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Lurbinectedin

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Catalog No. T15793Cas No. 497871-47-3
Alias PM01183

Lurbinectedin (PM01183) is a DNA minor groove covalent binder that demonstrates effective anti-tumor activity.

Lurbinectedin

Lurbinectedin

😃Good
Purity: 98.11%
Catalog No. T15793Alias PM01183Cas No. 497871-47-3
Lurbinectedin (PM01183) is a DNA minor groove covalent binder that demonstrates effective anti-tumor activity.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
100 μg$198In StockIn Stock
1 mg$455In StockIn Stock
5 mg$1,180In StockIn Stock
10 mg$1,980In StockIn Stock
25 mg$3,880-In Stock
50 mg$5,230-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:98.11%
Appearance:Solid
Color:White to Yellow
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Product Introduction

Bioactivity
Description
Lurbinectedin (PM01183) is a DNA minor groove covalent binder that demonstrates effective anti-tumor activity.
Targets&IC50
RMG2:1.16 nM, RMG1:1.25 nM
In vitro
Lurbinectedin inhibits RMG1 and RMG2 cell growth (IC50: 1.25 and 1.16 nM, respectively). Lurbinectedin exhibits significant antitumor activity toward chemosensitive and chemoresistant human ovarian clear cell carcinoma (CCC) cells in vitro[1]. Lurbinectedin-DNA adducts in living cells give rise to double-strand breaks, triggering S-phase accumulation, and apoptosis. Lurbinectedin is a new synthetic tetrahydroisoquinoline alkaloid that is currently in phase I clinical development for the treatment of solid tumors. The potent cytotoxic activity of Lurbinectedin is ascertained in a 23-cell line panel with a mean GI50 value of 2.7 nM[2].
In vivo
Lurbinectedin inhibits tumor growth significantly with no weight loss of treated animals, in four murine xenograft models of human cancer[2]. Mouse CCC cell xenografts show that lurbinectedin significantly inhibits tumor growth. Lurbinectedin plus SN-38 causes a significant synergistic effect[1].
SynonymsPM01183
Chemical Properties
Molecular Weight784.87
FormulaC41H44N4O10S
Cas No.497871-47-3
Smiles[H][C@@]12Cc3cc(C)c(OC)c(O)c3[C@@]([H])(N1C)[C@@]1([H])N([C@H]2O)[C@@]2([H])COC(=O)[C@]3(CS[C@]1([H])c1c(OC(C)=O)c(C)c4OCOc4c21)NCCc1c3[nH]c2ccc(OC)cc12
Relative Density.1.55 g/cm3 (Predicted)
Storage & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 15 mg/mL (19.11 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.2741 mL6.3705 mL12.7410 mL63.7048 mL
5 mM0.2548 mL1.2741 mL2.5482 mL12.7410 mL
10 mM0.1274 mL0.6370 mL1.2741 mL6.3705 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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%
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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