Miriplatin hydrate
(Synonyms: 米铂水合物,SM-11355 (hydrate)) 目录号 : GC36615Miriplatin hydrate (SM-11355 hydrate) 为有效的化疗剂,是烷化剂 (alkylator) 的一种。
Cas No.:250159-48-9
Sample solution is provided at 25 µL, 10mM.
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Cell experiment: | Aliquots of AH109A cells are plated into 24-well microplates. Following cell adherence (1 day), Lipiodol (LPD) alone and agents (Miriplatin, etc.) suspended in LPD are added to Falcon cell culture inserts, equipped with a 0.4-μm pore membrane on their bottom. After 7 days of incubation at 37°C in 5% CO2, the numbers of viable cells are examined using AlamarBlue. The IC50 value is defined as the concentration inhibiting cell growth by 50% compared with treatment with LPD alone. To examine platinum concentrations in the medium, agents suspended in LPD are added to Falcon cell culture inserts in wells containing the culture medium alone. The platinum concentrations are quantitatively analyzed by FAAS. Alternatively, aliquots of AH109A cells are plated into 96-well microplates. Following cell adherence (1 day), agents in aqueous solution are added. After 3 days of incubation at 37°C in 5% CO2, the numbers of viable cells are examined using AlamarBlue[2]. |
Animal experiment: | Rats[2]Rats bearing a tumor approximately 100-250 mm3 in area are randomly allocated into different treatment groups and a control group, each of which consists of seven rats. Tumor diameters are measured with calipers, and estimated tumor area is calculated by the formula: (smaller diameter) × (larger diameter). All agents (Miriplatin, etc.) suspended in Lipiodol (LPD) and LPD alone are injected into the hepatic artery of tumor-bearing rats at the volume of 0.02 mL/head. The therapeutic dose of each agent is defined in this study as follows: Miriplatin (400 μg/head, 20 mg/mL in LPD), cisplatin (400 μg/head, 20 mg/mL) and zinostatin stimalamer (20 μg/head, 1 mg/mL). After the intra-hepatic arterial administration, the gastroduodenal artery and abdomen are closed with uninterrupted sutures. The tumor growth rate (%) is calculated with the following formula: A7/A70 × 100, where A7 is the estimated tumor area at day 7 and A70 is the estimated tumor area at the initiation of the treatment (day 0). The systemic toxicity of the treatments is assessed in terms of changes in body weight during the experiments. These are calculated as (W7 − W70)/W70 × 100 where W7 is body weight at day 7 and W70 is body weight at day 0[2]. |
References: [1]. Kishimoto S, et al. Antitumor effects of a novel lipophilic platinum complex (SM-11355) against a slowly-growing rat hepatic tumor after intra-hepatic arterial administration. Biol Pharm Bull. 2000 Mar;23(3):344-8. |
Miriplatin hydrate (SM-11355 hydrate) is a chemotherapy agent which belongs to the class of alkylating agents.
Miriplatin suspended in lipiodol (miriplatin/LPD, 100 μg/mL) inhibits the growth of AH109A cells, forms platinum-DNA adducts, and induces apoptosis[2].
Miriplatin (0.02-0.4 mg/20 μL) in lipiodol reduces tumor growth rates in a dose dependent manner in rats bearing AH109A tumor cells[1]. Miriplatin/LPD (400 μg/head) significantly reduces the growth of tumor in rats bearing AH109A cells[2].
[1]. Kishimoto S, et al. Antitumor effects of a novel lipophilic platinum complex (SM-11355) against a slowly-growing rat hepatic tumor after intra-hepatic arterial administration. Biol Pharm Bull. 2000 Mar;23(3):344-8. [2]. Hanada M, et al. Intra-hepatic arterial administration with miriplatin suspended in an oily lymphographic agent inhibits the growth of tumors implanted in rat livers by inducing platinum-DNA adducts to form and massive apoptosis. Cancer Chemother Pharmacol. 2009 Aug;64(3):473-83.
Cas No. | 250159-48-9 | SDF | |
别名 | 米铂水合物,SM-11355 (hydrate) | ||
Canonical SMILES | NC1CCCCC1N.[O-]C(CCCCCCCCCCCCC)=O.[O-]C(CCCCCCCCCCCCC)=O.O.[Pt+2] | ||
分子式 | C34H70N2O5Pt | 分子量 | 782.01 |
溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
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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 |
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给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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Comparison of epirubicin hydrochloride and Miriplatin hydrate as anticancer agents for transcatheter arterial chemoembolization of hepatocellular carcinoma
Hepatol Res 2013 May;43(5):475-80.PMID:23046493DOI:10.1111/j.1872-034X.2012.01100.x.
