A DNA-crosslinking agent
Carboplatin is a DNA synthesis inhibitor.
DNA synthesis is the natural or artificial creation of deoxyribonucleic acid (DNA) molecules.
Carboplatin inhibits DNA synthesis by binding to DNA and interfering with repair mechanism. In MTT assays with A2780, SKOV-3, IGROV-1 and HX62 human ovarian cancer cells, Carboplatin inhibited cell proliferation with IC50 of 6.2 μM, 12.4 μM, 2.2 μM and 116 μM for A2780, SKOV-3, IGROV-1 and HX62, respectively [1]. In UMC-11, H727 and H835 lung carcinoid cell line, Carboplatin also shows the anti-proliferative activities [2].
In xenograft-bearing mice, Carboplatin (60 mg/kg) had a modest antitumor effect and the relative tumor volumes on day 6 were 8.4 relative to the control of 11.9 [1]. Treatment of 56 small cell lung carcinoma patients with Carboplatin (300-400 mg/m2), 23 patients achieved a response including 5 complete remissions. 18 of 30 previously untreated patients achieved a response. Carboplatin was well tolerated and there was no nephrotoxicity [3].
参考文献:
[1].? Banerji U, Sain N, Sharp SY, et al. An in vitro and in vivo study of the combination of the heat shock protein inhibitor 17-allylamino-17-demethoxygeldanamycin and carboplatin in human ovarian cancer models. Cancer Chemother Pharmacol, 2008, 62(5): 769-778.
[2].? Fiebiger W, Olszewski U, Ulsperger E, et al. In vitro cytotoxicity of novel platinum-based drugs and dichloroacetate against lung carcinoid cell lines. Clin Transl Oncol, 2011, 13(1): 43-49.
[3].? Smith IE, Evans BD. Carboplatin (JM8) as a single agent and in combination in the treatment of small cell lung cancer. Cancer Treat Rev, 1985, 12 Suppl A: 73-75.
| Cell experiment [1]: | |
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Cell lines |
A2780, SKOV3, IGROV-1 and HX62 cells |
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Preparation method |
The solubility of this compound in DMSO is limited. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
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Reacting condition |
0 ~ 200 μM; 72 hrs |
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Applications |
In a panel of human ovarian cancer cell lines, e.g. A2780, SKOV3 and IGROV-1 cells, Carboplatin significantly inhibited cell proliferation, with the IC50 values of 6.1 μM, 12.4 μM and 2.2 μM, respectively. When it was combined with 17-allylamino-17-demethoxygeldanamycin (17-AAG), antagonism instead of synergistic effect was indicated. |
| Animal experiment [1]: | |
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Animal models |
Nude mice bearing A2780 tumors |
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Dosage form |
60 mg/kg; i.p. |
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Applications |
In nude mice bearing A2780 tumors, Carboplatin alone exhibited a modest antitumor effect, with the relative tumor volume of 8.4 on day 6. Moreover, the tumor weight relative to control (T/C) was 67%. When Carboplatin was combined 17-AAG, significantly greater antitumor activity was shown with the relative tumor volume and the T/C value reduced to 4.2 and 22% on day 6, respectively. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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参考文献: [1]. Banerji U, Sain N, Sharp SY, et al. An in vitro and in vivo study of the combination of the heat shock protein inhibitor 17-allylamino-17-demethoxygeldanamycin and carboplatin in human ovarian cancer models. Cancer Chemother Pharmacol, 2008, 62(5): 769-778. |
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