Lurbinectedin
- Product Name
- Lurbinectedin
- CAS No.
- 497871-47-3
- Chemical Name
- Lurbinectedin
- Synonyms
- PM01183;PM-01183;PM 01183;LURBINECTEDIN;Lurbinectidine;UNII-2CN60TN6ZS;Lurbinectedin (PM01183);PM01183;PM-01183;PM 01183;Cypermethrin Impurity 18 (Phenothrin);Lurbinectedin,DNA/RNA Synthesis,inhibit,DNA Alkylator/Crosslinker,PM-01183,Inhibitor,PM 01183
- CBNumber
- CB82628057
- Molecular Formula
- C41H44N4O10S
- Formula Weight
- 784.88
- MOL File
- 497871-47-3.mol
Lurbinectedin Property
- Density
- 1.55±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- pka
- 9.79±0.40(Predicted)
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H400Very toxic to aquatic life
H410Very toxic to aquatic life with long lasting effects
- Precautionary statements
-
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P273Avoid release to the environment.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P330Rinse mouth.
P391Collect spillage. Hazardous to the aquatic environment
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- orb573146
- Product name
- Lurbinectedin
- Purity
- >98%
- Packaging
- 5mg
- Price
- $2839
- Updated
- 2021/12/16
- Product number
- CS-6323
- Product name
- Lurbinectedin
- Purity
- 99.91%
- Packaging
- 2mg
- Price
- $3360
- Updated
- 2021/12/16
- Product number
- orb573146
- Product name
- Lurbinectedin
- Purity
- >98%
- Packaging
- 10mg
- Price
- $4173.5
- Updated
- 2021/12/16
- Product number
- orb573146
- Product name
- Lurbinectedin
- Purity
- >98%
- Packaging
- 25mg
- Price
- $5210.5
- Updated
- 2021/12/16
- Product number
- CS-6323
- Product name
- Lurbinectedin
- Purity
- 99.91%
- Packaging
- 100ug
- Price
- $550
- Updated
- 2021/12/16
Lurbinectedin Chemical Properties,Usage,Production
Description
Lurbinectedin is a synthetic tetrahydropyrrolo [4, 3, 2-de]quinolin-8(1H)-one alkaloid analogue with potential antineoplastic activity. Lurbinectedin covalently binds to residues lying in the minor groove of DNA, which may result in delayed progression through S phase, cell cycle arrest in the G2/M phase and cell death. Lurbinectedin was approved for medical use in the United States in June 2020.
Uses
Lurbinectedin is being developed for the treatment of various cancers. It has been granted approval for treatment of metastatic small cell lung cancer.
Application
Lurbinectedin is indicated for the treatment of adult patients with metastatic small cell lung cancer (SCLC) with disease progression on or after platinum-based chemotherapy.
Biological Activity
Lurbinectedin (PM01183, PM-1183, LY-01017, Tryptamicidin, Zepsyre, ZEPZELCA), 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.
Mechanism of action
Lurbinectedin is a next-generation DNA minor groove binder that exerts potent antitumor activity in a low nanomolar range. Furthermore, it inhibits RNA-polymerase-II activity and promotes its specific degradation by the ubiquitin/proteasome machinery. In several human cancer cell lines, lurbinectedin blocks the transcription process through binding to CG-rich sequences near the promoters of protein-coding genes. This drug triggers both the degradation of phosphorylated RNA polymerase II (Pol II) on the DNA template and the generation of SSBs and DSBs that drive tumor cells to apoptosis. By attenuating the activity of the nucleotide excision repair (NER) mechanism, lurbinectedin was able to overcome cisplatin resistance in NER hyperactive cell lines. Lurbinectedin was also shown to inactivate Ewing Sarcoma Oncoprotein (EWS-FLI1) by nuclear redistribution leading to promotor inactivity and decreased mRNA and protein levels[1-2].
Side effects
The most common side effects include leukopenia, lymphopenia, fatigue, anemia, neutropenia, increased creatinine, increased alanine aminotransferase, increased glucose, thrombocytopenia, nausea, decreased appetite, musculoskeletal pain, decreased albumin, constipation, dyspnea, decreased sodium, increased aspartate aminotransferase, vomiting, cough, decreased magnesium and diarrhea.
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.
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.
Mode of action
Lurbinectedin is an Alkylating Drug. The mechanism of action of lurbinectedin is as an Alkylating Activity.
References
[1] Kauffmann-Guerrero D, et al. Orphan Drugs in Development for the Treatment of Small-Cell Lung Cancer: Emerging Data on Lurbinectedin. Lung Cancer: Targets and Therapy, 2020; 11: 27–31.
[2] Gadducci A, et al. Trabectedin and lurbinectedin: Mechanisms of action, clinical impact, and future perspectives in uterine and soft tissue sarcoma, ovarian carcinoma, and endometrial carcinoma. Frontiers in Oncology, 2022; 12: 914342.
Lurbinectedin Preparation Products And Raw materials
Raw materials
Preparation Products
Lurbinectedin Suppliers
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- 15317222985
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View Lastest Price from Lurbinectedin manufacturers
- Product
- Lurbinectedin 497871-47-3
- Price
- US $6.00-1.00/KG
- Min. Order
- 1KG
- Purity
- 99%
- Supply Ability
- g-kg-tons, free sample is available
- Release date
- 2024-03-28
- Product
- Lurbinectedin 497871-47-3
- Price
- US $30.00-1.00/kg
- Min. Order
- 1kg
- Purity
- 0.99
- Supply Ability
- 10 tons
- Release date
- 2023-11-24