Lurbinectedin
Based on 8 publication(s) in Google Scholar
Lurbinectedin (PM01183) is a DNA minor groove covalent binder with potent anti-tumour activity; inhibits RMG1 and RMG2 cell growth with IC50 values of 1.25 and 1.16 nM, respectively.
For research use only. We do not sell to patients.
- Purity: 99.70%
- CAS No.: 497871-47-3
- Formula: C41H44N4O10S
- Molecular Weight:784.87
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Lurbinectedin
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Customer Validation & Images
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Cell Proliferation/Viability Assay
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Apoptosis Analysis
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Cell Imaging/Staining
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WB
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Bio/Physico-chemical Assay
All DNA/RNA Synthesis Isoforms
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Biological Activity
IC50: 1.25 nM (RMG1), 1.16 nM (RMG2)[1]
PM01183 is a new synthetic tetrahydroisoquinoline alkaloid that is currently in phase I clinical development for the treatment of solid tumours. PM01183–DNA adducts in living cells give rise to double-strand breaks, triggering S-phase accumulation and apoptosis. The potent cytotoxic activity of PM01183 is ascertained in a 23-cell line panel with a mean GI50 value of 2.7 nM[2]. Lurbinectedin exhibits significant antitumor activity toward chemosensitive and chemoresistant human ovarian clear cell carcinoma (CCC) cells in vitro[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 497871-47-3
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Appearance Solid
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Molecular Weight 784.87
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Formula C41H44N4O10S
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Color White to light yellow
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SMILES
O[C@@H]([C@@](CC1=CC(C)=C2OC)([H])N(C)[C@]3([H])C1=C2O)N([C@](COC4=O)([H])C5=C(OCO6)C6=C7C)[C@@]3([H])[C@@](SC[C@@]4(NCC8)C9=C8C%10=CC(OC)=CC=C%10N9)([H])C5=C7OC(C)=O
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Synonyms
PM01183; LY-01017
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (8)
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Journal Impact Factor
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Most Recent
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Int J Mol Sci
The DNA Minor Groove Binders Trabectedin and Lurbinectedin Are Potent Antitumor Agents in Human Intrahepatic Cholangiocarcinoma. [Abstract]2025 Sep 18;26(18):9085. PMID: 41009648
Lurbinectedin purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2025 Sep 18;26(18):9085. [Abstract]
Effect Lurbinectedin on the viability of intrahepatic cholangiocarcinoma cell lines. Cell viability of six human intrahepatic cholangiocarinoma (iCCA) cell lines (CCLP1, HUCCT1, KKU055, KKU156, KKU213, and SG231) exposed to 0-100 nM Lurbinectedin for 48 h was assessed by MTT assay. A summary of the IC50 of the conpound in the six cell lines is depicted next to the graph. Dashed horizontal lines indicate 50% cell viability.
Lurbinectedin purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2025 Sep 18;26(18):9085. [Abstract]
Apoptosis was assessed in HUCCT1, CCLP1, KU055, KKU156, KKU213 and SG231 cell lines treated for 48 hours with trabectedin (TRB) and Lurbinectedin (LUR) at 1 nM and 5 nM concentrations. Cells treated with solvent (DMSO) served as controls.
Lurbinectedin purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2025 Sep 18;26(18):9085. [Abstract]
Lurbinectedin (LUR) restrain the growth of HUCCT1 and KKU213 intrahepatic cholangiocarcinoma cells grown as 3D cultures (spheroids). HUCCT1- and KKU213-derived spheroids were treated with DMSO (vehicle) and increasing concentrations of trabectedin (TRB) and lurbinectedin (LUR; 0.25–2 nM; n = 3 wells per condition). Note the decrease in size and number of spheroids following the treatment with Lurbinectedin (LUR), as assessed by the optical microscope. Original magnification: 10×; scale bar: 100 µm.
Lurbinectedin purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2025 Sep 18;26(18):9085. [Abstract]
Western blot analysis was applied to assess the levels of several effectors of DNA damage response and apoptosis pathways in HUCCT1, SG231, CCLP1, and KKU055 intrahepatic cholangiocarcinoma (iCCA) cell lines exposed to trabectedin (TRB) and Lurbinectedin (LUR) at 1 nM concentration. Cells were treated for 48 h, and Western blot analysis was conducted at this time point. Representative blots are shown.
