| Size | Price | Stock | Qty |
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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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| Targets |
SARS-CoV M pro(Ki= 0.1 nM)
XP-59 targets multiple molecular targets depending on the context. It is reported to inhibit the SARS-CoV Mpro (main protease), an enzyme essential for viral replication. It is also described as a nucleoside analog that inhibits viral DNA polymerase and reverse transcription. Furthermore, XP-59 targets the c-Myc oncoprotein, a key driver of tumorigenesis. Its diverse reported targets suggest it may be a versatile tool for studying viral and cancer biology. |
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| ln Vitro |
Because it is essential to the creation of the viral replicase/transcriptase complex, the SARS-CoV main proteinase (Mpro) is a prime candidate for therapeutic development[1].
XP-59 exhibits potent in vitro activity as a SARS-CoV Mpro inhibitor with a Ki of 0.1 μM. As a nucleoside analog, it is used to study viral DNA polymerase and reverse transcription suppression. Preclinical studies indicate that XP-59 can inhibit tumor growth in a variety of cancer models by targeting the c-Myc oncoprotein. These in vitro activities confirm its potential as a research tool for antiviral and anticancer studies. |
| ln Vivo |
In vivo, XP-59 has demonstrated preclinical activity in cancer models. As a c-Myc inhibitor, it can inhibit tumor growth in a variety of cancer models. Its activity against SARS-CoV Mpro suggests potential antiviral efficacy, though in vivo data are limited. The compound's ability to target multiple pathways makes it a valuable tool for studying both viral infections and cancer.
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| Enzyme Assay |
In vitro enzyme assays for XP-59 involve measuring its inhibition of SARS-CoV Mpro activity. These assays use recombinant Mpro and a fluorogenic peptide substrate. The enzyme is incubated with the substrate and varying concentrations of XP-59, and the decrease in fluorescence is measured to determine the Ki (0.1 μM). For its role as a nucleoside analog, assays measuring viral polymerase or reverse transcriptase activity are used.
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| Cell Assay |
In vitro cellular assays for XP-59 are conducted in cancer cell lines to assess its c-Myc inhibitory activity. Cells are treated with the compound at various concentrations, and cell proliferation is measured using MTT or CellTiter-Glo assays. c-Myc target gene expression is assessed by qPCR. Apoptosis is evaluated by measuring caspase activity or Annexin V staining. For antiviral studies, cells infected with SARS-CoV are treated with XP-59, and viral replication is measured.
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| Animal Protocol |
In vivo animal experiments with XP-59 are conducted in mouse xenograft models of cancer. Tumor-bearing mice are administered XP-59 at various doses. Tumor growth is monitored, and tumor tissues are harvested for analysis of c-Myc target gene expression and apoptosis markers. For antiviral studies, animal models of SARS-CoV infection could be used to assess viral load and survival.
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| ADME/Pharmacokinetics |
XP-59 has a molecular weight of 282.30 and a molecular formula of C15H14N4O2. It is soluble in DMSO at ≥35 mg/mL. The compound is typically stored as a powder at -20°C (3 years) or 4°C (2 years), and in solution at -80°C (6 months) or -20°C (1 month). Its half-life and bioavailability have not been extensively characterized.
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| Toxicity/Toxicokinetics |
Comprehensive toxicological data for XP-59 are limited. The compound is intended for research use only and is not approved for human therapeutic use. Standard laboratory safety precautions should be followed when handling this compound. Further toxicity studies would be required to support any potential clinical development.
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| References | |
| Additional Infomation |
XP-59 is a small molecule inhibitor with reported activity against SARS-CoV Mpro (Ki = 0.1 μM), viral polymerases, and the c-Myc oncoprotein. It has shown preclinical antitumor activity in various cancer models. The compound is also known as a nucleoside analog for studying reverse transcription and is used in drug resistance profiling.
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| Molecular Formula |
C15H14N4O2
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|---|---|
| Molecular Weight |
282.29726266861
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| Exact Mass |
282.11
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| Elemental Analysis |
C, 63.82; H, 5.00; N, 19.85; O, 11.33
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| CAS # |
890402-73-0
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| PubChem CID |
15959236
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| Appearance |
Solid powder
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| LogP |
3.1
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
21
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| Complexity |
369
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN(C)C1=CC=C(C=C1)C(=O)ON2C3=CC=CC=C3N=N2
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| InChi Key |
UOITWBIZHQLMTH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H14N4O2/c1-18(2)12-9-7-11(8-10-12)15(20)21-19-14-6-4-3-5-13(14)16-17-19/h3-10H,1-2H3
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| Chemical Name |
1H-benzo[d][1,2,3]triazol-1-yl 4-(dimethylamino)benzoate
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| Synonyms |
XP-59; XP 59; XP59;
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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 : ~62.5 mg/mL (~221.40 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 6.25 mg/mL (22.14 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 62.5 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: ≥ 6.25 mg/mL (22.14 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 can add 100 μL of 62.5 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: ≥ 6.25 mg/mL (22.14 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 | 3.5423 mL | 17.7117 mL | 35.4233 mL | |
| 5 mM | 0.7085 mL | 3.5423 mL | 7.0847 mL | |
| 10 mM | 0.3542 mL | 1.7712 mL | 3.5423 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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