Belotecan
Based on 2 publication(s) in Google Scholar
Belotecan (CKD-602 free base) is a DNA topoisomerase I inhibitor. Belotecan induces cell apoptosis and cell-cycle arrest. Belotecan is a camptothecin analogue with anti-tumor effects, it can be used for the research of cancer.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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 : 99.86%
- CAS 番号: 256411-32-2
- 分子式: C25H27N3O4
- 分子量:433.50
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保管条件:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 Belotecan
MoreTopoisomerase アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
IC50 & Target
IC50: 30 ng/mL (Caski cells), 150 ng/mL (HeLa cells), 150 ng/mL (SiHa cells)[1]
体外実験
Belotecan (0-600 ng/mL; 0-72 h) time- and dose-dependently inhibits viability of Caski cells, HeLa cells and SiHa cells at 48 h with IC50 values of 30, 150 and 150 ng/mL, respectively[1]. Belotecan (0-150 ng/mL; 48 h) induces cell apoptosis and cell-cycle arrest, and affects PARP, cleaved PARP, BAX, p53, Ser15, cell cycle related protein expression and cancer invasion in cervical cancer[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Caski, HeLa and SiHa cell lines
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Concentration:0-150 ng/mL
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Incubation Time:48 h
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Result:Showed strong pro-apoptotic activities to Caski, HeLa and SiHa cells.
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Cell Line:Caski, HeLa and SiHa cell lines
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Concentration:0-150 ng/mL
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Incubation Time:48 h
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Result:Increased the expression of PARP, cleaved PARP, BAX, p53, Ser15, cyclin B1, phosphorylated cyclin B1 and phospho-cdc2 (Tyr15) protein, and decreased MMP2 and VEGF protein expression.
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Cell Line:Caski, HeLa and SiHa cell lines
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Concentration:0-150 ng/mL
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Incubation Time:48 h
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Result:Induced cell-cycle arrest in the G2/M phase in cervical cancer.
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Cell Line:Caski, HeLa and SiHa cell lines
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Concentration:0-150 ng/mL
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Incubation Time:48 h
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Result:Inhibited cancer invasion in cervical cancer.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c-nude mice with CaSki cells injection[1]
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Dosage:25 mg/kg
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Administration:Intravenous injection; 25 mg/kg; 16 days at 4-day intervals
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Result:Significantly inhibited the tumor growth and showed no significant difference in bodyweight of xenograft mice and the controls.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 256411-32-2
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性状 Solid
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分子量 433.50
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分子式 C25H27N3O4
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Color Light yellow to yellow
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SMILES
O=C1[C@](O)(CC)C2=C(CO1)C(N3CC4=C(CCNC(C)C)C5=CC=CC=C5N=C4C3=C2)=O
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別名
CKD-602 free base
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Publications (2)
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Journal Impact Factor
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Most Recent
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J Mol Med (Berl)
2019 Aug;97(8):1183-1193. PMID: 31201471 -
溶剤 & 溶解度
体外:
DMSO : 12.5 mg/mL (28.84 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.25 mg/mL (2.88 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (282 KB)
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SDS (479 KB)
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- Portuguese - PT (479 KB)
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取扱説明書 (2659 KB)
参考文献
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 (protect from light, stored under nitrogen). 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 |
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| DMSO | 1 mM | 2.3068 mL | 11.5340 mL | 23.0681 mL | 57.6701 mL |
| 5 mM | 0.4614 mL | 2.3068 mL | 4.6136 mL | 11.5340 mL | |
| 10 mM | 0.2307 mL | 1.1534 mL | 2.3068 mL | 5.7670 mL | |
| 15 mM | 0.1538 mL | 0.7689 mL | 1.5379 mL | 3.8447 mL | |
| 20 mM | 0.1153 mL | 0.5767 mL | 1.1534 mL | 2.8835 mL | |
| 25 mM | 0.0923 mL | 0.4614 mL | 0.9227 mL | 2.3068 mL |
Belotecan 関連分類
HY-13566 関連分類
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