Lurbinectedin

製品コードS9603 バッチS960303

印刷

化学情報

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)

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <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, a DNA minor groove covalent binder with potent in vitro and in vivo anti-tumour activity. Lurbinectedin inhibits RMG1 and RMG2 cell growth with IC50 of 1.25 nM and 1.16 nM, respectively.
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.^[1]
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.^[1]

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 (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

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。