Lurbinectedin purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2025 Sep 18;26(18):9085. [Abstract]
Effect of trabectedin and Lurbinectedin (LUR) on the mitochondrial respiration of human intrahepatic cholangiocarcinoma cells. For the Seahorse XF Mito Stress Test, KKU055 cells were treated with 1 nM Lurbinectedin (LUR), or a matched DMSO concentration for 24 h. The Seahorse Mito Stress Test profile of normalized oxygen consumption rate (OCR) in LUR-treated KKU055 cells is shown. The results showed LUR administration significantly decreased most parameters (basal and compensatory glycolysis, and basal proton efflux rate). All OCR levels were background corrected and normalized to nuclei fluorescent staining. Dotted lines indicate the time point of compound injection. Cell #, cell number; FCCP, carbonyl cyanide-p-trifluoromethoxyphenylhydrazone; Rot/AA, rotenone/antimycin A.
Lurbinectedin purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2025 Sep 18;26(18):9085. [Abstract]
Microscopic images demonstrate that treatment with trabectedin (TRB) and Lurbinectedin (LUR) (2.5-20 nM; 72 h) resulted in a reduction in the compact, well-organized structure of the organoids, evidenced by the loss of the typical cystic shape associated with cholangiocarcinoma organoids.
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iScience
Teriflunomide/leflunomide synergize with chemotherapeutics by decreasing mitochondrial fragmentation via DRP1 in SCLC. [Abstract]2024 May 27;27(6):110132. PMID: 38993482 -
Thorac Cancer
High mRNA expression of POU2F3 in small cell lung cancer cell lines predicts the effect of lurbinectedin. [Abstract]2022 Apr;13(8):1184-1192. PMID: 35278040 -
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Solvent & Solubility
DMSO : 20 mg/mL (25.48 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocol
The MTS assay is used to analyze the effects of each drug. Cells are plated in 96-well plates and treated with PM01183 (0, 0.1, 0.3, 1, 3 nM) . After 48 hours’ incubation, the number of surviving cells is assessed by determining the A490nm of the dissolved formazan product after the addition of MTS for 1 hour. Cell viability is calculated as follows: Aexp group / Acontrol×100[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice: Mice are transplanted with fragments of OVAX1 and OVAX1R tumors, and when tumors reaches a homogeneous palpable size are randomly allocated into the treatment groups: i) Placebo; ii) Lurbinectedin (0.18 mg/kg); iii) NSC 119875 (3.5 mg/kg); and iv) Lurbinectedin plus NSC 119875 (0.18 + 3.5 mg/kg). Drugs are i.v. administered once per week for 3 consecutive weeks (days 0, 7, and 14). Seven days after the final dose (day 21), animals are sacrificed, their ovaries dissected out, and weighed. Representative fragments are either frozen in nitrogen or fixed and then processed for paraffin embedding[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (288 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Takahashi R, et al. Preclinical Investigations of PM01183 (Lurbinectedin) as a Single Agent or in Combination with Other Anticancer Agents for Clear Cell Carcinoma of the Ovary. PLoS One. 2016 Mar 17;11(3):e0151050. [Content Brief]
[2]. Leal JF, et al. PM01183, a new DNA minor groove covalent binder with potent in vitro and in vivo anti-tumour activity. Br J Pharmacol. 2010 Nov;161(5):1099-110. [Content Brief]
[3]. Vidal A, et al. Lurbinectedin (PM01183), a new DNA minor groove binder, inhibits growth of orthotopic primary graft of NSC 119875-resistant epithelial ovarian cancer. Clin Cancer Res. 2012 Oct 1;18(19):5399-411. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.2741 mL | 6.3705 mL | 12.7410 mL | 31.8524 mL |
| 5 mM | 0.2548 mL | 1.2741 mL | 2.5482 mL | 6.3705 mL | |
| 10 mM | 0.1274 mL | 0.6370 mL | 1.2741 mL | 3.1852 mL | |
| 15 mM | 0.0849 mL | 0.4247 mL | 0.8494 mL | 2.1235 mL | |
| 20 mM | 0.0637 mL | 0.3185 mL | 0.6370 mL | 1.5926 mL | |
| 25 mM | 0.0510 mL | 0.2548 mL | 0.5096 mL | 1.2741 mL |
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