Lurbinectedin
- CAS No.
- 497871-47-3
- Chemical Name:
- Lurbinectedin
- Synonyms
- PM01183;PM 01183;PM-01183;Rubitidine;LURBINECTEDIN;Lurbinectidine;UNII-2CN60TN6ZS;Lurbinectedin (PM01183);Lurbinectedin Impurity;PM01183;PM-01183;PM 01183
- CBNumber:
- CB82628057
- Molecular Formula:
- C41H44N4O10S
- Molecular Weight:
- 784.88
- MDL Number:
- MFCD22665743
- MOL File:
- 497871-47-3.mol
| Density | 1.55±0.1 g/cm3(Predicted) |
|---|---|
| storage temp. | Store at -20°C |
| solubility | Soluble in DMSO |
| pka | 9.79±0.40(Predicted) |
| form | Solid |
| color | White to light yellow |
| NCI Dictionary of Cancer Terms | lurbinectedin |
| FDA UNII | 2CN60TN6ZS |
| NCI Drug Dictionary | lurbinectedin |
| ATC code | L01XX69 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |   GHS07,GHS09 |
|---|---|
| Signal word | Warning |
| Hazard statements | H410-H302-H400 |
| Precautionary statements | P273-P391-P501-P264-P270-P301+P312-P330-P501-P273-P391-P501 |
Lurbinectedin price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Biorbyt Ltd | orb573146 | Lurbinectedin >98% | 497871-47-3 | 5mg | $2839 | 2021-12-16 | Buy |
| ChemScene | CS-6323 | Lurbinectedin 99.91% | 497871-47-3 | 2mg | $3360 | 2021-12-16 | Buy |
| Biorbyt Ltd | orb573146 | Lurbinectedin >98% | 497871-47-3 | 10mg | $4173.5 | 2021-12-16 | Buy |
| Biorbyt Ltd | orb573146 | Lurbinectedin >98% | 497871-47-3 | 25mg | $5210.5 | 2021-12-16 | Buy |
| ChemScene | CS-6323 | Lurbinectedin 99.91% | 497871-47-3 | 100ug | $550 | 2021-12-16 | Buy |
Lurbinectedin Chemical Properties,Uses,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
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Hebei Yanxi Chemical Co., Ltd. | +8617531190177 | peter@yan-xi.com | China | 5857 | 58 |
| Henan Fengda Chemical Co., Ltd | +86-371-86557731 +86-13613820652 | info@fdachem.com | China | 20285 | 58 |
| BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD. | +86-18600796368 +86-18600796368 | sales@sjar-tech.com | China | 456 | 58 |
| BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19553 | 58 |
| CE Pharm Co.,Ltd | +86 13816833708 | binbin.lin@cepharm.cn | CHINA | 52 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32161 | 58 |
| Career Henan Chemica Co | +86-0371-86658258 +8613203830695 | laboratory@coreychem.com | China | 30239 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10473 | 58 |
| ChemExpress | +86-021-58950125 +86-021-58950125; | info@chemexpress.com | China | 778 | 58 |
| Beijing Mesochem Technology Co.,Ltd | +8613651027935 | rachel@mesochem.com | China | 191 | 58 |
Related articles
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View Lastest Price from Lurbinectedin manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2024-11-19 | Lurbinectedin
497871-47-3
|
US $2960.00-1480.00 / mg | 98.11% | 10g | TargetMol Chemicals Inc. | ||
 |
2024-11-18 | Lurbinectedin
497871-47-3
|
US $0.00 / g | 1g | More Than 99% | 100kg/Month | BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD. | |
 |
2024-10-25 | Lurbinectedin
497871-47-3
|
US $30.00-1.00 / kg | 1kg | 0.99 | 10 tons | Hebei Yanxi Chemical Co., Ltd. |
-
- Lurbinectedin
497871-47-3
- US $2960.00-1480.00 / mg
- 98.11%
- TargetMol Chemicals Inc.
-
- Lurbinectedin
497871-47-3
- US $0.00 / g
- More Than 99%
- BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.
-
- Lurbinectedin
497871-47-3
- US $30.00-1.00 / kg
- 0.99
- Hebei Yanxi Chemical Co., Ltd.