| Size | Price | Stock | Qty |
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| 100mg |
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| 1g | |||
| Other Sizes |
| Targets |
Miriplatin targets DNA through the formation of platinum-DNA adducts. As a platinum-based alkylating agent, miriplatin forms covalent crosslinks with DNA, primarily at N7 positions of guanine bases. These DNA adducts interfere with DNA replication and transcription, leading to cell cycle arrest and apoptosis. Miriplatin is a lipophilic platinum complex containing myristates as leaving groups. When suspended in Lipiodol, the compound is selectively delivered to the liver and gradually releases active platinum compounds in tumor tissue. The lipophilic nature of miriplatin allows for selective retention in tumor tissues, enhancing its therapeutic efficacy while minimizing systemic toxicity. The compound's mechanism of action is similar to other platinum-based drugs such as cisplatin, but its unique formulation provides targeted delivery to liver tumors.
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| ln Vitro |
When suspended in lipiodol, mireplatin (Mireplatin/LPD, 100 μg/mL) slows the development of AH109A cells, generates platinum-DNA adducts, and triggers apoptosis [2].
In vitro, miriplatin demonstrates potent anticancer activity against hepatocellular carcinoma cells. When suspended in Lipiodol, miriplatin (100 μg/mL) slows the development of AH109A cells, produces platinum-DNA adducts, and triggers apoptosis. In cellular assays, miriplatin's effects on cancer cell proliferation, apoptosis, and DNA damage can be assessed. The compound forms platinum-DNA adducts, which can be measured by atomic absorption spectroscopy or immunoassays. Miriplatin's in vitro activity against HCC cells supports its use in TACE for the treatment of hepatocellular carcinoma. The compound's less severe toxicity profile compared to other platinum anticancer agents is an advantage. |
| ln Vivo |
In rats harboring AH109A tumor cells, the dose-dependent reduction of tumor growth rate is achieved by mereplatin 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 vivo, miriplatin demonstrates efficacy in the treatment of hepatocellular carcinoma. The compound is used in TACE, where it is suspended in Lipiodol and injected into the hepatic artery, allowing for selective delivery to liver tumors. Miriplatin is selectively delivered to the liver; platinum and radioactive components are gradually released into systemic circulation and excreted into urine. In dogs with renal impairment, the compound's pharmacokinetics have been studied. Miriplatin has a less severe toxicity profile compared to other platinum anticancer agents. The compound's unique formulation allows for selective retention in tumor tissues, enhancing its therapeutic efficacy while minimizing systemic toxicity. Miriplatin has been approved for use in Japan for the treatment of hepatocellular carcinoma. |
| Enzyme Assay |
In vitro assays for miriplatin typically measure platinum-DNA adduct formation and cytotoxicity. For DNA adduct studies, cancer cells are treated with miriplatin, and DNA is extracted. Platinum-DNA adducts are measured by atomic absorption spectroscopy or by using specific antibodies in immunoassays. For cytotoxicity studies, cancer cells are treated with miriplatin at various concentrations, and cell viability is assessed using MTT or resazurin reduction assays. Apoptosis is assessed by flow cytometry or by measuring caspase activity. For studies investigating the mechanism of action, cell cycle analysis and DNA damage marker expression are assessed.
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| Cell Assay |
In vitro cellular assays for miriplatin employ hepatocellular carcinoma cell lines such as AH109A. Cells are cultured in appropriate media and treated with miriplatin at various concentrations, either alone or suspended in Lipiodol. Cell proliferation is assessed using standard assays such as MTT or resazurin reduction. Apoptosis is assessed by flow cytometry or by measuring caspase activity. Platinum-DNA adduct formation is measured by atomic absorption spectroscopy or immunoassays. The compound's effects on cell cycle distribution are assessed by flow cytometry. The compound's effects on signaling pathways can be assessed by Western blotting.
