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Lurbinectedin

Cat. No. M10037
Lurbinectedin Structure
Synonym:

PM01183; PM-1183; LY-01017; Tryptamicidin

Size Price Availability Quantity
5mg USD 3000  USD3000 In stock
10mg USD 4800  USD4800 In stock
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Quality Control & Documentation
Biological Activity

Lurbinectedin, also known as PM01183, is a marine-derived covalent DNA binder with potential antineoplastic activity. Lurbinectedin (PM01183) 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 significantly inhibits tumor growth in a mouse CCC cell xenografts.

Protocol (for reference only)
Cell Experiment
Cell lines CCC cells
Preparation method CCC cells (2×105) were incubated with lurbinectedin at the indicated concentrations for 48 hours. The cells were then fixed with 75% ethanol overnight at -20°C and stained with propidium iodide (PI; 50 μg/mL) in the presence of RNase A (100 μg/mL; Roth) for 60 minutes at 4°C. In each experiment, the cell cycle distribution was determined by analyzing 10,000 cells using a FACScan flow cytometer and Cell Quest software (Becton Dickinson, NJ, USA), as reported previously.
Concentrations -
Incubation time 48 hours
Animal Experiment
Animal models Five- to 7-week-old nude mice injected RMG1 cells
Formulation -
Dosages 0.180 mg/kg
Administration i.v. administered each week for 6 weeks
Chemical Information
Molecular Weight 784.87
Formula C41H44N4O10S
CAS Number 497871-47-3
Solubility (25°C) DMSO 1 μmol/L
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Ryoko Takahashi, et al. PLoS One. Preclinical Investigations of PM01183 (Lurbinectedin) as a Single Agent or in Combination with Other Anticancer Agents for Clear Cell Carcinoma of the Ovary

[2] J F M Leal, et al. Br J Pharmacol. PM01183, a new DNA minor groove covalent binder with potent in vitro and in vivo anti-tumour activity

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Keywords: Lurbinectedin, PM01183; PM-1183; LY-01017; Tryptamicidin supplier, DNA/RNA Synthesis, inhibitors, activators


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