| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| ln Vitro |
Suspended in LPD (mireplatin/LPD, 100 μg/mL), mireplatin (SM-11355) can cause apoptosis, form platinum-DNA adducts, and stop the growth of AH109A cells [2].
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| ln Vivo |
In rats with AH109A tumor cells, the dose-dependent reduction of tumor growth rate is shown with meplatin (SM-11355) in lipiodol (0.02-0.4 mg/20 μL) [1]. Rats harboring AH109A cells showed a substantial reduction in tumor growth when treated with mireplatin/LPD (400 μg/head) [2].
In a slowly-growing rat hepatic tumor model (AH109A cells transplanted into the liver), intra-hepatic arterial administration of SM-11355 suspended in Lipiodol (SM-11355/Lipiodol) showed significant antitumor effects. Tumor growth rates one week after administration of 20 µl Lipiodol containing 0.02, 0.04, 0.1, 0.2, or 0.4 mg of SM-11355 were 86%, 110%, 81%, 51%, and 40%, respectively, compared to 244% for the Lipiodol-only control. Massive necrosis was observed in tumors treated with 0.2 and 0.4 mg doses at one week. Four weeks after administration, tumors in groups treated with 0.2 mg and 0.4 mg of SM-11355/Lipiodol had almost disappeared, with scar tissue observed at the tumor site. The tumor treated with 0.1 mg did not grow from day 0 to week 4. The antitumor effect of 0.2 mg SM-11355/Lipiodol was comparable to that of 0.4 mg CDDP/Lipiodol. [1] |
| Animal Protocol |
A slowly-growing hepatic tumor model was established in Donryu male rats by successive transplantation of AH109A ascites hepatoma cells into the liver parenchyma. Approximately twenty days after tumor implantation, when the tumor size reached about 5-20 mm in its major axis, the drug was administered. Under laparotomy and anesthesia, a catheter was inserted into the gastroduodenal artery and advanced to the branching point of the common and proper hepatic arteries. A volume of 20 µl of SM-11355 suspended in Lipiodol (preparation method: mixing SM-11355 with Lipiodol to form a stable colloidal suspension) was injected into the proper hepatic artery via the catheter. Tumor size (major and minor axes) was measured on the day of administration (day 0), and at 1 week and 4 weeks post-administration to evaluate antitumor effects. [1]
For hepatic toxicity evaluation, the same intra-hepatic arterial administration procedure was performed on normal rats (without tumors). Blood samples were collected one day after drug administration, and serum GOT and GPT levels were measured using a commercial test kit. [1] |
| ADME/Pharmacokinetics |
This article describes SM-11355/Lipiodol as a stable colloidal suspension and sustained-release formulation. Studies have shown that the active platinum compound in SM-11355/Lipiodol is released more slowly than that in CDDP/Lipiodol, thus prolonging its localization time in tumor vessels and the extracapillary space of tumor tissue. Specific pharmacokinetic parameters (e.g., half-life, AUC) of SM-11355 are not provided in this article. [1]
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| Toxicity/Toxicokinetics |
The method for assessing hepatotoxicity was as follows: serum aspartate aminotransferase (GOT) and alanine aminotransferase (GPT) levels were measured one day after intrahepatic artery administration. The minimum doses at which SM-11355/iodized oil caused a significant increase in serum GOT and GPT levels compared to iodized oil alone were 0.2 mg (GPT) and 0.4 mg (GOT), respectively. At a dose of 0.1 mg, SM-11355/iodized oil inhibited tumor growth for up to 4 weeks without showing significant hepatotoxicity. During the above 48-hour observation period, no deaths or other significant toxic symptoms were reported in any of the tested dose groups. [1]
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| References |
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| Additional Infomation |
SM-11355 is a lipophilic platinum complex, specifically named cis-[(1R,2R)-1,2-cyclohexanediamine-N,N']bis(myristate)]platinum(II). It was originally developed for hepatic artery chemotherapy, using iodized oil as a carrier. Its main feature is that it can form a stable colloidal suspension in iodized oil, thereby achieving sustained release, unlike the unstable suspension of water-soluble cisplatin (CDDP) in iodized oil. [1] The study concluded that in this rat model, SM-11355/iodized oil had higher antitumor activity and lower hepatotoxicity than CDDP/iodized oil. The article noted that SM-11355 was undergoing clinical trials at the time of publication. [1]
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| Molecular Formula |
2[C14H27O2-].C6H14N2.PT+4
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|---|---|
| Molecular Weight |
763.992720000001
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| Exact Mass |
763.482
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| CAS # |
141977-79-9
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| Related CAS # |
Miriplatin (hydrate);250159-48-9
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| PubChem CID |
9832045
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| Appearance |
White to off-white solid powder
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| LogP |
8.487
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
22
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| Heavy Atom Count |
41
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| Complexity |
212
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| Defined Atom Stereocenter Count |
2
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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) |
Acetone :< 1 mg/mL
DMF :< 1 mg/mL H2O : < 0.1 mg/mL |
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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 | 1.3089 mL | 6.5446 mL | 13.0892 mL | |
| 5 mM | 0.2618 mL | 1.3089 mL | 2.6178 mL | |
| 10 mM | 0.1309 mL | 0.6545 mL | 1.3089 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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