| Size | Price | Stock | Qty |
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| 5mg |
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| Targets |
Lobaplatin targets DNA by forming highly reactive, charged platinum complexes that bind to nucleophilic groups such as GC- and AG-rich sites in DNA, inducing intrastrand DNA cross-links. It also targets apoptosis pathways including caspase and Bcl-2 family members.
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| ln Vitro |
The antiproliferative effect of lobaplatin (D-19466, 0.25-32 μg/mL; 24-72 hours) is demonstrated against cell lines of esophageal squamous cell carcinoma (ESCC) [1]. Inducing apoptosis in esophageal squamous cell carcinoma (ESCC) and controlling the expression of proteins linked to apoptosis are two of the effects of lobaplatin (0–16 μg/mL; 48 hours) [1]. In a time-dependent way, lobaplatin (1.45 μg/mL; 0-48 hours; SMMC-7721 cells) inhibits the progression of the cell cycle in the G1 and G2/M phases [2]. Lobaplatin (1.45 μg/mL; 0-48 hours; SMMC-7721 cells) inhibits the Rb/E2F complex and upregulates CDK inhibitors in addition to inhibiting the mRNA levels of cyclin B, CDK1, and CDC25C phosphatase [2].
In vitro, lobaplatin (0.25-32 µg/mL; 24-72 h) exhibits anti-proliferative activities against esophageal squamous cell carcinoma (ESCC) cell lines. It arrests the cell cycle at G1 and G2/M phases and induces apoptosis by increasing expressions of caspase and Bax while decreasing expression of Bcl-2. |
| ln Vivo |
In esophageal squamous cell carcinoma (ESCC) xenografts, loplatin (5 and 10 mg/kg; intraperitoneally; once weekly for 3 weeks) suppresses tumor growth [1].
In vivo, lobaplatin has demonstrated anti-tumor activity in various cancer models. It inhibits prostate cancer proliferation and migration through regulation of BCL2 and BAX. It is a promising anti-tumor chemotherapy drug active in patients with multiple tumor types. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for lobaplatin typically involve evaluating its DNA-binding activity using gel electrophoresis or mass spectrometry. The formation of DNA adducts and cross-links is measured after incubation with purified DNA or DNA fragments.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: KYSE-410 cells and EC-109 Cell Tested Concentrations: 0.25, 0.5, 1, 2, 4, 8, 16 and 32 μg/mL Incubation Duration: 24, 48 and 72 hrs (hours) Experimental Results: Inhibition The growth of KYSE-410 and EC-109 cells was dose- and time-dependent. Inhibits the clonogenic activity of KYSE-410 and EC-109 cells in a dose-dependent manner. Apoptosis analysis[1] Cell Types: KYSE-410 cells and EC-109 cells Tested Concentrations: 0.25, 1, 4 and 16 μg/mL Incubation Duration: 48 hrs (hours) Experimental Results: The percentage of apoptotic cells increased in a dose-dependent manner. Western Blot Analysis[1] Cell Types: KYSE-410 cells and EC-109 cells Tested Concentrations: 0, 1, 4 and 16 μg/mL Incubation Duration: 48 hrs (hours) Experimental Results: Increased expression of cleaved-caspase-3, cleaved-caspase-8 , cleave caspase-9 and Bax, while reducing the expression of Bcl-2. Cell cycle analysis [2] Cell Types: SMMC-7721 Cell Tested Concentrations: 1.45 μg/mL Incubation Duration: 0, 24, 36, 48 hrs (hours) Experimental Results: The ratio of G1, S, G2/M phases in the cells was 45.31, For in vitro cell-based assays, lobaplatin is dissolved in water or PBS and applied to cultured cancer cells at concentrations ranging from 0.25-32 µg/mL. Cell viability, apoptosis, and cell cycle distribution are assessed after 24-72 hours of treatment using MTT, flow cytometry, or Western blotting. |
| Animal Protocol |
Animal/Disease Models: Male BALB/c nude mice (4-6 weeks) ESCC xenograft [1]. Dosing once weekly for 3 weeks: 5 and 10 mg/kg
Experimental Results: Inhibition of tumor volume in a dose-dependent manner. Bax expression is increased and Bcl-2 expression is diminished. In vivo animal studies commonly use mouse xenograft models. Lobaplatin is administered intravenously or intraperitoneally at doses ranging from 1-20 mg/kg. Anti-tumor efficacy is evaluated by measuring tumor volume, tumor weight, and histopathological examination of tumor tissues. |
| ADME/Pharmacokinetics |
Lobaplatin is water-soluble (50 mg/mL in H₂O; 125.84 mM). It is a third-generation platinum drug developed as a potential alternative to cisplatin and carboplatin. It is typically stored as a powder at -20°C.
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| Toxicity/Toxicokinetics |
Lobaplatin has a manageable toxicity profile compared to earlier platinum drugs. Common side effects are similar to other platinum-based chemotherapeutics but may be less severe.
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| References |
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| Additional Infomation |
Lobaplatin is a third-generation platinum-based antitumor drug that has been developed for clinical use. It exhibits a unique mechanism of action by forming DNA cross-links that disrupt DNA replication and transcription, leading to apoptosis in cancer cells. It has been used in clinical trials for various cancer types.
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| Molecular Formula |
C9H18N2O3PT
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|---|---|
| Molecular Weight |
397.33
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| Exact Mass |
395.081
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| CAS # |
135558-11-1
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| Appearance |
White to off-white solid powder
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| Boiling Point |
179.5ºC at 760 mmHg
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| Melting Point |
220ºC
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| Flash Point |
75.1ºC
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| Vapour Pressure |
0.937mmHg at 25°C
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| LogP |
0.538
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| Synonyms |
Lobaplatin; D-19466; D19466
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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) |
H2O : ~50 mg/mL (~125.84 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (251.68 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5168 mL | 12.5840 mL | 25.1680 mL | |
| 5 mM | 0.5034 mL | 2.5168 mL | 5.0336 mL | |
| 10 mM | 0.2517 mL | 1.2584 mL | 2.5168 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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