Lurbinectedin (PM01183)

製品コードS9603 バッチS960303

印刷

化学情報

 Chemical Structure Synonyms PM-1183, LY-01017, Tryptamicidin, PM01183 Storage
(From the date of receipt)
3 years -20°C powder
化学式

C41H44N4O10S

分子量 784.87 CAS No. 497871-47-3
Solubility (25°C)* 体外 DMSO 100 mg/mL (127.4 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液(一定の濃度)を調合する

生物活性

製品説明 Lurbinectedinは、強力なin vitroおよびin vivo抗腫瘍活性を有するDNAマイナーグルーブ共有結合結合剤です。Lurbinectedinは、RMG1およびRMG2細胞の増殖をそれぞれ1.25 nMおよび1.16 nMのIC50で阻害します。
in vitro

Lurbinectedin exhibits significant antitumor activity toward chemosensitive and chemoresistant CCC cells in vitro. This compound plus SN-38 combination has strong synergistic effects on both the cisplatin-resistant and paclitaxel-resistant CCC cell lines.

in vivo

An examination of mouse CCC cell xenografts reveals that lurbinectedin significantly inhibits tumor growth. This compound plus SN-38 combination results in a significant synergistic effect. Everolimus significantly enhances the antitumor activity of this chemical-based chemotherapies.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 The human ovarian CCC cell lines (RMG1, RMG2, KOC7C, HAC2)
濃度 0.1 nM, 0.3 nM, 1 nM, 3 nM
反応時間 48 h
実験の流れ

CCC cells (2~5×105) are treated with lurbinectedin, SN38 or in combination of the two drugs at the indicated concentrations for 48 hours. Then, the cells are harvested and stained with PI and annexin V using the annexin V-fluorescein isothiocyanate (FITC) apoptosis detection kit, according to the manufacturer's instructions. Fluorescence data are collected using flow cytometry. The sum total of early apoptotic cells (annexin V(+), PI(−) cells) and late apoptotic cells (annexin V(+), PI(+) cells) is defined as the total number of apoptotic cells. The experiments are repeated at least three times.

動物実験 動物モデル 5- to 7-week-old nude mice
投薬量 0.180 mg/kg
投与方法 IV

参考

  • https://pubmed.ncbi.nlm.nih.gov/26986199/
  • https://pubmed.ncbi.nlm.nih.gov/20977459/

Selleckの高級品が、幾つかの出版された研究調査結果(以下を含む)で使われた:

The Effect of Lurbinectedin as a Monotherapy and in Combination with Ionizing Radiation on Sarcoma Cell Lines [ Cancers, 2025, 2930] PubMed: 40941027.0
The Effect of Lurbinectedin as a Monotherapy and in Combination with Ionizing Radiation on Sarcoma Cell Lines [ Cancers (Basel), 2025, 17(17)2930] PubMed: 40941027
Protocol to co-culture SCLC cells with human CD8+ T cells to measure tumor cell killing and T cell activation [ STAR Protoc, 2025, 6(2):103767] PubMed: 40232937
Lurbinectedin sensitizes PD-L1 blockade therapy by activating STING-IFN signaling in small-cell lung cancer [ Cell Rep Med, 2024, 5(12):101852] PubMed: 39657664
The Novel ATR Inhibitor Tuvusertib (M1774) Induces Replication Protein Overexpression and Broad Synergy with DNA-targeted Anticancer Drugs [ Molecular Cancer Therapeutics, 2024, 911-923] PubMed: 38466804.0

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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