Simmitecan
Simmitecan is a potent topoisomerase I (TOP1) inhibitor, which is a 9-substituted lipophilic camptothecin (Camptothecin (HY-16560)) derivative. Simmitecan blocks DNA replication and transcription, thereby inducing tumor cell apoptosis by inhibiting the activity of TOP1. Simmitecan can be used in the research of cancers such as liver 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。
- CAS 番号: 951290-31-6
- 分子式: C34H38N4O6
- 分子量:598.70
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
Topoisomerase アイソフォーム固有の製品をすべて表示
More
生物活性
製品説明
IC50 & Target
[1]|
Top1 |
CYP3A4 8.95 μM (IC50) |
CYP2D6 32.9 μM (IC50) |
体外実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | Cmax | AUC0-24 | T1/2 | MRT | CLplasma | Vss |
|---|---|---|---|---|---|---|---|---|
| Mice[1] | 15 mg/kg | i.v. | 5124 nM | 8142 nM·h | 0.95 h | 1.14 h | 3.16 L/h/kg | 3.57 L/kg |
| Rat[1] | 3.75 mg/kg | i.v. | 1651 nM | 3709 nM·h | 1.45 h | 1.85 h | 1.82 L/h/kg | 3.34 L/kg |
| Rat[1] | 7.5 mg/kg | i.v. | 3518 nM | 8922 nM·h | 1.46 h | 1.92 h | 1.54 L/h/kg | 2.91 L/kg |
| Rat[1] | 15 mg/kg | i.v. | 7192 nM | 17906 nM·h | 1.42 h | 1.91 h | 1.51 L/h/kg | 2.86 L/kg |
| Dog[1] | 1.25 mg/kg | i.v. | 616 nM | 2050 nM·h | 1.95 h | 2.74 h | 1.12 L/h/kg | 3.03 L/kg |
| Dog[1] | 2.5 mg/kg | i.v. | 1135 nM | 3712 nM·h | 1.90 h | 2.74 h | 1.20 L/h/kg | 3.27 L/kg |
| Dog[1] | 5 mg/kg | i.v. | 2101 nM | 6417 nM·h | 1.72 h | 2.45 h | 1.46 L/h/kg | 3.54 L/kg |
体内実験
Simmitecan (15 mg/kg; intravenous injection; single administration; 8 h) exhibits extensive distribution in tissues including tumors and substantial conversion into its active metabolite L-2-Z in nude mouse xenograft models bearing the human hepatocellular carcinoma SMMC-7721 cell line[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Sprague-Dawley (male and female, 250-300 g)[1]
-
Dosage:3.75 mg/kg; 7.5 mg/kg; 15 mg/kg
-
Administration:i.v.; single dose; 48 h
-
Result:Was rapidly biotransformed into its active metabolite L-2-Z in vivo and extensively distributed in most tissues (with the highest concentrations observed in the pancreas, kidneys, and liver).
Was predominantly eliminated via biliary excretion, and metabolism was also a major elimination route for the intact drug after iv administration.
-
Animal Model:Nude (male and female, 18-20 g, xenograft model of human hepatic cancer SMMC-7721 cells)[1]
-
Dosage:15 mg/kg
-
Administration:i.v.; single dose; samples harvested at 0.25, 1, 2, 4, 8 h
-
Result:Simmitecan and its active metabolite L-2-Z rapidly distributed to tissues, reaching peak concentrations 15 minutes after dosing.
化学情報
-
CAS 番号 951290-31-6
-
分子量 598.70
-
分子式 C34H38N4O6
-
SMILES
O=C1N2C(C=3C(C2)=CC=4C(N3)=CC=C(OC(=O)N5CCC(CC5)N6CCCCC6)C4CC=C)=CC7=C1COC(=O)[C@@]7(CC)O
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[1]. Hu ZY, et al. Pharmacokinetic evaluation of the anticancer prodrug simmitecan in different experimental animals. Acta pharmacologica Sinica. 2013 Nov;34(11):1437-48. [Content Brief]
[2]. Zhou J, et al. A validated HPLC-MS/MS method for determination of simmitecan and its metabolite chimmitecan in human plasma and its application to a pharmacokinetic study in Chinese patients with advanced solid tumor. Journal of separation science. 2021 Nov;44(21):3959-3966. [Content Brief]
[3]. Zhang Q, et al. A Phase Ib Study of the Simmitecan Single Agent and in Combination With 5-Fluorouracil/Leucovorin or Thalidomide in Patients With Advanced Solid Tumor. Frontiers in pharmacology. 2022;13:833583. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Simmitecan 関連分類
HY-107133A 関連分類
Powered by Bioz