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| Targets |
Inhibitor of apoptosis proteins (IAPs). UC-112 is a novel IAP inhibitor that potently inhibits cancer cell growth. The compound inhibits X chromosome-linked IAP (XIAP) and reduces survivin levels. It also inhibits P-glycoprotein function. IAPs are negative regulators of apoptosis that are often overexpressed in cancer cells.
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| ln Vitro |
UC-112 demonstrates strong inhibitory activity against cell growth in various cancer cell lines including human melanoma (A375 and M14) and prostate (PC-3 and DU145) cancer cells, with IC50 values ranging from 0.7 to 3.4 μM. The compound also potently inhibits the growth of P-glycoprotein-expressing cells. As an IAP inhibitor, it promotes apoptosis in cancer cells by neutralizing the anti-apoptotic function of IAP proteins. The compound shows broad anti-cancer activity across multiple cell lines.
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| ln Vivo |
UC-112 strongly inhibits tumor growth in an A375 human melanoma xenograft model in vivo. Treatment with UC-112 reduces both X chromosome-linked IAP (XIAP) and survivin levels in tumors. The compound's IAP inhibitory activity translates to in vivo anti-tumor efficacy. The compound's ability to inhibit P-glycoprotein suggests potential for overcoming multi-drug resistance. Detailed dosing, administration route, and treatment schedules are limited in publicly available sources.
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| Enzyme Assay |
IAP binding assays are performed using recombinant IAP proteins (XIAP, cIAP1, cIAP2) and fluorescently labeled peptide substrates representing the Smac/DIABLO binding motif. The assay measures the displacement of the labeled peptide by test compounds, with fluorescence polarization used to quantify binding affinity. Compounds are serially diluted in assay buffer (50 mM HEPES pH 7.5, 150 mM NaCl, 0.1% BSA, 0.01% Triton X-100) and incubated with IAP protein and labeled peptide for 1-2 hours at room temperature. IC50 values are determined by non-linear regression analysis. Each concentration is tested in duplicate or triplicate with appropriate positive and negative controls.
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| Cell Assay |
Cellular activity is evaluated in cancer cell lines including A375 (melanoma), M14 (melanoma), PC-3 (prostate), and DU145 (prostate). Cells are cultured in DMEM or RPMI-1640 with 10% FBS at 37°C in 5% CO2. Cells are seeded in 96-well plates and treated with UC-112 at various concentrations (0.1-100 μM) for 24-72 hours. Cell viability is assessed using MTT, CCK-8, or CellTiter-Glo assays. Apoptosis is evaluated by Annexin V/PI staining, caspase-3/7 activity assays, and Western blotting for PARP cleavage and IAP protein levels (XIAP, survivin). P-glycoprotein function is assessed using fluorescent substrate accumulation assays. Each experiment includes DMSO vehicle controls and known IAP inhibitors as positive controls.
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| Animal Protocol |
In vivo efficacy is evaluated in mouse xenograft models using A375 human melanoma cells. Tumor cells are implanted subcutaneously in immunodeficient mice. UC-112 is administered via intraperitoneal injection or oral gavage at doses determined by preclinical studies. Tumor growth is monitored by caliper measurements. At study endpoint, tumors are harvested for histopathological analysis and biochemical assays including Western blotting for XIAP and survivin levels. Body weight and clinical signs are monitored throughout the study. Sample sizes typically range from 6-10 animals per group.
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| ADME/Pharmacokinetics |
Limited PK data are available. UC-112 has a molecular weight of 348.44 g/mol. Solubility: soluble in DMSO (33.33 mg/mL with sonication). Storage: powder at -20°C for up to 3 years; 4°C for up to 2 years. Appearance: solid. Purity: typically >98%. Bioavailability, half-life, and tissue distribution data are not publicly available. The compound is a research tool for studying IAP biology and cancer therapeutics.
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| Toxicity/Toxicokinetics |
Limited toxicology data are available for UC-112. As an IAP inhibitor that promotes apoptosis, potential toxicities may include effects on normal tissues with high turnover rates. Standard toxicology studies would include acute and subchronic toxicity in rodents, genotoxicity screening, and evaluation of effects on hematopoiesis and immune function. No clinical trials have been reported for this compound. The compound is intended for research use only.
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| References |
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| Additional Infomation |
5-(benzoxymethyl)-7-(1-pyrrolidinylmethyl)-8-quinolinol is a hydroxyquinoline.
UC-112 is a novel and potent IAP inhibitor. It demonstrates strong inhibitory activity against human melanoma (A375 and M14) and prostate (PC-3 and DU145) cancer cells with IC50 values of 0.7-3.4 μM. The compound also inhibits P-glycoprotein. In vivo, it reduces XIAP and survivin levels in A375 xenografts. The compound is also known as 5-((benzyloxy)methyl)-7-(pyrrolidin-1-ylmethyl)quinolin-8-ol. No clinical trials or regulatory approvals have been reported. |
| Molecular Formula |
C22H24N2O2
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|---|---|
| Molecular Weight |
348.44
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| Exact Mass |
348.184
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| CAS # |
383392-66-3
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| PubChem CID |
3426979
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| Appearance |
White to off-white solid powder
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| LogP |
4.19
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
26
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| Complexity |
420
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CCN(C1)CC2=CC(=C3C=CC=NC3=C2O)COCC4=CC=CC=C4
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| InChi Key |
LTGLGIQQZXSLLF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H24N2O2/c25-22-18(14-24-11-4-5-12-24)13-19(20-9-6-10-23-21(20)22)16-26-15-17-7-2-1-3-8-17/h1-3,6-10,13,25H,4-5,11-12,14-16H2
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| Chemical Name |
5-(phenylmethoxymethyl)-7-(pyrrolidin-1-ylmethyl)quinolin-8-ol
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| Synonyms |
UC112; UC 112; UC-112
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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 : ~33.33 mg/mL (~95.65 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.17 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 25.0 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: 2.5 mg/mL (7.17 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 25.0 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: ≥ 2.5 mg/mL (7.17 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 | 2.8699 mL | 14.3497 mL | 28.6993 mL | |
| 5 mM | 0.5740 mL | 2.8699 mL | 5.7399 mL | |
| 10 mM | 0.2870 mL | 1.4350 mL | 2.8699 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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