Home DNA Damage/DNA Repair DNA/RNA Synthesis modulator Lurbinectedin For research use only.

Lurbinectedin

Synonyms: PM-1183, LY-01017, Tryptamicidin, PM01183

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.

Lurbinectedin Chemical Structure

Lurbinectedin Chemical Structure

CAS No. 497871-47-3

Purity & Quality Control

Lurbinectedin Related Products

Signaling Pathway

DNA/RNA Synthesis Signaling Pathways

DNA/RNA Synthesis Signaling Pathway

Biological Activity

Description 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.
Targets
DNA minor groove [1] RMG2 cell growth [1]
(Cell-based assay)		 RMG1 cell growth [1]
(Cell-based assay)
1.16 nM 1.25 nM
In vitro
In vitro

Lurbinectedin exhibits significant antitumor activity toward chemosensitive and chemoresistant CCC cells in vitro. Lurbinectedin plus SN-38 combination has strong synergistic effects on both the cisplatin-resistant and paclitaxel-resistant CCC cell lines.[1]
Cell Research Cell lines The human ovarian CCC cell lines (RMG1, RMG2, KOC7C, HAC2)
Concentrations 0.1 nM, 0.3 nM, 1 nM, 3 nM
Incubation Time 48 h
Method

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.
In Vivo
In vivo

An examination of mouse CCC cell xenografts reveals that lurbinectedin significantly inhibits tumor growth. Lurbinectedin plus SN-38 combination results in a significant synergistic effect. Everolimus significantly enhances the antitumor activity of lurbinectedin-based chemotherapies.[1]
Animal Research Animal Models 5- to 7-week-old nude mice
Dosages 0.180 mg/kg
Administration IV
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06385548 Not yet recruiting
Endometrial Cancer
Vall d''Hebron Institute of Oncology
 May 2024 Phase 1|Phase 2
NCT06228066 Recruiting
Small Cell Carcinoma of the Bladder|High Grade Neuroendocrine Tumors of the Urinary Tract
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)
 May 15 2024 Phase 2
NCT06088290 Recruiting
Leiomyosarcoma
PharmaMar
 September 21 2023 Phase 2|Phase 3
NCT05734066 Recruiting
Refractory Ewing Sarcoma|Relapsed Ewing Sarcoma|Ewing Sarcoma
Jazz Pharmaceuticals
 May 23 2023 Phase 1|Phase 2

Chemical Information & Solubility

Molecular Weight 784.87 Formula

C41H44N4O10S
CAS No. 497871-47-3 SDF --
Smiles CC1=CC2=C(C3C4C5C6=C(C(=C7C(=C6C(N4C(C(C2)N3C)O)COC(=O)C8(CS5)C9=C(CCN8)C2=C(N9)C=CC(=C2)OC)OCO7)C)OC(=O)C)C(=C1OC)O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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