Imifoplatin
Based on 1 Customer Validation
Imifoplatin (PT-112) is a platinum-based active molecule and a member of the phosphaplatins family. Imifoplatin can induce Apoptosis and exhibits antitumor activity.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 95.0%
- CAS 番号: 1339960-28-9
- 分子式: C6H16N2O7P2Pt
- 分子量:485.23
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
生物活性
Imifoplatin (5–20 µM, 72 hours) shows dose-dependent proliferation inhibition in HCT116 cells[2]. Imifoplatin (10 µM, 24 hours) significantly induces apoptosis in HCT116 cells[2]. Imifoplatin (0.287–222.14 µM, 72 hours) significantly inhibits proliferation in CT26 cells[2]. Imifoplatin (2–10 μM, 24–72 hours) has notable selectivity, showing strong inhibition of glycolytic tumor cells with mtDNA mutations[3]. Imifoplatin (10 μM, 48–72 hours) significantly increases mtROS, especially in glycolytic L929dt and Cybrid cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Mouse fibroblast L929, mtDNA mutant L929dt, and Cybrid cells
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Concentration:2, 6, 10 μM
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Incubation Time:24–72 hours
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Result:Inhibited L929dt and Cybrid cells by about 80% after 48 hours, while inhibition in OXPHOS-competent L929 cells was lower.
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Cell Line:HCT116 (human colorectal cancer cells)
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Concentration:5, 10, 20 µM
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Incubation Time:72 hours
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Result:Significantly inhibited cell proliferation at higher concentrations.
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Cell Line:HCT116 (human colorectal cancer cells)
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Concentration:10 µM
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Incubation Time:24 hours
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Result:Increased proportions of early and late apoptotic cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MC38 colorectal carcinoma xenograft model in C57BL/6J mice[2]
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Dosage:90 mg/kg
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Administration:Intravenous injection (i.v.), once weekly for 7 weeks
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Result:Inhibited tumor growth, extended survival; further enhanced survival when combined with PD-1 blockade (Avelumab (HY-108730)).
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Animal Model:CT26 colorectal carcinoma xenograft model in BALB/c mice[2]
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Dosage:90 mg/kg
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Administration:Intravenous injection (i.v.), once weekly for 5 weeks
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Result:Significantly inhibited tumor growth, increased T-cell infiltration, reduced immunosuppressive TAMs.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1339960-28-9
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性状 Solid
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分子量 485.23
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分子式 C6H16N2O7P2Pt
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Color White to off-white
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SMILES
O=[P]([O-][Pt+2]1([O-][P]2(O)=O)[NH2][C@@](CCCC3)([H])[C@]3([H])[NH2]1)(O2)O
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別名
PT-112
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
H2O : 1.25 mg/mL (2.58 mM; Need ultrasonic; DMSO can inactivate Imifoplatin's activity)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (284 KB)
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SDS (252 KB)
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- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[2]. Yamazaki T, et al. PT-112 induces immunogenic cell death and synergizes with immune checkpoint blockers in mouse tumor models. Oncoimmunology. 2020 Feb 11;9(1):1721810. [Content Brief]
[3]. Soler-Agesta R, et al. PT-112 induces mitochondrial stress and immunogenic cell death, targeting tumor cells with mitochondrial deficiencies[J]. Cancers, 2022, 14(16): 3851. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 2.0609 mL | 10.3044 mL | 20.6088 mL | 51.5220 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.