Home DNA Damage/DNA Repair DNA/RNA Synthesis modulator Lurbinectedin

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Lurbinectedin DNA/RNA Synthesis modulator

Cat.No.S9603

Lurbinectedin, a DNA minor groove covalent binder with potent in vitro and in vivo anti-tumour activity. This compound inhibits RMG1 and RMG2 cell growth with IC50 of 1.25 nM and 1.16 nM, respectively.
Lurbinectedin DNA/RNA Synthesis modulator Chemical Structure

Chemical Structure

Molecular Weight: 784.87

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Quality Control

Chemical Information, Storage & Stability

Molecular Weight 784.87 Formula

C41H44N4O10S

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 497871-47-3 -- Storage of Stock Solutions

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

Solubility

In vitro
Batch:

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Mass Concentration Volume Molecular Weight

In vivo
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In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
DNA minor groove [1]
RMG2 cell growth [1]
(Cell-based assay)
1.16 nM
RMG1 cell growth [1]
(Cell-based assay)
1.25 nM
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]
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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