| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
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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].
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| 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].
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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, |
| 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. |
| References |
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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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