Aim: The aim of this retrospective study was to compare the local control effects of transcatheter arterial chemoembolization (TACE) using epirubicin (EPIR) and that using miriplatin (MPT) for hepatocellular carcinoma (HCC). Methods: Between January 2010 and July 2011, 218 HCC cases were treated with TACE, including 69 cases using EPIR or MPT as initial treatment. All 69 patients were treated with iodized oil and gelatin sponge particles. The local control rate (modified Response Evaluation Criteria in Solid Tumors [RECIST] ver. 1.0), time to treatment failure (Kaplan-Meier and log-rank test) and adverse events were evaluated. Results: Forty-two cases were treated using EPIR, and 27 cases were treated using MPT. All 69 patients had no previous treatment with TACE or hepatic arterial infusion. No serious adverse events were observed in either group. The response rates, including complete response (CR) and partial response (PR), of the EPIR group and the MPT group were 85.7% and 81.5%, respectively, with a time to treatment failure of 5.1 and 7.5 months, respectively. Excluding whole liver TACE cases, time to treatment failure was 5.4 months for the EPIR group and 10.1 months for the MPT group. Conclusion: In TACE naïve cases, there was no significant difference in local control between EPIR and MPT.
[Transcatheter arterial chemoembolization with a lipophilic platinum complex SM-11355(Miriplatin hydrate)--safety and efficacy in combination with embolizing agents]
Gan To Kagaku Ryoho 2010 Feb;37(2):271-5.PMID:20154484doi
SM-11355 is a cisplatin derivative with high affinity for iodized ethyl esters of fatty acids of poppyseed oil. Clinical trials have shown that SM-11355 is effective for treatment of hepatocellular carcinoma. Transcatheter arterial chemoembolization is commonly used in combination with embolizing agents, but concomitant use of SM-11355 and embolizing agents has not been evaluated in previous trials. In this study, the safety and efficacy of SM-11355 in combination with embolizing agents were investigated in 10 patients with hepatocellular carcinoma. An anti-tumor effect of TE4 was achieved in 4 of 9 patients and no serious adverse events were observed, indicating that this therapy can be used safely for hepatocellular carcinoma.
Use of contrast-enhanced ultrasonography with a perflubutane-based contrast agent performed one day after transarterial chemoembolization for the early assessment of residual viable hepatocellular carcinoma
Eur J Radiol 2013 Sep;82(9):1471-80.PMID:23769188DOI:10.1016/j.ejrad.2013.04.045.
Objective: We evaluated the efficacy of contrast-enhanced ultrasonography (US), compared with contrast-enhanced computed tomography (CT), for early assessments after transarterial chemoembolization (TACE) for the treatment of hypervascular hepatocellular carcinoma (HCC) lesions. Subjects and methods: Thirty-two patients with 59 HCC lesions who were scheduled to receive TACE were enrolled in this prospective study. TACE was performed by injecting a mixture of iodized oil and Miriplatin hydrate, followed by a gelatin sponge. Digital subtraction angiography (DSA) and/or contrast-enhanced CT were performed 2-6 months after TACE and were used as the reference standard for residual HCC; the detection rates for residual viable HCC using contrast-enhanced US with a perflubutane-based contrast agent and a high mechanical index (MI) mode performed one day after TACE were also compared with those obtained using contrast-enhanced CT performed one month after TACE. The comparisons were made using the McNemar test. Results: Forty-seven (79.7%) of the 59 HCC lesions were diagnosed as having residual viability based on DSA and contrast-enhanced CT findings obtained 2-6 months after TACE. Eight (17.0%) of the 47 HCC lesions that were diagnosed as having residual viability using one-day contrast-enhanced US were not detected using one-month contrast-enhanced CT because of artifacts produced by the high attenuation of the iodized oil. The detection rate for residual HCC lesions using one-day contrast-enhanced US (95.7%, 45/47) was significantly higher than that using one-month contrast-enhanced CT (78.7%, 37/47) (P<0.05). Conclusion: Contrast-enhanced US performed one day after TACE is more sensitive than contrast-enhanced CT performed one month after TACE for detecting residual viable HCC.