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| Animal Protocol |
In vivo animal experiments for miriplatin employ models of hepatocellular carcinoma. For TACE studies, animal models with liver tumors are used, and miriplatin suspended in Lipiodol is injected into the hepatic artery. Tumor growth is measured by imaging or by histological assessment. For pharmacokinetic studies, animals are administered miriplatin, and platinum concentrations in plasma and tissues are measured by atomic absorption spectroscopy. For toxicology studies, animals are administered miriplatin at various doses, and adverse effects are assessed. Dosing regimens vary depending on the experimental objectives.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of miriplatin have been characterized in preclinical studies. Miriplatin is selectively delivered to the liver; platinum and radioactive components are gradually released into systemic circulation and excreted into urine. In dogs with renal impairment, the compound's pharmacokinetics have been studied. Miriplatin has a molecular weight of 782.01 and a molecular formula of C₃₄H₇₀N₂O₅Pt. The compound's unique formulation allows for selective retention in tumor tissues, enhancing its therapeutic efficacy while minimizing systemic toxicity. The compound's pharmacokinetics support its use in TACE for hepatocellular carcinoma.
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| Toxicity/Toxicokinetics |
The toxicity profile of miriplatin is less severe compared to other platinum anticancer agents. Common adverse effects may include myelosuppression, hepatotoxicity, and gastrointestinal disturbances. The compound's selective delivery to the liver may reduce systemic toxicity compared to cisplatin or other platinum agents. However, as with all platinum-based drugs, miriplatin can cause nephrotoxicity, neurotoxicity, and ototoxicity. The compound should be used with caution in patients with renal impairment or preexisting liver disease. Miriplatin has been approved for use in Japan for the treatment of hepatocellular carcinoma.
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| References |
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| Additional Infomation |
Miriplatin hydrate is a lipophilic platinum complex used in TACE for the treatment of hepatocellular carcinoma. It contains myristates as leaving groups and can be easily suspended in Lipiodol. When suspended in Lipiodol, miriplatin (100 μg/mL) slows the development of AH109A cells, produces platinum-DNA adducts, and triggers apoptosis. Miriplatin is selectively delivered to the liver; platinum and radioactive components are gradually released into systemic circulation and excreted into urine. Miriplatin has a less severe toxicity profile compared to other platinum anticancer agents. It has a molecular weight of 782.01 and a molecular formula of C₃₄H₇₀N₂O₅Pt. Miriplatin is an effective chemotherapeutic agent and a type of alkylating agent.
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| Molecular Formula |
C34H70N2O5PT
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|---|---|
| Molecular Weight |
782.008014202118
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| Exact Mass |
781.493
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| CAS # |
250159-48-9
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| Related CAS # |
Miriplatin;141977-79-9
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| PubChem CID |
23725065
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
8.423
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
22
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| Heavy Atom Count |
42
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| Complexity |
212
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| Defined Atom Stereocenter Count |
2
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| SMILES |
NC1CCCCC1N.[O-]C(CCCCCCCCCCCCC)=O.[O-]C(CCCCCCCCCCCCC)=O.O.[Pt+2]
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| InChi Key |
LWDBMUAJGMXQAY-GSEQGPDBSA-L
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| InChi Code |
InChI=1S/2C14H28O2.C6H14N2.H2O.Pt/c2*1-2-3-4-5-6-7-8-9-10-11-12-13-14(15)16;7-5-3-1-2-4-6(5)8;;/h2*2-13H2,1H3,(H,15,16);5-6H,1-4,7-8H2;1H2;/q;;;;+2/p-2/t;;5-,6-;;/m..1../s1
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| Chemical Name |
(1R,2R)-cyclohexane-1,2-diamine;platinum(2+);tetradecanoate;hydrate
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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) |
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 | 1.2788 mL | 6.3938 mL | 12.7876 mL | |
| 5 mM | 0.2558 mL | 1.2788 mL | 2.5575 mL | |
| 10 mM | 0.1279 mL | 0.6394 mL | 1.2788 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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