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.
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 |
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 |
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.
Related DNA/RNA Synthesis Products |
---|
DTP3 TFA
DTP3 TFA is a potent and selective GADD45β/MKK7 (growth arrest and DNA-damage-inducible β/mitogen-activated protein kinase kinase 7) inhibitor. |
Mating Factor α (1-6)
Mating Factor α (1-6) is a mating factor produced by α-mating type cells of Saccharomyces cerevisiae and an acts as an inhibitor of the initiation of DNA synthesis in the cells. |
Polynucleotide kinase
Polynucleotide Kinase is a DNA repair enzyme. |
Tetrapeptide
Tetrapeptide, an analogue of α-MSH, induces melanin synthesis. |
Branaplam hydrochloride
Branaplam hydrochloride is an orally active, brain-permeable, selective modulator of SMN2 splicing, with an EC50 of 20 nM for SMN, and enhances full-length SMN protein and prolongs survival in a mouse model of severe spinal muscular atrophy (SMA). Branaplam hydrochloride also inhibits hERG with an IC50 of 6.3 μM. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.