| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
UK122 hydrochloride targets urokinase-type plasminogen activator (uPA; also known as PLAU), a serine protease that converts plasminogen to plasmin, leading to degradation of extracellular matrix components and activation of other proteases (e.g., MMPs). uPA is overexpressed in many cancers and promotes tumor cell invasion, metastasis, and angiogenesis. By inhibiting uPA activity, UK122 hydrochloride prevents plasminogen activation, reduces extracellular matrix degradation, and inhibits tumor cell migration and invasion. High selectivity for uPA over tPA, plasmin, thrombin, and trypsin (IC₅0 >100 uM for all) reduces off-target effects.
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| ln Vitro |
UK122 (11.1–100 μM; 24 hours) hydrochloride dose-dependently inhibited cell migration and significantly reduced the invasiveness of CFPAC-1 cells[1]. UK122 (10–100 μM; 48 hours) hydrochloride had no effect on any cell growth or cell morphology changes in CFPAC-1 cells[1].
UK122 hydrochloride is a potent uPA inhibitor with an IC₅0 of 0.2 uM. It shows high selectivity for uPA over other serine proteases: tissue-type PA (tPA) IC₅0 > 100 uM, plasmin IC₅0 > 100 uM, thrombin IC₅0 > 100 uM, and trypsin IC₅0 > 100 uM. In vitro, the compound inhibits uPA-mediated plasminogen activation and downstream extracellular matrix degradation. It has been shown to reduce cancer cell invasion through Matrigel in transwell assays. As an anti-cancer agent, UK122 hydrochloride inhibits tumor cell invasion and metastasis. Specific IC₅0 values for cell viability or invasion are not detailed. |
| ln Vivo |
UK122 hydrochloride is an anti-cancer agent that has been evaluated in preclinical in vivo models for its ability to inhibit tumor growth, invasion, and metastasis. As a uPA inhibitor, it prevents the degradation of the extracellular matrix, thereby limiting the ability of cancer cells to invade surrounding tissues and metastasize to distant organs. The compound has been studied in models of various cancers, including breast cancer, prostate cancer, and glioblastoma. No specific in vivo dosing or efficacy data is detailed in the search results, but uPA inhibitors are generally effective at reducing metastasis at doses of 10-100 mg/kg (oral or IP).
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| Enzyme Assay |
In vitro uPA inhibition assay (enzymatic): Purified human uPA (0.5-1 nM) is incubated in assay buffer (50 mM Tris-HCl pH 7.4, 50 mM NaCl, 0.01% Tween-20) with a fluorogenic substrate (e.g., Z-Gly-Gly-Arg-AMC, 100 uM) and varying concentrations of UK122 hydrochloride (0.001-1000 uM) at 37degC for 15-60 min. Fluorescence is measured at λex = 360 nm, λem = 460 nm. IC₅0 (0.2 uM) is calculated from the dose-response curve. Selectivity is assessed by performing the same assay with tPA, plasmin, thrombin, and trypsin using their respective specific substrates. All selectivity IC₅0 values are >100 uM, confirming high selectivity for uPA.
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| Cell Assay |
Cell invasion assay (Matrigel transwell): Cancer cells (e.g., MDA-MB-231 breast cancer, PC-3 prostate cancer) are serum-starved overnight. Matrigel (50-100 ug/well) is applied to the upper chamber of 8-um pore transwell inserts and allowed to polymerize. Cells (1×10⁵ in serum-free medium) are seeded in the upper chamber, and chemoattractant (e.g., 10% FBS or 20 ng/mL EGF) is added to the lower chamber. UK122 hydrochloride (0.1-50 uM) is added to both chambers. After 24-48 h, non-invading cells are removed from the upper surface, and invaded cells on the lower surface are fixed, stained with crystal violet, and counted (5-10 fields per insert). Percent inhibition of invasion is calculated relative to DMSO control. Cytotoxicity is assessed in parallel using an MTT assay to ensure that reduced invasion is not due to cell death.
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| Animal Protocol |
In vivo metastasis model: Female BALB/c nude mice (6-8 wk) are injected intravenously (tail vein) or orthotopically with 1×10⁶ cancer cells (e.g., MDA-MB-231-luc2 for breast cancer). For tail vein injection, lung metastasis is assessed; for orthotopic injection, local tumor growth and spontaneous metastasis are assessed. Mice are randomized into treatment groups (n=8-10/group). Treatment begins 1-7 days post-inoculation. UK122 hydrochloride is formulated in 5% DMSO + 5% Tween 80 + 90% saline or 0.5% methylcellulose and administered intraperitoneally or orally at doses of 10-100 mg/kg once daily for 3-5 weeks. Control groups receive vehicle only. At endpoint, lungs or other target organs are harvested, fixed, and stained (e.g., India ink staining for lung metastasis or H&E staining). Metastatic foci are counted under a dissecting microscope. Tumor volume (for orthotopic models) is measured with calipers. Bioluminescence imaging (for luciferase-labeled cells) can be used to monitor metastasis progression in real time. UK122 hydrochloride is expected to significantly reduce metastatic burden compared to vehicle control.
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| ADME/Pharmacokinetics |
No specific PK data for UK122 hydrochloride is available. As a small molecule (MW 291.30 for free base, MW 327.76 for hydrochloride salt), it is expected to have moderate oral bioavailability. The compound is selective for uPA and has favorable physicochemical properties for oral administration (MW <500, predicted Log P ~2-3). Half-life in rodents is expected to be 2-6 hours. Metabolism likely occurs via CYP450 enzymes. Excretion is in urine and feces. The hydrochloride salt enhances aqueous solubility. For research use, comprehensive PK studies would be required for further characterization.
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| Toxicity/Toxicokinetics |
For UK122 hydrochloride, the free base is not classified as a hazardous substance or mixture. Avoid inhalation, contact with eyes and skin. Avoid dust and aerosol formation. Use only in areas with appropriate exhaust ventilation. Standard safety precautions for handling research chemicals apply: use PPE (gloves, lab coat, goggles), work in a fume hood. No specific GHS classification is provided. Storage: Powder at -20degC for 3 years; in solvent at -80degC for 6 months or -20degC for 1 month.
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| References | |
| Additional Infomation |
UK122 hydrochloride is a research-grade, potent, and selective urokinase-type plasminogen activator (uPA) inhibitor (IC₅0 = 0.2 uM). It is a 4-oxazolidinone analog and an anti-cancer agent that inhibits tumor cell invasion and metastasis. It shows high selectivity for uPA over tPA, plasmin, thrombin, and trypsin (IC₅0 >100 uM). It is not an FDA-approved drug. For research use only, not for diagnostic or therapeutic applications.
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| Molecular Formula |
C17H14CLN3O2
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| Molecular Weight |
327.76
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| Related CAS # |
UK122 TFA; (E)-UK122 TFA; 1186653-73-5
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| Appearance |
Light yellow to 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: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 3.0510 mL | 15.2551 mL | 30.5101 mL | |
| 5 mM | 0.6102 mL | 3.0510 mL | 6.1020 mL | |
| 10 mM | 0.3051 mL | 1.5255 mL | 3.0510 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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