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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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Other Sizes |
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ZAP-180013 is a novel and potent inhibitor of zeta-chain-associated protein kinase 70 (ZAP-70) with an IC50 of 1.8 μM. ZAP-180013 inhibits the interaction of ZAP-70 SH2 domain with immunoreceptor tyrosine-based activation motif (ITAMs).
ln Vitro |
The molecule ZAP-70 plays a crucial role in both T cell activation and signal transduction during T cell acquisition. When T cell acquisition is activated, ZAP-70 is drawn to the intracellular z chain, where it colocalizes with the substrate and becomes activated. ZAP-70 may be used in organ transplant or autoimmune treatments. ZAP-180013 breaks the link between ZAP-70 and T cell receptors; its IC50 values in FP and TR-FRET assays are 9.6 μM and 16.841 μM, respectively [1].
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References |
[1]. Patrick R Visperas, et al. Identification of Inhibitors of the Association of ZAP-70 With the T Cell Receptor by High-Throughput Screen. SLAS Discov. 2017 Mar;22(3):324-331.
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Molecular Formula |
C19H17CL2N3O4S
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Molecular Weight |
454.326981306076
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CAS # |
873080-25-2
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O=C(C1=NC(S(=O)(CC)=O)=NC=C1Cl)N(CC2=CC=C(Cl)C=C2)CC3=CC=CO3
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InChi Key |
GTWKIPDKVRLUKN-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C19H17Cl2N3O4S/c1-2-29(26,27)19-22-10-16(21)17(23-19)18(25)24(12-15-4-3-9-28-15)11-13-5-7-14(20)8-6-13/h3-10H,2,11-12H2,1H3
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Chemical Name |
5-Chloro-N-[(4-chlorophenyl)methyl]-2-(ethylsulfonyl)-N-(2-furanylmethyl)-4-pyrimidinecarboxamide
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Synonyms |
ZAP 180013 ZAP180013 ZAP-180013
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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 : ~250 mg/mL (~550.26 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.58 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.08 mg/mL (4.58 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.58 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.2010 mL | 11.0052 mL | 22.0104 mL | |
5 mM | 0.4402 mL | 2.2010 mL | 4.4021 mL | |
10 mM | 0.2201 mL | 1.1005 mL | 2.2010 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.