2. Cell Cycle/DNA Damage
  3. DNA Alkylator/Crosslinker DNA/RNA Synthesis
  4. Lurbinectedin

Lurbinectedin  (Synonyms: PM01183; LY-01017)

Cat. No.: HY-16293 Purity: 99.70%
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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.

CAS No. : 497871-47-3

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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of Lurbinectedin:

Lurbinectedin Related Antibodies

Top Publications Citing Use of Products
Cell Proliferation/Viability Assay
Apoptosis Analysis
Cell Imaging/Staining
WB
Bio/Physico-chemical Assay
2D/3D Cell Culture and Differentiation

    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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    Description

    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.

    IC50 & Target

    IC50: 1.25 nM (RMG1), 1.16 nM (RMG2)[1]
    In Vitro

    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.

    Lurbinectedin Related Antibodies
    In Vivo

    Mouse CCC cell xenografts reveals that lurbinectedin significantly inhibits tumor growth. Lurbinectedin plus SN-38 results in a significant synergistic effect[1]. In four murine xenograft models of human cancer, PM01183 inhibits tumour growth significantly with no weight loss of treated animals[2]. Single lurbinectedin or NSC 119875-combined therapies are effective in treating NSC 119875-sensitive and NSC 119875-resistant preclinical ovarian tumor models. The strongest synergistic effect is observed for combined treatments, especially in NSC 119875-resistant tumors. Lurbinectedin tumor growth inhibition is associated with reduced proliferation, increased rate of aberrant mitosis, and subsequent induced apoptosis[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    784.87

    Formula

    C41H44N4O10S
    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    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
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.2741 mL 6.3705 mL 12.7410 mL
    5 mM 0.2548 mL 1.2741 mL 2.5482 mL
    View the 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.

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    This equation is commonly abbreviated as: C1V1 = C2V2

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    Working solution concentration: mg/mL
    Purity & Documentation

    Purity: 99.71%

    SDS (393 KB)

    COA (267 KB) HNMR (437 KB) RP-HPLC (235 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [1]

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [3]

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References

    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
    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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    Lurbinectedin Related Classifications

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Lurbinectedin497871-47-3PM01183 LY-01017PM 01183PM-01183LY01017LY 01017LY-01017DNA Alkylator/CrosslinkerDNA/RNA SynthesisInhibitorinhibitorinhibit

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