicokinetics |
As a research compound, RDN2150 TFA is not intended for human therapeutic use, and comprehensive toxicological data are limited to preclinical studies. Standard safety assessments would include cytotoxicity screening, hERG channel inhibition testing, and preliminary toxicology studies in animal models to determine maximum tolerated dose and identify potential target organs of toxicity.
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| References | |
| Additional Infomation |
RDN2150 TFA (Compound 25) is a potent ZAP-70 inhibitor with an IC50 of 14.6 nM that covalently binds to the C346 residue of ZAP-70. The compound inhibits CD25 and CD69 expression and CD4+ T cell activation, and can be used for the research of psoriasis. RDN2150 TFA is available as a research reagent for immunology and inflammatory disease studies.
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| Molecular Formula |
C30H30CLF3N8O6
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|---|---|
| Molecular Weight |
691.06
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| Appearance |
White to light yellow solid powder
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 :~125 mg/mL (~180.88 mM; with sonication)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.4471 mL | 7.2353 mL | 14.4705 mL | |
| 5 mM | 0.2894 mL | 1.4471 mL | 2.8941 mL | |
| 10 mM | 0.1447 mL | 0.7235 mL | 1.4471 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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